In Vitro and In Vivo Assessment of Matrix Type Transdermal Therapeutic System of Labetalol Hydrochloride

Ashu      Mittal; Shikha      Parmar; Brijendra      Singh

Abstract

Objective: The main objective of the present study was to establish and evaluate matrix type transdermal therapeutic systems containing new polymeric combinations (Eudragit E PO/Eudragit RL 100 & Plasdone S 630) as polymers and Labetalol Hydrochloride (LBHCl) as a model drug. Experimental: The matrix type TTS of LBHCl were prepared by film casting technique. The patches were characterized for physical, in vitro release studies and ex-vivo permeation studies using human cadaver skin. On the basis of in vitro drug release study and skin permeation, formulation A1 was found more effective than the other formulations, so it was selected as the optimized formulation. The optimized formulation patch was assessed in detail for its pharmacokinetic, pharmacodynamic, skin irritation potential, and stability studies. Results: The maximum percentage drug release and Permeation in 48 hrs were 92.43 % and 76.24 % respectively for optimized patch. The Korsmeyer peppas release exponent value of 0.604 in the optimized formulation was highly suggestive of release mechanism towards first order release. The observations obtained from the in vivo characterization of the optimized patch were indicative of sustained action of the developed formulation. The interaction studies analysis indicated no chemical interaction among the drug and polymers. The optimized patch appeared free from potentially hazardous skin irritation as observed by skin irritation score of 0.915 < 2.00 (under Draize score test). The optimized formulation was found to be stable at ambient storage conditions. Conclusion: The above TTS holds promise for improved bioavailability and better management of hypertension in long term basis.

Keywords: Matrix type, transdermal, human cadaver skin, labetalol hydrochloride, eudragit E PO, eudragit RL 100, plasdone S -630 (copovidone)

« Previous Next »