Research Articles

2018  |  Vol: 4(5)  |  Issue: 5 (September- October)  |  https://doi.org/10.31024/ajpp.2018.4.5.13
Glibenclamide loaded Ethosomal Gel for Transdermal Delivery: Formulation, optimization and ex - vivo study

Abdul Wahid Ambekar1*, Nagaraju Ravouru2, Subhash Chandra Bose Penjuri3

1Department of Pharmaceutics, Dr. V.V.P.F’s College of Pharmacy, Vilad Ghat; P.O M.I.D.C, Ahmednagar – 414111 (M.S), India

2Institute of Pharmaceutical Technology, Sri Padmavati MahilaVisvavidyalayam (Women’s University) Tirupati, (A.P.) India

3Department of Pharmaceutics, MNR College of Pharmacy, Sangareddy; (Telengana State), India

*Address for Corresponding Author

Abdul Wahid Ambekar

Department of Pharmaceutics                                         

Dr. Vithalrao Vikhe Patil Foundation’s College of Pharmacy

Vadgaon Gupta (Vilad Ghat) MIDC, Ahmednagar – 414111 (MS) India

Abstract

Objective: Glibenclamide is important and popular drug required in the treatment of hyperglycemia in Non-Insulin Dependent Diabetes Mellitus (NIDDM). Glibenclamide is affected by first pass metabolism and has a plasma half-life of 4 to 6 hrs, thus require high and frequent administration which in turn results in several side effect like nausea, vomiting, heartburn etc. To overcome this drawback glibenclamide was loaded into ethosomes to improve its therapeutic efficacy and decrease side effect via transdermal route. Material and methods: Six different ethosomal formulations with different concentration of ethanol, soya lecithin and cholesterol were prepared by cold method and characterized for vesicle size, polydispersity index (PI), zeta potential, vesicle surface morphology and entrapment efficiency (EE). Ex - vivo permeation study was conducted using excised abdominal skin of rat as a permeation barrier using franz diffusion cell. Results: Formulation GF4 showed 7 fold higher (p<0.05) transdermal flux (56.08 ± 1.78 µg/cm2/hr) than the drug solution (7.64 ± 2.37 µg/cm2/hr) and 3 fold higher than GF6 formulation (19.46 ± 2.64 µg/cm2/hr). The high transdermal flux of GF4 formulation may be attributed to its smaller vesicle size (119.4 ± 1.1527 nm) and high entrapment efficiency. Based on the above findings the GF4 ethosomal formulation was converted to ethosomal gel formulation by incorporating it into 1% Carbopol 324 gel, which was further evaluated and compared with conventional gel formulation for skin permeability across the excised rat skin. Conclusion: Ethosomal gel formulation show significant (p<0.05) transdermal flux (37.23 ± 1.24 µg/cm2/hr) as compared to conventional gel formulation (16.35 ± 1.75 µg/cm2/hr). It can be concluded that ethosomal gel formulations is an effective tool for transdermal delivery of glibenclamide.

Keywords: Lecithin, Glibenclamide, ethosome, ethosomal gel, Non-Insulin Dependent Diabetes Mellitus

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