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Original Research Article
Enhancement of In Vitro
Skin Transport and In Vivo Hypoglycemic Efficacy
of Glimepiride Transdermal Patches
Osama AA Ahmed1,2*,
Tarek A Ahmed1,3, Ashraf B Abdel-Naim4,
Alaa Khedr5, Zainy M Banjar6 and
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:
Email:
osama712000@gmail.com,
oaahmed@kau.edu.sa; Tel:
+966599120686; Fax: +96626951696
Received: 19 March 2014
Revised accepted: 17 July
2014
Tropical
Journal of Pharmaceutical Research, August 2014; 13(8): 1207-1213
http://dx.doi.org/10.4314/tjpr.v13i8.3
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 |
