Osama AA Ahmed1,2
,
Tarek A Ahmed1,3,
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.
This is an Open Access article that uses a funding model which does not charge readers or their institutions for access and distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0) and the Budapest Open Access Initiative (http://www.budapestopenaccessinitiative.org/read), which permit unrestricted use, distribution, and reproduction in any medium, provided the original work is properly credited..
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