International Journal of Applied Pharmaceutics <div align="justify"> <p align="justify">International Journal of Applied Pharmaceutics (Int J App Pharm) is a peer-reviewed, bimonthly (onward March 2017) open access journal devoted to the excellence and research in the pure pharmaceutics. This Journal publishes original research work that contributes significantly to further the scientific knowledge in conventional dosage forms, formulation development and characterization, controlled and novel drug delivery, biopharmaceutics, pharmacokinetics, molecular drug design, polymer-based drug delivery, nanotechnology, nanocarrier based drug delivery, novel routes and modes of delivery; responsive delivery systems, prodrug design, development and characterization of the targeted drug delivery systems, ligand carrier interactions etc. However, the other areas which are related to the pharmaceutics are also entertained includes physical pharmacy and API (active pharmaceutical ingredients) analysis. The Journal publishes original research work either as a Original Article or as a Short Communication. Review Articles on a current topic in the said fields are also considered for publication in the Journal.</p> </div> Innovare Academic Sciences Pvt Ltd en-US International Journal of Applied Pharmaceutics 0975-7058 AN UPDATED REVIEW ON THE APPLICATION OF DENDRIMERS AS SUCCESSFUL NANOCARRIERS FOR BRAIN DELIVERY OF THERAPEUTIC MOIETIES <p>It’s been nearly 100 y of effort to study the organization and role of the blood brain-barrier and still, we strive to find better techniques to overcome this barrier to deliver the drugs to the brain effectively with reduced systemic side effects. The advances in nanotechnology have given newer horizons in achieving this goal since the nano-scaled systems can modify an existing drug to have a high degree of sensitivity to the physiological conditions and specificity to reach the target organ. Among the various nanocarriers, dendrimers owing to their unique physical and chemical characteristics, represent a potential therapeutic tool in biomedical and pharmaceutical science. Dendrimers, an established polymeric nanocarrier system of the time, can deliver both drugs and genetic material and are being extensively studied to target the brain. The surface modification of dendrimers can reduce their innate toxicity problems and increase the therapeutic efficacy of brain disorders. This review article is an attempt to update on the potential of dendrimers explored in the past five years as a drug delivery avenue that can be considered as a promising solution in the management of a wide range of disorders affecting the central nervous system, including neoplastic, degenerative, and ischemic conditions. The following search criteria were used to expand the review article with the keywords dendrimers, novel drug delivery, nanoparticles, site-specific drug delivery etc.</p> SARANYA SASI SHARON KUNNATH JOSEPH ARYA MANGALATH ARIAN SACHIN THOMAS AMRUTHA V. U. ARYA G. K. SREEJA C. NAIR Copyright (c) 2021 Saranya Sasi, Sharon Joseph, Arya Mangalath , Sachin Thomas, Amrutha V U, Arya G K, sreeja c nair 2021-01-07 2021-01-07 1 9 10.22159/ijap.2021v13i1.39812 THE COSMETIC EFFECTS OF VARIOUS NATURAL BIOFUNCTIONAL INGREDIENTS AGAINST SKIN AGING: A REVIEW <p>Nutricosmetics have emerged to indicate the health benefits of the products that create beauty from inside to outside. Nutricosmetic is the latest trend in the beauty industry. Cosmeceuticals are commonly used in skincare regimens to maintainhealthy skin and improve visible signs of aging. Natural products that target skin have gained great attention due to the general belief that they are harmless. A review of the biomedical literature was conducted using peer-reviewed journal articles toidentify laboratory, animal, and clinical studies that have evaluated recent breakthroughs in the biological properties and potential dermatologic uses of the different natural bioactive ingredients used in nutricosmetics and Cosmeceuticals. Bioactive ingredients used in Nutri-cosmeceutical products are derived from collagen, peptides, proteins, vitamins, carotenes, minerals, omega‐3 fatty acids and plant extracts. These ingredients have been shown to provide dermatologic benefits with potential applications for skin regeneration, photoprotection, wound healing, and more.The information provided by this article is valuable to get the picture of the latest trends. In addition, it might be helpful for clinicians and related manufacturing companies. Despite several developments in this field, extensive research is required for performing successful and precise clinical trials in the future. Further improvements would enable the researchers to develop new products in this field.</p> WISAM NASER Copyright (c) 2021 wisam 2021-01-07 2021-01-07 10 18 10.22159/ijap.2021v13i1.39806 DETAILED VIEW ON REPURPOSED DRUGS, TRACKING OF VACCINES,AND BRIEF VIEW ON PROPHYLACTIC NANOMEDICINES AS AN ALTERNATIVE APPROACH AND PATIENT CARE FOR COVID-19 <p>In December 2019, a rare case of pneumonia was reported in Wuhan, China. This was later analyzed and known to have similar characteristics as viral pneumonia caused by a novel coronavirus. Later, on 11 February 2020, the World Health Organization (WHO) officially named the disease as COVID19. The Severe acute respiratory syndrome coronavirus 2(SARS-CoV-2) ought to taint both the upper respiratory tract and the lower respiratory tract. This COVID-19 is spreading quickly with an immense rise in cases around the world. This infection's mechanism stays obscure, and the medications explicit for the infection were not grown at this point. Infection is highly contagious. Severe Acute Respiratory Syndrome Coronavirus 2(SARS-CoV-2) is one of seven kinds of crown infection, including the one which causes severe maladies like Middle East respiratory disorder (MERS) and abrupt, intense respiratory syndrome(SARS). Since its revelation, the infection has spread and has caused anxiety and fear among people. Recent vaccines are tracked, and clinical trials can bring an immediate protocol on a medication approach. By including different therapeutic approaches, it is easier to combat the disease quickly. With very low mortality and high transmission rate, new approaches to vaccines and nanomedicines bring down the spread. Controlled patient care is also crucial. On 11 March, the World Health Organization (WHO) declared the disease as 'global pandemic’. COVID-19, therefore, poses a significant threat to global public health.</p> <p>This article reviews the epidemiology, pathogenesis, and diagnostic methods. The review also focuses on repurposed drugs, traced vaccines, and a quick view of prophylactic nanomedicines as an alternative for COVID 19. For this review, the complete database has been collected from various search engines such as PubMed, ScienceDirect, Scopus, Elsevier, etc., from the year 2001-2020 using the following keywords.</p> KRISHNANJANA S. NAIR SHIVALI KAMATH ARYA RAJAN SACHIN THOMAS ASWIN D. SUBIN MARY ZACHARIAH Copyright (c) 2020 SUBIN MARY ZACHARIAH, KRISHNANJANA S NAIR, SHIVALI KAMMATH, ARYA RAJAN, SACHIN THOMAS, ASWIN D 2021-01-07 2021-01-07 19 26 10.22159/ijap.2021v13i1.39705 A REVIEW ON POLOXAMER AND HYDROXY PROPYL METHYL CELLULOSE COMBINATION AS THERMORESPONSIVE POLYMERS IN NOVEL OPHTHALMIC IN SITU GEL FORMULATION AND THEIR CHARACTERIZATION <p>Poor bioavailability is one of the most significant problems in the delivery of the ocular drug system. Ophthalmic ointments, solutions and suspensions are the most frequently used dosage forms to treat ocular disease, and their effectiveness as a drug are compromised by several limitations that lead to poor ocular bioavailability. <em>In situ </em>gel is one of the most promising strategy and solutions to improve the ocular bioavailability of drugs. The purpose of this review is to discuss the formulation and characterization of <em>in situ </em>gel. This review is written based on the data or information obtained by using several search engines and several scientific journals, focused on Poloxamer 407 and Hydroxy Propyl Methyl Cellulose (HPMC) bases combination.</p> <p>Active ingredients to treat ocular disease such as Ciprofloxacin, Fluconazole and Ofloxacin can be formulated with the combination of Poloxamer 407 as polymer gelling agent and HPMC as viscosity enhancer to produce good quality <em>in situ </em>gel dosage forms. The <em>in situ </em>gel dosage forms can be a promising alternate solution for the ophthalmic delivery system.</p> INSAN SUNAN KURNIAWANSYAH TAOFIK RUSDIANA IYAN SOPYAN ANAS SUBARNAS Copyright (c) 2020 Insan Sunan Kurniawansyah 2021-01-07 2021-01-07 27 31 10.22159/ijap.2021v13i1.39697 PHARMACY PROFESSIONS IN INDIADURING COVID-19 PANDEMIC: PRESENT STATUS, FUTURE CHALLENGES AND A WAY FORWARD <p>People in every country became exposed to COVID-19 pandemic and cannot able to find a right solution and strategies to overcome from it. Pharmacy is the most important, dynamic and versatile health care profession in the world, whereas its scope and importance are always being emerging at any situation. Pharmacy professionals (PPs) working proactively for the public even in this pandemic situation. Since dependency is high, the responsibility and preference also high for PPs especially in this pandemic situation. Current status in pharmacy education and emerging future challenges of PPs in all aspects, particularly in thispandemic situation were addressed based on observational studies among various pharma industries and published news of Pharmacy Council of India (PCI). While in the development phase it has crossed many barriers, not only in the economic level,but also involves regulations, duration, process controls, legal hurdles and situational defects. The purpose of this review discusses the evolution and updates in pharmacy, education, pharmacy practice, regulations, and types of challenges along with recommendations for PPs in India in light of the COVID-19 pandemic.</p> <p>This review was carried out to summarize knowledge about the updates and challenges in pharmacy professions in all aspects. Sources were retrieved from relevant guidelines and published articles in Google scholar, Pubmed and Science direct of articles up to June 2020. The keywords used for gathering information were listed below.</p> VIGNESH M. GANESH G. N. K. Copyright (c) 2020 Vignesh M 2021-01-07 2021-01-07 32 35 10.22159/ijap.2021v13i1.39688 NOVEL DELIVERY APPROACHES OF CO-TRIMOXAZOLE FOR RECREATING ITS POTENTIAL USE-A REVIEW <p>Co-trimoxazole appropriates to category of broad-spectrum antimicrobial. They are active upon administration <em>in vitro</em> against an extensive collection of microorganisms. Their application in medical field has roughly spanned over decade now. There are numerous approaches that were progressed for improving their effectiveness towards their antimicrobial potency. However, routine use of this could accelerate the chance of bacterial resistance, and portrait it ineffective when required to treat infection. Consequently, newer investigations are necessary to keep the drug effective by minimise the development of resistance and maximise its safe use. Safe use is meant by safe delivery of drug in low dose, low frequency at the targeted molecule by effective ways. This can be achieved by using nanocarrier systems as they possess smart characteristics of effective drug delivery. These nanocarrier systems are including nanoparticle, liposomes, nanogels etc. Present review article deals with the historical perspectives with regards to co-trimoxazole, their mechanism of act/resistance and spectrum of activity in first section. In second portion different novel carriers, importance and application of nanogels, rational for co-trimoxazole nanogels are discussed. In conclusion, different literatures have proved the efficacy of nanogels in delivery of antimicrobial drug similar to co-trimoxazole. In the present time very less data is available for delivery of this drug with novel carriers. Therefore, this review aims to encourage researchers for creating some new findings in this perspective.</p> ROHITAS DESHMUKH RANJIT K. HARWANSH MAYUR SHARMA SWARNALI DAS PAUL Copyright (c) 2020 Rohitas Deshmukh, Ranjit K. Harwansh, mayur Sharma, Swarnali Das Paul 2021-01-07 2021-01-07 36 42 10.22159/ijap.2021v13i1.39623 SYSTEMATIC REVIEW: COCRYSTAL AS EFFORTS TO IMPROVE PHYSICOCHEMICAL AND BIOAVAILABILITY PROPERTIES OF ORAL SOLID DOSAGE FORM <p>Water solubility and low bioavailability of active pharmaceutical ingredients are some of the main challenges in the process of developing new drugs, especially drugs in oral solid dosage forms. One way to improve drug solubility is the principle of cocrystallization. Cocristallyzation itself is the process of combining the active ingredients of a less water-soluble drug with a coformer so that it becomes more soluble. Pharmaceutical cocrystal provides benefits to improve physicochemical properties without affecting its pharmacological properties. In this review, we have reviewed literature discussions and research that discuss co-crystallization as an aid to improve the physicochemical and bioavailability of drugs and also discuss some drugs in the form of cocrystal and their improvement in physicochemical-biopharmaceutical properties. The main references data used in this review are research journals published in the past 10 y (2010-2020) using keywords: cocrystal, physicochemistry, bioavailability, and solid dosage form, and using google scholar as a database. Discussion on the effect of cocrystal on physicochemical properties and bioavailability of drugs was produced. The method of producing cocrystal and its characterization was also discussed. Cocrystal offers a promising approach to improve the physicochemical properties of API. The benefits of cocrystal can be observed through increased solubility, dissolution rate, permeability, bioavailability, drug stability, and tabletability.</p> IYAN SOPYAN ALVIN B. INSAN SUNAN K. S. CIKRA IKHDA N. H. S. SANDRA MEGANTARA Copyright (c) 2020 iyan sopyan, Insan Sunan KS, Insan Sunan KS 2021-01-07 2021-01-07 43 52 10.22159/ijap.2021v13i1.39594 CORRELATION OF GENETIC POLYMORPHISM IN UGT1A1, SLCO1B1, NAT2, AND CYP2E1 WITH HEPATOTOXICITY <p>Tuberculosis (TB) has been identified as one of the most highly infectious diseases in the world. Tuberculosis can be identified as pulmonary or extrapulmonary. Therapy for TB is a combination of several drugs in one treatment. The effectiveness and toxicity of TB therapy may differ in each patient because of some risk factors, especially genetic variations. This review describes several genes that can affect the effectiveness and toxicity of antituberculosis drugs, namely <em>UGT1A1</em>, <em>SLCO1B1</em>, <em>NAT2</em>, and <em>CYP2E1</em>. This review was conducted utilizing the PubMed database, with keywords used as follows: polymorphism, antituberculosis, and tuberculosis. The presence of polymorphisms in these genes can result in hepatotoxicity and decreased drug bioavailability. Therefore, polymorphisms in these genes can determine the effectiveness of TB therapy.</p> GITA WIDI SETYOWATI NURUL ANNISA MELISA I. BARLIANA Copyright (c) 2021 Melisa Intan Barliana, Gita Widi Setyowati, Nurul Annisa 2021-01-07 2021-01-07 53 58 10.22159/ijap.2021v13i1.39540 NOVASOME: A PIONEERING ADVANCEMENTIN VESICULAR DRUG DELIVERY <p>Pharmaceutical research has developed various new types of innovative forms of drug delivery. Advancement in current drug delivery methods has led to the development of numerous new revolutionary technologies that support safe and efficient formulations over existing ones. Novasome technology is one of the latest liposome developments that have overcome many of the liposomal drug delivery system-related problems. This provides a seven bilayer membrane which is capable of absorbing water-soluble as well as insoluble drugs. The improved efficiency of entrapping drugs with good encapsulation features enables better frequency of dosing, which can be accomplished through the high shear system. These find their applications in diverse fields such as cosmetics, chemicals, personal care, food, pharmacy, and agrochemicals. Several products have already been launched into the market using this technology with an additional launch plan. Due to its depth of penetration, novasomes have been one of the most popular derma cosmetics. It is being studied continuously to obtain improved release characteristics. The prospect of drug delivery and targeting using novasomes is an important area of research and development. This review pinpoints the various aspect of the novasome and will be a milestone for the researchers in the area of drug delivery.</p> ASLAM ABDUL RAHIMAN C.A. KARTHIK KRISHNAN SREELEKSHMI A.S. ARJUN K.K. SREEJA C. NAIR Copyright (c) 2021 sreeja c nair, ASLAM ABDUL RAHIMAN C A, KARTHIK KRISHNAN, SREELEKSHMI A S, ARJUN K K 2021-01-07 2021-01-07 59 64 10.22159/ijap.2021v13i1.39528 HYDROGEL: RESPONSIVE STRUCTURES FOR DRUG DELIVERY <p>Hydrogels are water-swollen 3D networks made of polymers, proteins, small molecules, or colloids. They are porous in structure and entrap/encapsulate large amounts of therapeutic agents and biopharmaceuticals. Their unique properties like biocompatibility, biodegradability, sensitivity to various stimuli, and the ability to be easily conjugated with hydrophilic and hydrophobic drugs with a controlled-release profile make hydrogels a smart drug delivery system. Smart hydrogel systems with various chemically and structurally responsive moieties exhibit responsiveness to external stimuli including temperature, pH, ionic concentration, light, magnetic fields, electrical fields, and chemical and biological stimuli with selected triggers includes polymers with multiple responsive properties have also been developed elegantly combining two or more stimuli-responsive mechanisms. This article emphasized the types, features, and various stimuli systems that produce responsive delivery of drugs.</p> MALLIKARJUN P. N. ANUSHA S. SAI NANDINI V. RAMA RAO B. KAMALA KUMARI P. V. SRINIVASA RAO Y. Copyright (c) 2021 Mallikarjun P.N. 2021-01-07 2021-01-07 65 76 10.22159/ijap.2021v13i1.39507 IMPORTANCE OF NANOCARRIERS AND PROBIOTICS IN THE TREATMENT OF ULCERATIVE COLITIS <p>Ulcerative colitis (UC) is an inflammatory chronic disease primarily affecting the colonic mucosa; the extent and severity of colon involvement are variable. Ulcerative colitis is identified by mucus diarrhea, tenesmus, bowel distension, and anemia. 5-aminosalicylic acid drugs, steroids, and immune suppressants are used for the therapy of ulcerative colitis. The mainchallenges in the management of thediseaseare drug-related side-effects and local targeting. To overcome these challengesprobiotics and micro and Nanoparticulate systemauspiciousapproaches to overcome drug-related adverse side effects and local targeting.Upon ingestion, the probiotics can result in beneficial health effects. Probiotics and micro and nanoparticulate approaches for suitable targeting and overcome the drug-associated side effect. Probiotics are mainly used as gut modulators but are also nowadays explored for their use in ulcerative colitis.The current therapeutic goals are to achieve clinical remission along with mucosal healing, avoidance of complications such as side effects of the drug and to improve the quality of life. The use of probiotics to increase the health of the intestine and used to block or manage intestinal disorders. They may prevent the induction of inflammatory reactions. Probiotics must be inspected for efficacy in the prevention and management of a wide spectrum of gastrointestinal diseases, like antibiotic-associated diarrhea.Micro and Nanoparticulate drug delivery system has been achieving huge importance for targeting of the drug to colon locally at a controlled and sustained rate.</p> VANDANA THAKUR BHUPENDRA SINGH ANKITA SHARMA NISHA KUMARI INDER KUMAR KRITIKA VERMA ARVIND KUMAR SUSHMITA RANA Copyright (c) 2021 vandana Thakur 2021-01-07 2021-01-07 77 85 10.22159/ijap.2021v13i1.37510 IN SITU GEL POLYMERS: A REVIEW <p>In situ gels have become one of the most prominent and accessible systems. These systems have several advantages like simple manufacturing, easy to use, improved adherence, and patient comfort by minimizing drug administration frequency by its unique characteristic features of sol to gel transition. In the 'sol-gel' method, the precursor goes through hydrolysis and polymerization or condensation to produce a colloidal suspension or solution. As they can administer in solution form, these in situ gelling systems undergo gelation at the achievement site. Some researchers recently developed in situ gelling systems of liposomes, microspheres, nanoemulsions, nanospheres, etc. This review mainly focused on the introduction, advantages, disadvantages, types of polymers, and suitable characteristics for preparing in situ gels.</p> MOUNIKA KONATHAM MOUNIKA TEJASWI GORLE NAVEEN PATHAKALA VASUDHA BAKSHI YASO DEEPIKA MAMIDISETTI PRIYANKA CHINTHAKINDI RAJENDRA KUMAR JADI Copyright (c) 2021 RAJENDRA KUMAR JADI 2021-01-07 2021-01-07 86 90 10.22159/ijap.2021v13i1.39504 REVIEW ON EVALUATING THE ROLE OF NSAIDS FOR THE TREATMENT OF ALZHEIMER'S DISEASE <p>Recently, several studies have been reported that nonsteroidal anti-inflammatory drugs can fight against neurodegenerative disorders by various mechanisms. Currently, available therapies of neurodegenerative disorders (NDs) provide only symptomatic relief. This is the point at which we need an alternative that acts on the root cause of disease. Parkinson’s disease and Alzheimer’s disease are the two NDs concentrated here. Since the drug profile is already known, drug repurposing is a promising technique in research, thereby reducing the cost and period effectively. Epidemiological studies on various nonsteroidal anti-inflammatory drugs (NSAIDs) showed good results, but when it came to clinical studies the results are found to be poor. Hence, it can be concluded that NSAIDs provide its neuroprotective activity on its long-term use only, as the brain accessibility of this kind of drug is poor due to its lower lipophilicity.</p> KRISHNENDU P. R. ARJUN B. VIBINA K. NIVEA CLEO T. S. DRISYA N. K. RADHIKA MOHANDAS SUBIN MARY ZACHARIAH SUBIN MARY ZACHARIAH Copyright (c) 2021 subin mary zachariah 2021-01-07 2021-01-07 91 94 10.22159/ijap.2021v13i1.39928 MICROFLUIDIC DEVICES AS A TOOL FOR DRUG DELIVERY AND DIAGNOSIS: A REVIEW <p>Microfluidic devices are a good example of the collaboration of chemical, biological, and engineering sciences. Microfluidic devices emerge as an in fluent technology which provides an alternative to conventional laboratory methods. These devices are employed for the precise handling and transport precise quantities of drugs without toxicity. This system is emerging as a promising platform for designing advanced drug delivery systems and analysis of biological phenomena on miniature devices for easy diagnosis. Microfluidics enables the fabrication of drug carriers with controlled geometry and specific target sites. Microfluidic devices are also used for the diagnosis of cancer circulating tumor cells. In the current review, different microfluidic drug delivery systems and diagnostic devices have described.</p> ISHA SHARMA MONIKA THAKUR SHAVETA SINGH ASTHA TRIPATHI Copyright (c) 2021 Isha Sharma 2021-01-07 2021-01-07 95 102 10.22159/ijap.2021v13i1.39032 STUDY OF ISOTONICITY AND OCULAR IRRITATION OF CHLORAMPHENICOL IN SITU GEL <p><strong>Objective: </strong>The objective of this study was to find out the isotonicity of chloramphenicol ophthalmic <em>i</em><em>n situ</em> gel and to know the irritating effect of its in the eyes of test animals, so it can be to maximize absorption of the drug in the eye, minimize drug loss before corneal penetration and safe to used.</p> <p><strong>Methods: </strong>This study were started by making four aseptic formulations of <em>i</em><em>n situ</em> gel preparations with a comparison of the baseline concentrations of different Poloxamer 407 and HPMC, F1 (5: 0.45), F2 (10: 0.45), F3 (5: 1) and F4 (10: 1). Four aseptic of <em>i</em><em>n situ</em> gel preparations, followed by a qualitative isotonicity test using blood cells to see the comparison between control and test preparations, and ocular irritation test using the draize test method to determine the presence or absence of the irritation.</p> <p><strong>Results: </strong>The results obtained from the isotonicity test showed that the four preparations have normal blood cells that similar with isotonic control solution; therefore, it can be said that the preparations have been made isotonic.</p> <p>The results of the ocular irritation test using the draize test method showed for each category, such as cornea, iris, conjunctiva and edema were zero. A zero value on the cornea indicates no ulceration or opacity, and the iris, conjunctiva and edema were normal. <strong>Conclusion: </strong>Chloramphenicol <em>i</em><em>n situ</em> gel are isotonic and do not cause irritation to the rabbit's eyes, so they are safe to use and the formulation can be used for further research until the final goal is obtained.</p> INSAN SUNAN KURNIAWANSYAH TAOFIK RUSDIANA ZAHRA DZAKIRAH ABNAZ IYAN SOPYAN ANAS SUBARNAS Copyright (c) 2021 INSAN SUNAN KURNIAWANSYAH, TAOFIK RUSDIANA, ZAHRA DZAKIRAH ABNAZ, IYAN SOPYAN, ANAS SUBARNAS 2021-01-07 2021-01-07 103 107 10.22159/ijap.2021v13i1.39925 EXPERIMENTAL DEVELOPMENT AND MOLECULAR DOCKING: NANOSTRUCTURED LIPID CARRIERS (NLCs) OF COENZYME Q10 USING STEARIC ACID AND DIFFERENT LIQUID LIPIDS AS LIPID MATRIX <p><strong>Objective: </strong>To develop coenzyme Q10 (co-Q10) nanostructured lipid carriers (NLCs) using stearic acid (SA) and various liquid lipids with different lipophilicity as well as highlights the use of <em>in silico</em> studies for predicting and elucidating the interaction of drug-lipid used as carries in NLCs, at the molecular level.</p> <p><strong>Methods: </strong>The co-Q10 NLCs were prepared using SA as solid lipid and oleic acid (OA), isopropyl myristate (IPM), as well as isopropyl palmitate (IPP) as liquid lipids by the high shear homogenization method. Firstly, the formulas were optimized by the appropriate required HLB (rHLB). The optimized NLCs were characterized in the particle size, distribution of particle size, zeta potential, crystallinity behavior, Fourier transform infrared (FT-IR) spectra, morphology, entrapment efficiency (EE), drug loading (DL), and pH value. The interaction of drug-lipids <em>in silico</em> was studied using the AutoDock Vina program.</p> <p><strong>Results: </strong>The co-Q10 NLCs using SA and the various liquid lipid possessed the mean particle size, polydispersity index (PDI), zeta potential, EE, DL, and pH values were 180 to 350 nm,&lt;0.5,&lt;-30 mV, 83 to 88%, 10 to 11%, and 5.0 to 5.6, respectively. The EE and DL of co-Q10 NLCs increased with decreasing in binding energy (∆G) <em>in silico</em>.</p> <p><strong>Conclusion: </strong>The co-Q10 NLCs using SA as solid lipid and OA, IPM, as well as IPP as liquid lipids were developed successfully. Furthermore, <em>in silico</em> study by molecular docking is a potential approach in predicting and elucidating the interaction of drug-lipid in the development of NLCs formulation.</p> NI LUH DEWI ARYANI SISWANDONO WIDJI SOERATRI FANNY PUTRI RAHMASARI DIAN RIZKI KARTIKA SARI Copyright (c) 2021 Ni Luh Dewi Aryani, SISWANDONO, WIDJI SOERATRI, FANNY PUTRI RAHMASARi, DIAN RIZKI KARTIKA SARI 2021-01-07 2021-01-07 108 116 10.22159/ijap.2021v13i1.39890 COMPARATIVE DISSOLUTION STUDIES OF WARFARIN SODIUM TABLETS: INFLUENCE OF AGITATION RATE, DISSOLUTION MEDIUM, AND USP APPARATUS <p><strong>Objective: </strong>The aim of this study was to carry out comparative dissolution studies with warfarin sodium reference tablets under the hydrodynamic environments generated by the USP basket and paddle apparatus and flow-through cell using different agitation rates and dissolution media.</p> <p><strong>Methods: </strong>Dissolution profiles were obtained with the USP basket and paddle apparatus at 50, 75, and 100 rpm and 900 ml of water as dissolution medium. After this, dissolution profiles of warfarin sodium were obtained with the USP paddle apparatus and flow-through cell method using 0.1 N hydrochloric acid, acetate buffer pH 4.5, phosphate buffer pH 6.8, and water. Spectrophotometric determination at 308 nm was carried out during 30 min. Dissolution profiles were compared with model-independent and model-dependent approaches.</p> <p><strong>Results: </strong>Significant differences were found with mean dissolution time and dissolution efficiency at 50 and 75 rpm (*P&lt;0.05). Makoid-Banakar was the best-fit model used to describe the <em>in vitro</em> release performance of warfarin sodium with 50-100 rpm and the USP basket and paddle apparatuses. Significant differences in all calculated parameters were found (*P&lt;0.05) excepting percent dissolved at 30 min with 0.1 N hydrochloric acid and phosphate buffer pH 6.8.</p> <p><strong>Conclusion: </strong>More research is necessary to identify the <em>in vitro</em> release performance of poorly soluble drugs under available USP apparatuses considering factors as agitation rate and kind of dissolution media. The knowledge of the <em>in vitro</em> release performance of reference drug products is important for the design of better generic formulations</p> JOSE RAUL MEDINA LOPEZ LUIS DANIEL MAZON ROMAN JUAN MANUEL CONTRERAS JIMENEZ JUAN CARLOS RUIZ-SEGURA Copyright (c) 2020 José Raúl Medina-López, Luis Daniel Mazón-Román, Juan Manuel Contreras-Jiménez, Juan Carlos Ruiz-Segura 2021-01-07 2021-01-07 117 123 10.22159/ijap.2021v13i1.39842 DETERMINATION OF CARBOHYDRATES CONTENT IN GENTIANA CRUCIATA L. BY GC/MS METHOD <p><strong>Objective: </strong>Thus, the aim of our research was to determine the qualitative composition and quantitative content of carbohydrates in the studied plant material with the prospect of its application as a medicinal plant raw material.</p> <p><strong>Methods: </strong>The carbohydrates of the herb of <em>Gentiana cruciata</em> L. determined by GC/MS method. Identification of monosaccharides was based on comparing their retention times with retention times of standards of the mass spectral library NIST 02. Quantification was done by using sorbitol added to the sample.</p> <p><strong>Results: </strong>The quantitative content of 4 free carbohydrates such as D-saccharose (38.39 mg/g), D-Pinitol (12.01 mg/g), D-glucose (10.05 mg/g) and D-fructose (1.69 mg/g) was established in the herb of <em>Gentiana cruciata</em> L. Also, this method established the qualitative composition and quantitative content of eight carbohydrates (monosaccharides and their derivatives after hydrolysis): D-glucose (29.66 mg/g), D-Pinitol (22.24 mg/g), L-arabinose (4.26&nbsp;mg/g), D-galactose (3.55 mg/g), D-xylose (1.80 mg/g), L-rhamnose (1.49 mg/g), D-Dulcitol (0.76 mg/g) and D-mannose (0.44 mg/g).</p> <p><strong>Conclusion: </strong>The results of the study showed that carbohydrates from the <em>Gentiana cruciata</em> L. can be used as important resources of new ingredients for the pharmaceutical industry.</p> LILIIA BUDNIAK LIUDMYLA SLOBODIANIUK SVITLANA MARCHYSHYN PAVLINA KLEPACH YANA HONCHARUK Copyright (c) 2021 Liliia Budniak, Liudmyla Slobodianiuk, Yana Honcharuk 2021-01-07 2021-01-07 124 128 10.22159/ijap.2021v13i1.39820 CHITOSAN NANOPARTICLES MEDIATED DELIVERY OF MIR-106B-5P TO BREAST CANCER CELL LINES MCF-7 AND T47D <p><strong>Objective: </strong>The development of nanomedicine, such as miRNA transfection to cancer cells,has widely gained interest in the past decade. Unfortunately, miRNA tends to decay easily by the cellular enzymatic process and requires a carrier. As a cationic biopolymer, chitosan is widely known as a non-viral vector. However, research about chitosan as a miRNA delivery system remains limited. This study aimed to investigate the effect and characters of synthetic miRNA loaded chitosan nanoparticles on breast cancer cell lines.</p> <p><strong>Methods: </strong>To obtain the nanocomplex, chitosan-antimiR-106b-5p was formulated using natriumtripolyphosphate through ionic gelation methods. The nanochitosan formula was characterized by using gel electrophoresis; Nano Quant for encapsulation of entrapment quantification; morphology appearance as viewed by Scanning Electron Microscope (SEM), nanochitosan size analysis; <em>in vitro</em> analysis using MCF-7 and T47D breast cancer cell lines; <em>in silico</em> prediction of possible gene target; polymerase chain reaction analysis and gel electrophoresis for E2F1/GAPDH expression.</p> <p><strong>Results: </strong>The efficiency entrapment value was 96.7%, particle size analysis was 458±11.79 nm, and polydispersity index (PDI) was 0.65±0.07, with spherical morphology as viewed in SEM. There was no significant difference between the nanochitosan supplemented group and the control group in MCF-7 cells (<em>p</em>=0.067). However, the ratio of E2F1 to GAPDH was significantly lower than the control group after nanochitosan antimiR-106b-5p was loaded at concentration 140 nmol (<em>p</em>=0.022) and 35 nmol (<em>p</em>=0.016).</p> <p><strong>Conclusion: </strong>Our nanochitosan formula is non-toxic to use in MCF-7 cell lines. Most importantly, as the formula was conjugated to synthetic antimiR-106b-5p, the E2F1 expression decreased.</p> LEONNY DWI RIZKITA YSRAFIL RONNY MARTIEN INDWIANI ASTUTI Copyright (c) 2021 Leonny Dwi Rizkita; YSRAFIL YSRAFIL; RONNY MARTIEN, INDWIANI ASTUTI 2021-01-07 2021-01-07 129 134 10.22159/ijap.2021v13i1.39749 MUCOADHESIVE POLYMERIC FILMS OF ACYCLOVIR PRONIOSOMES FOR BUCCAL ADMINISTRATION <p><strong>Objective: </strong>The aim of the present work was to formulate and evaluate proniosomes of the poorly soluble drug, acyclovir incorporated in mucoadhesive polymeric films for improved buccal mucosal permeability of the drug while achieving prolonged release.</p> <p><strong>Methods: </strong>Acyclovir was formulated as proniosomes using Span 60 and cholesterol. The prepared proniosomes were loaded into mucoadhesive polymeric films prepared with varying quantities of carbopol 934P and HPMC K15M. The proniosome incorporated films were evaluated for physicomechanical characters, mucoadhesion, swelling index, drug content, <em>in vitro</em> drug release and <em>ex vivo </em>permeation through porcine buccal mucosa.</p> <p><strong>Results: </strong>Hydration of the proniosomes produced spherical vesicles or niosomes, which was confirmed by Scanning Electron Microscopy. The optimized formulation selected on the basis of vesicle size, entrapment efficiency PDI, Zetz potential and <em>in vitro</em> drug release was selected for incorporation into mucoadhesive polymeric films. All the films showed excellent physicomechanical characters. Formulations with higher proportions of carbopol produced slower <em>in vitro</em> drug release. The kinetics of release of drug from all the formulations appeared to be zero-order based on their regression coefficient values. Comparative evaluation of <em>ex vivo </em>permeation from niosomal and non-niosomal films indicated that the former demonstrated improved mucosal permeation and drug release was also sustained for the 8 h period.</p> <p><strong>Conclusion: </strong>Mucoadhesive films impregnated with acyclovir loaded proniosomes could be a potential approach for buccal delivery of acyclovir for improving its absorption and bioavailability<em>.</em>&nbsp;</p> DEEKSHA U. SUVARNA MARINA KOLAND ANANTH PRABHU SINDHOOR S. M. Copyright (c) 2021 Marina Koland, Deekhsa U Suvarna, ANANTH PRABHU, Sindhoor S. M 2021-01-07 2021-01-07 135 143 10.22159/ijap.2021v13i1.39657 TOPICAL DRUG DELIVERY OF GOSSYPIN FROM PRONIOSOMAL GEL FORMULATIONS: IN VITRO EFFICACY AGAINST HUMAN MELANOMA CELLS <p><strong>Objective: </strong>This work aimed to establish and formulate the gossypinproniosomal gel drug delivery system.</p> <p><strong>Methods: </strong>Gossypin-loaded proniosomal gels (GPG) was prepared using specific non-ionic surfactants (Spans), followed by particle size (PS), entrapment efficiency (percent EE), <em>in vitro</em>, ex-vivo drug release, and <em>in vitro</em> efficacy of Gossypin against human melanoma cells (A-375).</p> <p><strong>Results: </strong>The results showed that the percentage EE for the GPG is appropriate (81.3 %–95.5 %) and they are Nano-sized (189.3–912.0 nm) and the gels diffusion provided the desired sustaining effect for GPG-F7 formulation (75.5 percent). The GPG reported cell viability of 14.9±2.3 percent compared with 16.1±1.1 percent for free Gossypin at the maximum dose of 100 μg/ml for A-375 human melanoma cells after 24 hr incubation time. No major changes were seen in the percentage EE, PS of GPG after storage for 90d, in the physical stability report.</p> <p><strong>Conclusion: </strong>The results obtained suggest that the proniosomal drug delivery system can enhance the flux to the skin and achieve the ideal Gossypin sustainability effect. Consequently, the use of proniosomal gel may be advantageous with regard to the topical delivery of Gossypin for melanoma treatment management.</p> JAMPALA RAJKUMAR G.V. RADHA S. GANAPATY Copyright (c) 2021 rajkumar jampala 2021-01-07 2021-01-07 144 152 10.22159/ijap.2021v13i1.39609 RP-HPLC (STABILITY-INDICATING) BASED ASSAY METHOD FOR THE SIMULTANEOUS ESTIMATION OF DORAVIRINE, TENOFOVIR DISOPROXIL FUMARATE AND LAMIVUDINE <p><strong>Objective: </strong>In this study, a RP-HPLC (stability-indicating) based assay method for the estimation of doravirine (DRV), tenofovir disoproxil fumarate (TFF) and lamivudine (LMV) simultaneously in the tablets was described.</p> <p><strong>Methods: </strong>The simultaneous analysis of DRV, TFF and LMV was done with HPLC system (Agilent 1100 series) and Luna Phenomenex C18 (250 mm × 4.6 mm × 5 μ) column with isocratic mobile phase (35% volume ratio of methanol and 65% volume ratio of 20 mmol ammonium formate, pH 5). Validation of assay method was done on sensitivity, linearity, accuracy, selectivity, precision, robustness and specificity.</p> <p><strong>Results: </strong>The calibration curves were linear through the range of 25-200 µg/ml for DRV and 75-600 µg/ml for TFF and LMV. The percent relative standard deviation for intraday variation/precision, interday variation/precision, intermediate precision/ruggedness and robustness were lower than 2%. The recovery of LMV (99.09-99.76%), TFF (99.10-99.41%) and DRV (98.65-99.28%) confirmed the good accuracy. The stability of LMV, TFF and DRV in 0.1N NaOH, 3% peroxide, 0.1 N HCl, UV light and dry heat of 60 °C was determined.</p> <p><strong>Conclusion: </strong>The results have allowed the method to be implemented in the tablets to quantify DRV, TFF, and LMV.</p> V. L. N. BALAJI GUPTA TIRUVEEDHI VENKATESWARA RAO BATTULA KISHORE BABU BONIGE Copyright (c) 2021 V L N Balaji Gupts Tiruveedhi, Venkateswara Rao Battula, Kishore babu Bonige 2021-01-07 2021-01-07 153 159 10.22159/ijap.2021v13i1.39608 A VALIDATED RP-HPLC METHOD FOR IMPURITY PROFILING OF SODIUM NITROPRUSSIDE IN INJECTION DOSAGE FORM <p><strong>Objective: </strong>The main objective of this research work is to develop and validate a single reverse-phase high-performance liquid chromatography (RP-HPLC) method. This method should becapable of quantifying all the known, as well as other possible degradation impurities of sodium nitroprusside (SNP) in its injection formulation.</p> <p><strong>Methods: </strong>Of allmethod development trails, we have observed better separations between known and degradation impuritiesin Inert sustain C18, (250 x 4.6) mm, 5 µm column at 30 °C temperature. Isocratic elution was carried out by using pH 8.6 phosphate buffer and acetonitrile in the ratio of 65:35 %v/v with a flow rate of 0.8 ml/min. The detection was carried out at 220 nm, with an injection volume of 10 µl.</p> <p><strong>Results: </strong>In the proposed method, SNP was eluted at 22.5 min. Nitrite, nitrate, and ferrocyanide were linear from 0.25 to 37 μg/ml, ferricyanide was linear from 1.0 to 37 μg/ml, and SNP was linear from 0.75 to 37 μg/ml. The % RSD for six spiked samples (precision)was found to be less than 0.5 %. Accuracy was performed for known impurities from LOQ to 150 % for a 0.5 % specification level. The resultswere found to be in the acceptance range of 90-110 %. The LOQ concentration of nitrite, nitrate, and ferrocyanide was 0.25 μg/ml each,LOQ offerricyanide and SNP was found to be 1.0 μg/ml and 0.75 μg/ml, respectively. The SNP injection samples were exposed to different degradation conditions, and the results were found specific in the proposed methodology.</p> <p><strong>Conclusion: </strong>The proposed RP-HPLC method is specific, precise, accurate, linear, stable, and robust for quantification of known and other possible degradation impurities in SNP injection formulation.</p> MURALI KRISHNAM RAJU P. VENKATA NARAYANA B. SHYAMALA P. SRINIVASU KONDRA HSN RAJU DANTULURI Copyright (c) 2021 murali krishnam raju potturi 2021-01-07 2021-01-07 160 169 10.22159/ijap.2021v13i1.39534 THE DEVELOPMENT AND CHARACTERISATION OF FAST DISSOLVING FILM OF POORLY WATERSOLUBLE DRUG LURASIDONE HYDROCHLORIDE <p><strong>Objective: </strong>The objective of the present work was to formulate and evaluate a fast-dissolving oral film of lurasidone hydrochlorideused as an atypical antipsychotic for the treatment of schizophrenia capable of providing faster onset of action.</p> <p><strong>Methods: </strong>The fastdissolving films of lurasidone hydrochloride were prepared by the solvent casting technique using different compositions and combinations of hydroxypropyl methylcellulose E-3, E-5, E-15, and K4M as fast-dissolving polymer bases. A set of seven formulations were prepared and evaluated for parameters like physical characterization, thickness, weight uniformity, mechanical characteristics (folding endurance,tensile strength), surface pH, <em>in vitro</em> disintegration time, drug content, and an <em>in vitro</em> drug release.</p> <p><strong>Results: </strong>The prepared films exhibited uniform and a smooth surface with uniform weight, thicknessand 89-90% mg drug content. The formulation F7 Showed excellent elasticity and disintegration within seconds. Lurasidone hydrochloride was rapidly released <em>in vitro</em> from all formulations. The release was found to be rapid and maximum of 41.5% in Phosphate buffer pH 6.8 and 58.6% in 0.1 N hydrochloric acid over a period of 30 min. The further optimized formulation F7Adepicted a faster and maximum release of 78% as compared to the marketed tablet 74%.</p> <p><strong>Conclusion: </strong>The developed formulation is a better alternative to tablets by its ability to produce good drug release. </p> ANAGHA PRABHU ASMITA ARONDEKAR Arondeka PRASHANT BHIDE SHWETA BORKAR Copyright (c) 2021 Asmita Arondekar, Prashant Bhide, Shweta Borkar 2021-01-07 2021-01-07 170 177 10.22159/ijap.2021v13i1.39492 FORMULATION, OPTIMIZATIONANDEVALUATION OF SUBLINGUAL FILM OF ENALAPRILMALEATE USING 32 FULL FACTORIAL DESIGN <p><strong>Objective: </strong>The purpose of this investigation was to formulate, optimize and evaluate sublingual film of Enalapril maleate for rapid management of Hypertension.</p> <p><strong>Methods: </strong>Sublingual films were prepared by solvent casting method. Present investigation were formulated by using HPMC E 15 (X<sub>1</sub>) as polymer and Polyethylene glycol (X<sub>2</sub>) as plasticizer were chosen as independent variables in 3<sup>2</sup> full factorial design while Tensile strength (TS), Disintegration time (DT) and % Cumulative drug release at 10 min. (% CDR) were taken as dependent variables. The various physical parameters were evaluated for sublingual films such as thickness, tensile strength, folding endurance, disintegration time, surface pH and % CDR.</p> <p><strong>Results: </strong>From the experimental study, it was concluded that the optimized batch F<sub>8</sub> showed 98.6 %, the highest release of the drug. Stability study was performed by taking an optimized formulation and it was observed stable. The sublingual films showed acceptable results in all studies such as thickness, tensile strength, folding endurance, disintegration time, surface pH and % CDR at 10 min. R<sup>2</sup> values for Tensile Strength (Y<sub>1</sub>), Disintegration time (Y<sub>2</sub>) and % cumulative drug release at 10 min. of Enalaprilmaleate(Y<sub>3</sub>) found to be 0.9852, 0.9829 and 0.9641 respectively. Thus, a good correlation between dependent and independent variables was developed.</p> <p><strong>Conclusion: </strong>3<sup>2</sup> full factorial design was successfully applied during preparation, optimization and evaluation of sublingual films of Enalapril maleate. The present investigation showed quick disintegration and fast release of the drug for rapid management of Hypertension.</p> SATYAJIT SAHOO KIRTI MALVIYA AMI MAKWANA PRASANTA KUMAR MOHAPATRA ASITRANJAN SAHU Copyright (c) 2021 SATYAJIT SAHOO C.U. SHAH COLLEGE OF PHARMACY AND RESERACH 2021-01-07 2021-01-07 178 186 10.22159/ijap.2021v13i1.39446 BIOWAIVER STUDY OF IMMEDIATE RELEASE GLIMEPIRIDE TABLETS <p><strong>Objective:</strong> Demonstrating therapeutic equivalency regarding the efficacy and safety among originator products and generics is a key step in permitting the marketing of generic products. The study aimed to evaluate the bioequivalence of five different generic brands of Glimepiride tablets under biowaiver conditions.</p> <p><strong>Methods: </strong>The quality of the tablet products, including uniformity of weight, friability, and disintegration test, was assessed using the United State Pharmacopeia&nbsp;(USP)&nbsp;general monograph for the tablet dosage form.&nbsp;The content of glimepiride in the tablets was measured using UV spectrophotometer at the wavelength 229 nm. The release of Glimepiride from the tested and originator tablet products was evaluated using the dissolution profiles conducted in HCI buffer pH 1.2, and phosphate buffer pH 6.4 and 7.8 by USP dissolution apparatus II.&nbsp;The bioequivalence of test&nbsp;products&nbsp;was&nbsp;assessed&nbsp;using&nbsp;the similarity and difference factors.&nbsp;</p> <p><strong>Results:</strong>The tested&nbsp;products&nbsp;complied to USP requirements for quality standards; all the&nbsp;products&nbsp;show&nbsp;rapid disintegration, D1&nbsp;show&nbsp;higher&nbsp;time&nbsp;(Three minutes) while D3 show&nbsp;lower&nbsp;time&nbsp;(28 seconds). The&nbsp;content&nbsp;of test&nbsp;products&nbsp;was&nbsp;(104.68, 93.75, 97.21, 97.03, and 102.10)&nbsp;for&nbsp;D1,&nbsp;D2,&nbsp;D3,&nbsp;D4, and&nbsp;D5&nbsp;, respectively, compare to 103.70 for OB. Dissolution profiles revealed that the highest similarity to the originator was showed in pH 6.4; f2 ranged (74.5-68.4)&nbsp;for all the tested products and&nbsp;low similarity&nbsp;in pH 7.8;&nbsp;f2&nbsp;ranged&nbsp;(45.2-64.7).</p> <p><strong>Conclusion:</strong> The study showed that the generic products has noticeable similarity with the originator brand and it can be interchangeable.</p> SIHAM ABDOUN DALIA GABER RAGHAD ALWAHABI NASHWA ALQUSSIR NEHAL ALMUTAIRI WAAD ALSALAMAH Copyright (c) 2021 Siham Abdoun, Dalia Gaber, Raghad Alwahabi, Nashwa Alqussir , Nehal Almutairi, Waad Alsalamah 2021-01-07 2021-01-07 187 192 10.22159/ijap.2021v13i1.39383 PREPARATION AND EVALUATION OF DOLUTEGRAVIR SOLID DISPERSIONS <p><strong>Objective: </strong>The current work mainly focuses on solubility enhancement of dolutegravir which is a BCS (Biopharmaceutical Classification System) class-II drug using various excipients.</p> <p><strong>Methods: </strong>Solid dispersions of dolutegravir were prepared by solvent evaporation and fusion methods using carriers like poloxamer-188 and plasdone K-29/32 in different ratios (1:0.5 to 1:3.0). The amount of dolutegravir used was kept constant and the polymer concentrations were increased. Various physical parameters like angle of repose, carr’s index, Hausner’s ratio were calculated for the prepared solid dispersions. They were also evaluated for particle size and drug content uniformity along with <em>in vitro </em>drug release. Characterization studies like Fourier Transform Infra-Red spectroscopy (FTIR), Differential Scanning Calorimetry (DSC), Scanning Electron Microscopy (SEM) and X-Ray Diffraction (XRD) were also done.</p> <p><strong>Results: </strong>Dolutegravir solid dispersions showed good to excellent flow properties. From <em>in vitro</em> dissolution studies, it was observed that the solid dispersion formulation DF3 containing dolutegravir and poloxamer-188 in 1:1.5 ratios prepared by fusion method showed better dissolution rate when compared with other formulations. The dissolution parameters were also evaluated. DF3 showed a higher drug release of 86.33% in 60 min. FTIR and DSC studies revealed that there were no major interactions between drug and excipients. XRD studies revealed the nature of formulations.</p> <p><strong>Conclusion: </strong>The solid dispersions prepared using poloxamer-188 by fusion method has enhanced the solubility of dolutegravir.</p> SUNDEEP MUPPARAJU VIDYADHARA SURYADEVARA SANDEEP DOPPALAPUDI Copyright (c) 2021 SANDEEP DOPPALAPUDI, VIDYADHARA SURYADEVARA 2021-01-07 2021-01-07 193 198 10.22159/ijap.2021v13i1.40113 ENHANCEMENT OF SOLUBILITY AND DISSOLUTION RATE OF ACETYLSALICYLIC ACID VIA CO-CRYSTALLIZATION TECHNIQUE: A NOVEL ASA-VALINE COCRYSTAL <p><strong>Objective: </strong>This study aims to synthesize acetylsalicylic acid (ASA) cocrystals using valine as a coformer via a co-crystallization technique to increase the solubility and dissolution rate of ASA.</p> <p><strong>Methods: </strong>The ASA-valine cocrystal (1:1 molar ratio) was prepared using the solvent evaporation technique with ethanol: water (50:50). The cocrystal was characterized using Fourier transform infrared spectroscopy (FT-IR), Differential scanning calorimetry (DSC), Powder X-ray diffraction (PXRD), Scanning electron microscopy (SEM), melting point to confirm the formation of cocrystal. The evaluation of cocrystal was done by drug content determination, solubility and dissolution studies.</p> <p><strong>Results: </strong>The prepared cocrystal was successfully confirmed for the formation of a hydrogen bond. The melting point of prepared cocrystal was decreased compared to pure ASA and valine, which indicated the formation of a new crystalline form. The FT-IR studies showed the formation of a new hydrogen bond by shifting the-O-H,-C=O and-N-H functional groups. SEM studies ensured that the prepared cocrystals were in needle-like appearance. Finally, DSC and PXRD studies were also indicated the successful formation of ASA-valine cocrystal. The drug release of cocrystal was found to be 100% at 60<sup>th</sup> min. Where in the case of pure ASA and marketed product of ASA exhibited the dissolution rate of 59% and 69% at 60<sup>th</sup> min respectively.</p> <p><strong>Conclusion: </strong>The co-crystallization technique can be adopted as the best strategy to increase the solubility and dissolution rate of BCS class 2 drugs. Therefore the prepared ASA-valine cocrystal can be a greater alternative to increase the solubility and dissolution rate compared with pure and marketed ASA.</p> SHANTHALA H. K. JAYAPRAKASH H. V. MUNIGANTI RADHAKRISHNA JASWANTH GOWDA B. H. KARTHIKA PAUL S. J. SHANKAR MOHAMMED GULZAR AHMED SANJANA A. Copyright (c) 2021 Jaswanth Gowda BH, Shanthala H.K., Jayaprakash H.V., Muniganti Radhakrishna, Karthika Paul, S.J. Shankar 2021-01-07 2021-01-07 199 205 10.22159/ijap.2021v13i1.40054 FABRICATION OF NANO CLAY INTERCALATED POLYMERIC MICROBEADS FOR CONTROLLED RELEASE OF CURCUMIN <p><strong>Objective: </strong>The objective of this study was to formulate and evaluate the Curcumin (CUR) encapsulated sodium alginate (SA)/badam gum (BG)/kaolin (KA) microbeads for controlled drug release studies.</p> <p><strong>Methods: </strong>The fabricated microbeads were characterized by fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), X-ray diffraction (X-RD), and scanning electron microscopy (SEM). Dynamic swelling studies and&nbsp;<em>in vitro&nbsp;</em>release kinetics were performed in simulated intestinal fluid (pH 7.4) and simulated gastric fluid (pH 1.2) at 37 °C.</p> <p><strong>Results: </strong>FTIR confirms the formation of microbeads. DSC studies confirm the polymorphism of CUR in drug loaded microbeads which indicate the molecular level dispersion of the drug in the microbeads. SEM studies confirmed the microbeads are spherical in shape with wrinkled and rough surfaces. XRD studies reveal the molecular dispersion of CUR and the presence of KA in the developed microbeads. <em>In vitro</em> release studies and swelling studies depend on the pH of test media, which might be suitable for intestinal drug delivery. The % of drug release values fit into the Korsmeyer-Peppas equation and n values are obtained in the range of 0.577-0.664, which indicates that the developed microbeads follow the non-Fickian diffusion drug release mechanism.</p> <p><strong>Conclusion: </strong>The results concluded that the CUR encapsulated microbeads are potentially good carriers for controlled drug release studies. </p> DHARMENDER PALLERLA SUMAN BANOTH SUNKARI JYOTHI Copyright (c) 2021 Dharmender Pallerla, Suman Banothu, Jyothi Sunkari 2021-01-07 2021-01-07 206 215 10.22159/ijap.2021v13i1.39965 FORMULATION, OPTIMIZATION AND IN VITRO EVALUATION OF 5-FLUOROURACIL LOADED LIQUORICE CRUDE PROTEIN NANOPARTICLES FOR SUSTAINED DRUG DELIVERY USING BOX-BEHNKEN DESIGN <p><strong>Objective: </strong>To formulate, optimize and evaluate 5-fluorouracil loaded liquorice crude protein nanoparticles for sustained drug delivery using Box-Behnken design.</p> <p><strong>Methods: </strong>5-fluorouracil (5-FU) loaded liquorice crude protein (LCP) nanoparticles were prepared by desolvation method using ethanol-water (1:2 ratio), Tween-80 (2%v/v) as stabilizing agent and gluteraldehyde (8% v/v) as cross linking agent. The optimization of prepared nanoparticles was carried out using Box-Behnken design with 3 factors 2 levels and 3 responses. The independent variables were A)5-FU concentration B)LCP concentration and C) sonication time while the responses were R1) Drug entrapment efficiency R2) Drug loading efficiency and R3) Particle size. The correlation between factors and responses were studied through response surface plots and mathematical equations. The nanoparticles were evaluated for FTIR, physicochemical properties like particle size and zeta potential by Photon correlation spectroscopy (PCS) and surface morphology by TEM. The entrapment efficiency, drug loading efficiency and <em>in vitro</em> drug release studies in PBS pH 7.4 (24 h) were carried out. The observed values were found to be in close agreement with the predicted value obtained from the optimization process.</p> <p><strong>Results: </strong>5-fluorouracil loaded LCP nanoparticles were prepared by desolvation method, the optimization was carried out by Box-Behnken design and the final formulation was evaluated for particle size (301.1 nm), zeta-potential (-25.8mV), PDI(0.226), with entrapment efficiency (64.07%), drug loading efficiency (28.54%),<em> in vitro</em> drug release (65.2% in 24 h) respectively. The formulated nanoparticles show Higuchi model drug release kinetics with sustained drug delivery for 24 h in pH7.4 buffer.</p> <p><strong>Conclusion: </strong>The results were proved to be the most valuable for the sustained delivery of 5-Fluorouracil using liquorice crude protein as carrier. 5-FU–LCP nanoparticles were prepared using Tween-80 as stabilizing agent and gluteraldehyde as cross-linking agent to possess ideal sustained drug release characteristics.</p> GEETHA V. S. MALARKODI VELRAJ Copyright (c) 2021 GEETHA V S, Dr. Malarkodi Velraj 2021-01-07 2021-01-07 216 226 10.22159/ijap.2021v13i1.39932 SLOW QUASIKINETIC CHANGES IN WATER-LACTOSE COMPLEXES DURING STORAGE <p><strong>Objective: </strong>To investigate kinetic changes in the spectral characteristics by Fourier Transform Infrared spectroscopy (FTIR) of water-lactose complexes (SMC), derived during the manufacturing process of the drug, containing release-active forms of antibodies.</p> <p><strong>Methods: </strong>lactose monohydrate substance, saturated with release-active forms of affinity-purified polyclonal rabbit antibodies to recombinant human interferon-gamma (RA forms of Abs); tablets produced from this substance by direct compression after the addition of excipients (microcrystalline cellulose, magnesium stearate). Powdered and tableted placebo samples saturated with technologically processed water or phosphate-buffered saline, as well as with intact ethanol were used as control. Kinetic changes in SMC were studied using an Agilent Cary 630 FTIR spectrophotometer with a diamond&nbsp;ATR&nbsp;accessory (Agilent Technologies, USA). We used the method of X-ray fluorescence spectroscopy (EDX-7000 Shimadzu energy dispersive X-ray fluorescence spectrometer) to track changes in the fluorescence signal at certain wavelengths. The range of measured elements–<sup>11</sup>Na-<sup>92</sup>U.</p> <p><strong>Results: </strong>Control of some technological characteristics of the obtained active substance (moisture, flowability) and dosage form (mean mass, disintegration rate) was used as indirect indicators of quality, but they did not allow reliably distinguishing intact lactose from the saturated one. Long-period oscillations on FTIR spectra were characteristic for all types of samples; oscillations occur at approximately two-week intervals; S/N indices were more stable for samples of RA forms of Abs than for placebo samples. On some days, the substance saturated with RA forms of Abs significantly differed from the intact lactose powder. The kinetics of the X-ray fluorescence intensity at certain wavelengths indicates the possibility of a periodic cooperative trigger transition of the system. Reversible conformational transitions are observed for powders on the 30th and 130th days (Kα 3.313 keV). For tablets at Kα 3.313 keV and Kα 1.740 keV small changes were visualized on those days (100–110<sup>th</sup> day) when hysteresis phenomena were recorded in the IR spectra of these samples.</p> <p><strong>Conclusion: </strong>As a result, the evidence for a long-period dramatic conformational mobility of the water-lactose complex was obtained. Based on the data on the semiannual kinetics of IR spectra, a universal criterion for the identity of lactose powder saturated with RA forms of Abs was obtained. Also, it was confirmed that the lactose conformation state was changed by saturation with RA forms of Abs.</p> M. A. MOROZOVA A. M. KOLDINA T. V. MAKSIMOVA A. V. MARUKHLENKO I. A. ZLATSKY A. V. SYROESHKIN Copyright (c) 2021 Mariya Morozova 2021-01-07 2021-01-07 227 232 10.22159/ijap.2021v13i1.39837 FABRICATION OF SODIUM ALGINATE/GUM GHATTI IPN MICROBEADS INTERCALATED WITH KAOLIN NANO CLAY FOR CONTROLLED RELEASE OF CURCUMIN <p><strong>Objective: </strong>The objective of this study is to fabricate sodium alginate (SA)/gum ghatti (GG) microbeads intercalated with Kaolin (KA) nano clay for the sustained release of curcumin (CUR).</p> <p><strong>Methods: </strong>The microbeads were prepared by a simple ionotropic gelation technique. The developed beads were characterized by fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), X-ray diffraction (X-RD), and scanning electron microscopy (SEM). Swelling studies and <em>in vitro</em> release studies were investigated under both pH 7.4 and pH 1.2 at 37 °C.</p> <p><strong>Results: </strong>The developed microbeads were characterized by FTIR, which confirms the interaction between CUR, polymeric matrix and KA. DSC and XRD analysis reveals that the CUR has molecularly dispersed in the polymer matrix. <em>In vitro</em> results illustrated that microbeads were influenced by the pH of test media, which might be suitable for intestinal drug delivery. The drug release mechanism was analyzed by fitting the release data into different kinetic equations and n values are obtained in the range of 0.609-0.640, suggesting that the developed microbeads showed the non-Fickian diffusion type drug release.</p> <p><strong>Conclusion: </strong>These results clearly illustrated that the developed KA intercalated polymeric microbeads are potential drug carriers for the controlled release of CUR.</p> D. GANESH P. SURESH G. SRINIVAS RAO Copyright (c) 2021 Ganesh D, Suresh P, Srinivasa Rao G 2021-01-07 2021-01-07 233 241 10.22159/ijap.2021v13i1.39963 PRONIOSOMAL GEL MEDIATED TRANSDERMAL DELIVERY OF GLIBENCLAMIDE AND ATENOLOL COMBINATION: EXVIVO AND PHARMACODYNAMIC STUDIES <p><strong>Objective: </strong>The objective of the present work was to develop an optimized dosage form for treating comorbidity in combination and evaluate it for its pharmacodynamic performance in male Wistar albino rats.</p> <p><strong>Methods: </strong>Transdermal proniosomal gel for Combination of Glibenclamide (GLB) and Atenolol (ATN) was developed and optimized by Box Behnken design. This optimized combinational proniosomal gel (OCPG), which was selected by a point prediction method, was evaluated for its <em>ex vivo</em>, skin irritation studies and pharmacodynamic activities of both drugs in rats in comparison with its oral therapy.</p> <p><strong>Results: </strong>The <em>ex-vivo</em> permeation behavior through different skins was studied and the findings were also confirmed by the values of the steady-state flux (J<sub>ss</sub>). The OCPG observed an increase of more than twice in the cumulative amount of impregnated drugs compared to pure drug films. The study on skin irritation revealed the non-irritability of the developed OCPG applied. OCPG significantly showed sustained hypoglycemic activity in rats (p&lt;0.001), when compared to orally treat animals up to 24 h. Systolic blood pressure (SBP) lowering effect of OCPG was found to be significant (p&lt;0.02), when compared to orally treat rats up to 24 h. However, the reduction was slow and sustained in the case of OPCG where a significant response was observed in the performed studies.</p> <p><strong>Conclusion: </strong>Overall, the results show that controlled release GLB and ATN proniosomes offer a useful and promising transdermal delivery system. Henceforth this may be an achievement in treating the diabetic hypertensive patient.</p> P. ANITHA S. V. SATYANARAYANA Copyright (c) 2021 Anitha Posina, Satyanarayana SV 2021-01-07 2021-01-07 242 248 10.22159/ijap.2021v13i1.39958 DRUG RELEASE CONTROL AND ENHANCEMENT USING CARRIERS WITH DIFFERENT CONCENTRATIONS OF CAPMUL® MCM C8 <p><strong>Objective: </strong>The main aim of this study was to design a drug carrier capable to control and enhance the release of poorly water soluble drugs.</p> <p><strong>Methods: </strong>Three polymeric formulations, based on poly (2-hydroxyethyl methacrylate) and loaded with different Capmul<sup>®</sup> MCM C8 concentrations (0, 10 and 20 % w/w), were prepared. Felodipine, which is a poorly soluble substance, was selected as a model drug. The effect of Capmul<sup>®</sup> MCM C8 on swelling behavior and <em>in vitro</em> release profile of the prepared polymer was investigated in PBS.</p> <p><strong>Results: </strong>The swelling profiles of allformulationswere statistically similar, which indicated the non-significant effect of added Capmul<sup>®</sup> MCM C8 on polymer's swelling behavior. All formulations showed a delayed drug release. Formulation-F3, which is loaded with 20% w/wCapmul<sup>®</sup> MCM C8 displayed a significant higher release compared to the other formulations.</p> <p><strong>Conclusion: </strong>Capmul<sup>®</sup> MCM products, which are widely used in food industries, can be used to improve the oral delivery of poorly soluble substances. The optimized formulation exhibited the ability to control and enhance the release of the model drug.</p> MOHAMMAD F. BAYAN Copyright (c) 2021 Mohammad F. Bayan 2021-01-07 2021-01-07 249 252 10.22159/ijap.2021v13i1.39742 HPLC DETERMINATION OF SILDENAFIL IN TABLETS <p><strong>Objective: </strong>The popularity of Sildenafil, the widespread distribution of various products and dietary supplements with added synthetic drugs, requires reliable analysis methods. This research study aimed to develop a simple isocratic HPLC method for the determination of Sildenafil in tablet dosage forms from the local market.</p> <p><strong>Methods: </strong>Separation was carried out at 30 °C, using column LiChrosorb<sup>®</sup> RP-18 (150 x 4.0 mm, 5 μm) with mobile phase consisting of acetonitrile: methanol: 0.5% triethylamine (15: 26: 59 v/v/v). The detector was set at 290 nm. The flow rate was 1.0 ml/min and the injection volume was 20 μl.</p> <p><strong>Results: </strong>Linear correlation was obtained within the range 6.25–50.0 μg/ml with correlation coefficient (R<sup>2</sup>) 0.9998. The achieved limits of detection and quantitation were 0.7 and 2.2 μg/ml, respectively.</p> <p class="western" style="margin-bottom: 0cm; line-height: 0.18cm;" align="JUSTIFY"><strong>Conclusion: </strong>The developed method can be applied for the quality control of Sildenafil preparations.</p> MIGLENA SMERIKAROVA STANISLAV BOZHANOV VANIA MASLARSKA Copyright (c) 2021 Miglena Smerikarova, Stanislav Bozhanov, Vania Maslarska 2021-01-07 2021-01-07 253 256 10.22159/ijap.2021v13i1.39719