FORMULATION AND EVALUATION OF IN-SITU GEL CONTAINING LINEZOLID IN THE TREATMENT OF PERIODONTITIS
Keywords:Linezolid, In-situ gel, Periodontal disease
Objective: The intent to prepare and evaluate Linezolid in-situ gel in the treatment of periodontitis.
Methods: pH-sensitive in-situ gel was formed by the cold method using a varying concentration of the drug, carbopol 934P and hydroxypropyl methylcellulose (HPMC) and carbopol 934P and sodium carboxy methylcellulose (CMC) (1:1,1:1.5,1:2,1:2.5). An optimized batch was selected based on gelling time and gelling capacity. The prepared in-situ gels were evaluated for appearance, pH, gelling capacity, viscosity, in vitro release studies, rheological studies, and finally, was subjected to drug content estimation and antibacterial activity test.
Results: FTIR study shows drug and physical mixture were compatible with each other. The rheology of formulated in-situ gel exhibited a pseudoplastic flow pattern. this may be because when polymer concentration was increased the prepared formulations become more viscous and in turn delayed the drug release and from the prepared formulation, LF4 and SF4 have polymer concentrations i. e, 0.9% carbopol and sodium CMC showed drug release up to 12 h.
Conclusion: When carbopol is appropriately mixed with other suitable polymers it forms an in-situ gel-forming system that was substantiated by the property to transform into stiff gels when the pH is increased. The in-situ gel was prepared using a combination of carbopol-HPMC and carbopol-Na CMC The formulations LF1 to SF4 showed high linearity (R2 = 0.490-0.682), indicating that the drug was released from the prepared in-situ gel by the diffusion-controlled mechanism. Thus, the formulation of batches LF4 and SF4 containing carbopol: HPMC and carbopol: NaCMC in 1:2 ratios were considered as optimum formulation based on optimum viscosity, gelling capacity and to extend the in vitro drug release.
Gorle A, Yadav R, Rathod M, Mali P. Formulation and evaluation of in-situ gel containing ciprofloxacin hydrochloride in the treatment of periodontitis. Asian J Pharm Clin Res 2017;10:154-59.
World Health Organization (WHO). Antimicrobial resistance: global report on surveillance; 2014. Available from: https://www.who.int/antimicrobial-resistance/publications/surveillancereport/en/ [Last accessed on 18 Dec 2020]
Zabransky RJ. Linezolid: the first class of a new class of antimicrobial agents. Clin Microbiol News l 2002;24:25–30.
Yoshizawa S, Tateda K, Saga T, Ishii Y, Yamaguchi K. Virulence-suppressing effects of linezolid on methicillin-resistant staphylococcus aureus: possible contribution to early defervescence. Antimicrob Agents Chemother 2012;56:1744–8.
Farahamed A, Sayar F, Tehrani RM, Eshfahani BJ. Clinical evaluation of topical application of doxycycline 3%+ketoprofen 2.5% gel in chronic periodontitis patients. J Dental Sci 2016;4:178-84.
Makwanan SB, Patel VA, Parmar SJ. Development and characterization of in-situ gel for ophthalmic formulation containing ciprofloxacin hydrochloride. Results Pharma Sci 2016;6:1–6.
Kassab HJ, Thomas LM, Jabir SA. Development and physical characterization of a periodontal bioadhesive gel of gatifloxacin. Int J Appl Pharm 2017;9:31-6.
Begum SG, Sekar M. Formulation and evaluation of tinidazole mucoadhesive buccal gels. Int J Pharma Bio Sci 2017;8:48-55.
Ahmed MG, Choudhari R, Acharya A. Formulation and evaluation of in situ gel of atorvastatin for the treatment of periodontitis. RGUHS J Pharma Sci 2015;5:53-60.
El-Kamel A, Al-Dosari H, Al-Jenoobi F. Environmentally responsive ophthalmic gel formulation of carteolol hydrochloride. Drug Delivery 2006;13:55-9.
Ariyana SD, Ervina I, Bangun D. Formulation and in vitro evaluation of alginate-based metronidazole periodontal gel. Asian J Pharm Clin Res 2014;7:223-7.
Indian Pharmacopoiea, Government of India. Ministry of health and family welfare. The controller of Publications, Delhi; 1996;1:100–24.
Doijad RC, Manvi FV, Malleswara Rao VSN, Prajakta Alsae. Sustained ophthalmic delivery of gatifloxacin from in situ gelling system. Indian J Pharm Sci 2006;68:814–8.
Martha J, Gentry N, Keith M, Olsen, Laurel CP. Pharmacodynamic activity and efficacy of linezolid in a rat model of Pneumococcal pneumonia. Antimicrob Agents Chemother 2002;46:1345–96.
Wani SUD, Gangadharappa HV, Ashish NP. Formulation, development and characterization of drug delivery systems based telmisartan encapsulated in silk fibroin nanosphere’s. Int J Appl Pharm 2019;11:247-54.
Wani SUD, Gautam SP, Qadrie ZL, Gangadharappa HV. Silk fibroin as a natural polymeric-based bio-material for tissue engineering and drug delivery systems-a review. Int J Biol Macromol 2020;165:2145-61.
Helal DA, El-Rhman DA, Abdel Halim SA, El-Nabarawi MA. Formulation and evaluation of fluconazole topical gel. Int J Pharm Pharm Sci 2012;4:176-83.
Biswas GR, Majee SB, Roy A. Combination of synthetic and natural polymers in hydrogel: an impact on drug permeation. J Appl Pharm Sci 2016;6:158-64.
Yellanki SK, Nerella NK, Goranti S, Deb SK. Development of metronidazole intravaginal gel for the treatment of bacterial vaginosis: effect of mucoadhesive natural polymers on the release of metronidazole. Int J Pharm Tech Res 2010;2:1746-50.
Parhi R, Terapalli BR, Teja B. Formulation and in vitro evaluation of minoxidil topical gel. Turk J Pharm Sci 2014;11:153-62.
Kalia S, Singh P, Singh G, Gill NS. Development and characterization of erythromycin estolate emulgel for topical delivery. Int J Recent Adv Pharm Res 2014;4:31-50.
Mekkawy A, Fathy M, El-Shanawany S. Formulation and in vitro evaluation of fluconazole topical gels. Br J Pharm Res 2013;3:293-313.
Hiremath SSP, Fatima SD, Abidabegum N, Vilas G, Mulla JS, Sreenivas SA, et al. Formulation and evaluation of a novel in situ gum-based ophthalmic drug delivery system of linezolid. Sci Pharm 2008;76:515-32.