Tropical Journal of Pharmaceutical Research
Pharmacotherapy Group, Faculty of Pharmacy, University of Benin, Benin City, Nigeria
Vol. 13, No. 8, 2014, pp. 1207-1213
Bioline Code: pr14167
Full paper language: English
Document type: Research Article
Document available free of charge
Tropical Journal of Pharmaceutical Research, Vol. 13, No. 8, 2014, pp. 1207-1213
© Copyright 2014 - Tropical Journal of Pharmaceutical Research
Enhancement of In Vitro Skin Transport and In Vivo Hypoglycemic Efficacy of Glimepiride Transdermal Patches|
Ahmed, Osama A.A.; Ahmed, Tarek A.; Abdel-Naim, Ashraf B.; Khedr, Alaa; Banjar, Zainy M. & Afouna, Mohsen I.
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.
Glimepiride; Transdermal patch; Coprecipitate; Inclusion complex; Hydroxypropyl methylcellulose; Polyvinyl pyrrolidone; Chitosan; Skin permeation
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