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  • WJPPS AUGUST ISSUE PUBLISHED
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Abstract

IN VITRO AND IN VIVO SKIN PERMEATION STUDIES ON TRANSDERMAL THERAPEUTIC SYSTEM OF LERCANIDIPINE HYDROCHLORIDE

Jiji Jose*, Narayanacharyulu R., Jisha Prems

ABSTRACT

Lercanidipine hydrochloride, an effective calcium channel blocker, widely used for the treatment of chronic stable angina and hypertension seems to be potential therapeutic transdermal system candidate, mainly due to its low oral bioavailability, short half life and high first-pass metabolism. Hence an attempt was made to develop transdermal therapeutic systems for lercanidipine hydrochloride using the polymer blend of eudragit RL100 and polyvinyl pyrolidone (PVP) in the ratio 1:4 by solvent casting method. propylene glycol (PG) (15 % w/w) and tween 80 (4% w/w) were selected as plasticizer and permeation enhancer respectively based on the preliminary optimization studies. Incorporation of PVP and PG improved the flexibility, folding endurance handling properties and drug release of the films. The skin irritation studies indicated that there is no recognizable changes on skin surface after the removal of the film. The patches were also evaluated for in vitro skin permeation using human cadaver skin. The presence of tween 80 produced significant increase in permeability and the film exhibited the cumulative amount of drug permeation across skin of 4813.903 μg/cm2 at the end of 24 h. In vivo bioavailability studies in rabbits demonstrated that the transdermal film provided steady state plasma concentrations with minimal fluctuations and nearly six fold enhancement of bioavailability of lercanidipine hydrochloride relative to oral administration. It may be concluded that the fabricated transdermal delivery system have the potential to provide controlled and extended drug release, better bioavailability and thus, they may improve the patient compliance.

Keywords: Transdermal therapeutic system; Lercanidipine hydrochloride; Eudragit; PVP; Skin Permeation.


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