薬学および生命科学における研究開発の国際ジャーナル

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PREPARATION AND IN VITRO EVALUATION OF HYDROXY PROPYL METHYLCELLULOSE FILMS FOR TRANSDERMAL DELIVERY OF SERTRALINE HYDROCHLORIDE

Vijaya R, Bhalamurugan G L

The study was aimed to develop hydroxy propyl methylcellulose (HPMC) based matrix type transdermal film for the antidepressant sertraline hydrochloride(SH) to avoid systemic side effects and gastric disorders after oral administration Polymeric grades HPMC K4M, HPMC K15M, HPMC K100M and
solvents such as acetone, ethanol and isopropyl alcohol were used in the preparation of film (S1 to S9) by solvent evaporation method. Polyethylene glycol 400 was added as a plasticizer at a concentration of 150% w/w of polymer. Permeation enhancers of propylene glycol and oleic acid were employed to enhance the skin permeation of SH. The films were evaluated in vitro for thickness, folding endurance, percentage moisture absorption, percentage moisture loss, water vapour transmission, tensile strength, drug content, in vitro release and skin permeation. Maximum SH release of 39.94%±0.543% was obtained for HPMC K15M formulation (S4) prepared using acetone and water as solvents at a ratio of 9:1. The permeation of SH across the rat abdominal skin was 20.27%±0.051% and was increased to 38.19%±0.063% in the presence of permeation enhancers oleic acid (1%) and propylene glycol (30%) at a ratio of 1:5.The optimized film S4 did not produce any noticeable skin reactions. The drug release followed higuchi kinetics with non fickian diffusion mechanism. In conclusion, the polymer grades of
HPMC containing plasticizer had influenced the SH release profile and the incorporation of permeation enhancers increased the permeation of SH.