Tropical Journal of Pharmaceutical Research

Original Research Article | OPEN ACCESS

Enhancement of In Vitro Skin Transport and In Vivo Hypoglycemic Efficacy of Glimepiride Transdermal Patches

Osama AA Ahmed^1,2 , Tarek A Ahmed^1,3, Ashraf B Abdel-Naim⁴, Alaa Khedr⁵, Zainy M Banjar⁶, Mohsen I Afouna³

¹Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Saudi Arabia; ²Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Minia University, Minia; ³Department of Pharmaceutics, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt; ⁴Department of Pharmacology & Toxicology, Faculty of Pharmacy; ⁵Department of Pharmaceutical Chemistry, Faculty of Pharmacy; ⁶Department of Clinical Biochemistry, Faculty of Medicine, King Abdulaziz University, Jeddah, Saudi Arabia.

For correspondence:- Osama Ahmed Email: osama712000@gmail.com Tel:+966599120686

Received: 19 March 2014 Accepted: 17 July 2014 Published: 18 August 2014

Citation: Ahmed OA, Ahmed TA, Abdel-Naim AB, Khedr A, Banjar ZM, Afouna MI. Enhancement of In Vitro Skin Transport and In Vivo Hypoglycemic Efficacy of Glimepiride Transdermal Patches. Trop J Pharm Res 2014; 13(8):1207-1213 doi: 10.4314/tjpr.v13i8.3

© 2014 The authors.
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Abstract

Purpose: To utilize hydroxybutyl-β-cyclodextrin (HB-β-CD) and polyvinyl pyrrolidone (PVP) for the enhancement of the transdermal delivery of glimepiride (GMD).

Methods: Matrix-type transdermal patches containing GMD, drug coprecipitate or its inclusion complex were prepared using different gelling agents, viz, hydroxypropyl methylcellulose (HPMC), hydroxypropyl cellulose (HPC), carbopol and chitosan. In vitro skin permeation evaluation of the formulations was conducted using automated diffusion system. Selected patch formulations were assessed for hypoglycemic activity as well as for GMD plasma concentration in rats.

Results: GMD- hydroxybutyl-β-cyclodextrin (HB-β-CD) binary systems (1:2 molar ratio) enhanced GMD aqueous solubility by > 10-fold. Diffusion test showed improved release of GMD-HB-β-CD inclusion complex compared with GMD alone. Maximum cumulative amounts of GMD- HB-β-CD that permeated through rat skin was 26.97 and 14.28 µg/cm² for patches prepared with fchitosan and HPMC, respectively. Thus, GMD-chitosan patches showed significantly higher (p < 0.05) drug permeation than GMD-HPMC after 6 h. Both chitosan and HPMC patches of GMD-HB-β-CD demonstrated substantial reduction (p < 0.05) in blood glucose level (192.67 ± 21.18 and 201 ± 15.11 mg/ dl, respectively), compared with the baseline value of 240 mg/ dl.

Conclusion: Application of chitosan and HPMC transdermal patches of GMD-HB-β-CD can serve as a potential alternative to peroral GMD with improved bioavailability and patient compliance.

Keywords: Glimepiride, Transdermal patch, Coprecipitate, Inclusion complex, Hydroxypropyl methylcellulose, Polyvinyl pyrrolidone, Chitosan, Skin permeation