EFFECT OF OILS, SURFACTANTS AND COSURFACTANTS ON PHASE BEHAVIOR AND PHYSICOCHEMICAL PROPERTIES OF SELF-NANOEMULSIFYING DRUG DELIVERY SYSTEM (SNEDDS) FOR IRBESARTAN AND OLMESARTAN


ALI NASR, AHMED GARDOUH, HASSAN GHONAIM, ELSAYED ABDELGHANY, MAMDOUH GHORAB

Abstract


Objective: The main purpose of this study was to optimize the different conditions for the preparation of self-nanoemulsifying drug delivery system (SNEDDS) for both Irbesartan (IRB) and Olmesartan (OLM).

Methods: Based on solubility study and emulsification efficiency, Preliminary investigations of various oils, surfactants and cosurfactants were carried out for selection of the proper SNEDDS ingredients. Pseudoternary phase diagrams were then plotted using series of concentrations to obtain optimum SNEDDS components that identify the efficient self-nanoemulsifying region. Sixteen unloaded SNEEDS formulae were prepared using Capryol 90, Cremophor RH 40 and Transcutol HP as oil, surfactant and cosurfactant respectively. The prepared SNEDDS were evaluated for self-nanoemulsification time, the effect of dilution (with different volumes at different pH values), optical clarity, viscosity, droplet size analysis as well as the polydispersity index (PDI). SNEDDS formulae were also evaluated for thermodynamic stability and zeta potential to confirm the stability of the prepared SNEDDS.

Results: The results showed that the mean droplet size of all reconstituted SNEDDS was found to be in the nanometric range (<100 nm) and showed optimum PDI values. All formulae also showed rapid emulsification time, good optical clarity and found to be highly stable. Formulae with the smallest particle size, lowest emulsification time, best optical clarity and robust to dilution and pH change were selected to be loaded with IRB and OLM for further study.

Conclusion: It was concluded that the prepared self-emulsified prototype was ready to incorporate many poorly soluble drugs in order to improve their solubility as well as bioavailability profile.

Keywords: Irbesartan, Olmesartan, Self-nanoemulsifying drug delivery system (SNEDDS), Capryol 90, Cremophor RH 40 and Transcutol HP.

 


| PDF | HTML |

References


Wang Z, Sun J, Wang Y, Liu X, Liu Y, Fu Q. Preparation and in vitro/in vivo evaluation of solid self-emulsifying nitrendipine pellets. Int J Pharm 2010;383:1-6.

Ratnam DV, Chandraiah G, Meena AK, Ramarao P, Kumar MN. The co-encapsulated antioxidant nanoparticles of ellagic acid and coenzyme Q10 ameliorate hyperlipidemia in high fat diet fed rats. J Nanosci Nanotechnol 2009;9:6741-6.

Shen H, Zhong M. Preparation and evaluation of self-microemulsifying drug delivery systems (SMEDDS) containing atorvastatin. J Pharm Pharmacol 2006;58:1183-91.

Anuradha S, Pratikkumar A, Darshana H. Peppermint oil based drug delivery system of aceclofenac with improved anti-inflammatory activity and reduced ulcerogenecity. Int J Pharma Biosci Technol 2013;1:89-101.

Pouton CW. Lipid formulations for oral administration of drugs: non-emulsifying, self-emulsifying and self-microemulsifying drug delivery systems. Eur J Pharm Sci 2000;11:93-8.

Ashok K, Kuldeep S, Murugesh K, Sriram R, Ramesh M. Formulation and development of an albendazole self-emulsifying drug delivery system (SEDDS) with enhanced systemic exposure. Acta Pharm 2012;62:563-80.

Kommuru T, Gurley B, Khan M, Reddy I. Formulation, development and bioavailability assessment of self-emulsifying drug delivery systems (SEDDS) of coenzyme Q10. Int J Pharm 2001;212:233-46.

Kale A, Patravale V. Design and evaluation of self-emulsifying drug delivery systems (SEDDS) of nimodipine. AAPS PharmSciTech 2008;9:191-6.

Kishanta K, Uma S, Subasini P, Debananda M, Ghanshyam P, Kanhu C. Method development, validation and stability study of irbesartan in bulk and pharmaceutical dosage form by UV-spectrophotometric method. Int J Pharm Biol Arch 2011;2:1114-22.

Prabhakar K, Vipan K, Sudhir R. Spectrophotometric estimation of olmesartan medoxomil in tablet dosage form with stability studies. Int J Chem Tech Res 2010;2:1129-34.

Patel J, Patel A, Raval M, Sheth N. Formulation and development of a self-nanoemulsifying drug delivery system of irbesartan. J Adv Pharm Tech Res 2011;2:9-16.

Nakagomi R, Nakai D, Kawai K, Yoshigae Y, Tokui T, Abe T, et al. Hepatobiliary transport of olmesartan, A novel angiotensin II blocker. Drug Metab Dispos 2006;34:862-9.

Dixit R, Nagarsenker M. Design, optimization and evaluation of self-nanoemulsifying granules of ezetimibe. Eur J Pharm Sci 2008;35:92-183.

Srinivas C, Sagar S. Enhancing the bioavailability of simvastatin using micro emulsion drug delivery system. Asian J Pharm Clin Res 2012;5:134-9.

Date A, Nagarsenker M. Design and evaluationof self-nanoemulsifying drug delivery systems (SNEDDS) for cefpodoxime proxetil. Int J Pharm 2007;329:166-72.

Patel A, Vavia P. Preparation and in vivo evaluation of SMEDDS (self-microemulsifying drug delivery system) containing fenofibrate. AAPS J 2007;9:344-52.

Divyakumar B, Priyanka B, Kiran B. Formulation and evaluation of self microemulsifying drug delivery system of low solubility drug for enhanced solubility and dissolution. Asian J Biomed Pharm Sci 2012;2:7-14.

Sheikh S, Shakeel F, Talegaonkar S, Ahmad F, Khar R, Ali M. Development and bioavailability assessment of ramipril nanoemulsion formulation. Eur J Pharm Biopharm 2007;66:227-43.

Atef E, Belmonte A. Formulation, in-vitro and in-vivo characterization of phenytoin self-emulsifying drug delivery system. Eur J Pharm Sci 2008;35:257-63.

Ehab I, Saleh A, Ahmed M, Mansoor A. Preparation and in-vitro characterization of self-nanoemulsified drug delivery system (SNEDDS) of all-trans-retinol acetate. Int J Pharm 2004;285:109-19.

Nekkanti V, Karatgi P, Prabhu R, Pillai R. Solid self-microemulsifying formulation for candesartan cilexetil. AAPS PharmSciTech 2010;11:9-17.

Chopade V, Chaudhari P. Development and evaluation of self emulsifying drug delivery system for lornoxicam. Int J Res Dev Pharm Life Sci 2013;2:531-7.

Khoo S, Humberstone A, Porter C, Edwards G, Charman W. Formulation, design and bioavailability assessment of lipidic self-emulsifying formulations of halofantrine. Int J Pharm 1998;167:155-64.

Balakrishnan P, Lee B, Oh D, Kim J, Hong M, Jee JP, et al. Enhanced oral bioavailability of coenzyme Q10 by a novel solid self-emulsifying drug delivery system. Int J Pharm 2009;374:66-72.

Ghosh P, Majithiya R, Umrethia M, Murthy S. Design and development of microemulsion drug delivery system of acyclovir for improvement of oral bioavailability. AAPS PharmSciTech 2006;7:172-7.

Balakrishnan P, Lee J, Oh D. Enhanced oral bioavailability of dexibuprofen by a novel solid self-emulsifying drug delivery system (SEDDS). Eur J Pharm Biopharm 2009;72:539-45.

Zakia B, Suyang Z, Wenli Z, Junlin W. Formulation, development and bioavailability evaluation of a self-nanoemulsifying drug delivery system (SNEDDS) of atorvastatin calcium. Int J Pharm 2013;29:1103-13.

Arpan C, Vineetkumar P, Manish N, Kamala V, Chamanlal S. A novel lipid-based oral drug delivery system of nevirapine. Int J PharmTech Res 2011;3:1159-68.

Humberstone A, Charman W. Lipid based vehicles for oral delivery of poorly water soluble drugs. Adv Drug Delivery Rev 2008;25:103-28.

Urvashi G, Ritika A, Geeta A. Formulation, design and evaluation of a self-microemulsifying drug delivery system of lovastatin. Acta Pharm 2012;62:357-70.

Farinato R, Rowell R. Optical properties of emulsions. Encyclopedia of emulsion technology, Marcel Dekker, New York; 2000;1:439-79.

Chen M. Lipid excipients and delivery systems for pharmaceutical development: a regulatory perspective. Adv Drug Delivery Rev 2008;60:768-75.

Spernath A, Yaghmur A, Aserin A, Hoffman R, Garti N. Food-grade microemulsions based on nonionic emulsifiers: media to enhance lycopene solubilization. J Agric Food Chem 2002;50:6917-22.

Li P, Ghosh A, Wagner R, Krill S, Joshi Y. Effect of combined use of nonionic surfactant on formation of oil-in-water microemulsions. Int J Pharm 2005;288:27-34.

Kallakunta V, Bandari S, Jukanti R, Veerareddy P. Formulation and evaluation of oral self-emulsifying powder of lercanidipine hydrochloride. Powder Technol 2012;221:375-82.

Sharma B, Sharma A, Arora S, Gupta S, Bishnoi M. Formulation, optimization and evaluation of novel nanoemulsion formulations for transdermal potential of celecoxib. Acta Pharm 2007;57:315-23.

Wu X, Xu J, Huang X, Wen C. Self-microemulsifying drug delivery system improves curcumin dissolution and bioavailability. Drug Dev Ind Pharm 2011;37:15-23.

Nazzal S, Nutan M, Palamakula A, Shah R, Zaghloul A, Khan M. Optimization of a self-nanoemulsified tablet dosage form of ubiquinone using response surface methodology: effect of formulation ingredients. Int J Pharm 2002;240:103-14.

Hong J, Kim J, Song Y, Park J, Kim C. A new self-emulsifying formulation of itraconazole with improved dissolution and oral absorption. J Controlled Release 2006;110:332-8.

Cui Y, Li L, Gu J, Zhang T, Zhang L. Investigation of microemulsion system for transdermal delivery of ligustrazine phosphate. Afr J Pharm Pharmacol 2011;5:1674-81.

Rai S, Yasir M. Preparation, optimization and in-vitro evaluation of cinnarizine loaded lipid based system. IOSR J Pharm 2012;2:47-56.

Maulik J, Natvarlal M, Ritesh B, Rakesh P. Formulation and evaluation of self-microemulsifying drug delivery system of lovastatin. Self-Microemulsion Lovastatin/Asian J Pharm Sci 2010;5:266-75.




About this article

Title

EFFECT OF OILS, SURFACTANTS AND COSURFACTANTS ON PHASE BEHAVIOR AND PHYSICOCHEMICAL PROPERTIES OF SELF-NANOEMULSIFYING DRUG DELIVERY SYSTEM (SNEDDS) FOR IRBESARTAN AND OLMESARTAN

Date

06-01-2016

Additional Links

Manuscript Submission

Journal

International Journal of Applied Pharmaceutics
Vol 8, Issue 1, 2016 Page: 13-24

Online ISSN

0975-7058

Statistics

405 Views | 201 Downloads

Authors & Affiliations

ALI NASR
Department of Pharmaceutics, Faculty of Pharmacy and Pharmaceutical Industries, Sinai University, Alarish, Egypt,

AHMED GARDOUH
Department of Pharmaceutics, Faculty of Pharmacy, Suez Canal University, Ismailia, Egypt

HASSAN GHONAIM
Department of Pharmaceutics, Faculty of Pharmacy, Suez Canal University, Ismailia, Egypt

ELSAYED ABDELGHANY
Department of Pharmaceutics, Faculty of Pharmacy and Pharmaceutical Industries, Sinai University, Alarish, Egypt,

MAMDOUH GHORAB
Department of Pharmaceutics, Faculty of Pharmacy, Suez Canal University, Ismailia, Egypt


Refbacks

  • There are currently no refbacks.