Enhancement of <i>In Vitro</i> Skin Transport and <i>In Vivo</i> Hypoglycemic Efficacy of Glimepiride Transdermal Patches

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/cm 2 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 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.

Vitamin E TPGS based transferosomes augmented TAT as a promising delivery system for improved transdermal delivery of raloxifene

“…Transdermal drug conveyance, if successful, is a promising alternative for medications with low oral bioavailability and can also offer a more patient-convenient dosage form [12]. The skin is normally acting as a barrier to exceedingly hydrophilic or lipophilic materials.…”

Formulation and clinical investigation of optimized vinpocetine lyoplant-tabs: new strategy in development of buccal solid dosage form

“…PVPs have been extensively used as hydrophilic carriers in the preparation of solid dispersion systems with a wide variety of drug classes 40. PVP K25, K30, and K90 are the most common grades that have been utilized for this purpose 16,41,42. The solubility and dissolution of various drugs such as mefenamic acid, glimepiride, sulindac, tenoxicam, tacrolimus, fenofibrate, and flurinazine have been increased following preparation of solid dispersions with PVPs 6,7,17.…”

Finasteride nano-transferosomal gel formula for management of androgenetic alopecia: ex vivo investigational approach

“…Steady-state flux (J SS ), permeability coefficient (Pc), and diffusion coefficient (D) were calculated as previously reported. 26 , 29 In addition, the obtained permeation data were fitted into different kinetic models: zero, first, Higuchi, Hixson–Crowell, and Baker-Lonsdale models. 19 , 30 , 31 Linearity and correlation coefficient ( r ) were evaluated.…”