FORMULATION DEVELOPMENT AND EVALUATION (INVITRO-IN VIVO STUDY) OF TRANSDERMAL DRUG DELIVERY SYSTEMS WITH ANTIHYPERTENSIVE DRUG.
Ritesh Suresh Bathe*, Girendra Kumar Gautam and Reni Kapoor
ABSTRACT
The present work aim to formulate and characterize transdermal drug delivery systems of carvedilol applying
different ratios of polymer HPMCK15M, (PVPK30) Polyvinyl Pyrrolidone and Ethyl Cellulose, & In –Vivo study
by monitoring the effect of the TDDS on blood pressure of methyl prednisolone acetate induced hypertensive rats.
The blood pressure of rats was measured using a noninvasive rat B.P. instrument based on cuff tail techniques.
Formulations F4 & F5 were most effective in the reduction of systolic BP. The developed transdermal patches
increase the efficacy of carvedilol for the therapy of hypertension. A significant fall in the rat B.P. was observed in
the treatment of hypertensive rats. It was concluded that a single patch application of carvedilol TDDS can
effectively control hypertension in rats. Solvent evaporation method was used for the formulation of patches. The
patches showed satisfactory folding endurance and tensile strength and it indicated good physical stability.
Transdermal permeation of carvedilol through rat abdominal skin was determined by using modified Franz
diffusion cells, Based on the drug release and physicochemical values, formulation F4 and F5 were considered as
an optimized formulation which shows higher percentage of drug release at 24 hours. The drug-excipients
compatibility studies were performed by Infrared spectrophotometer (FTIR). Release kinetics studies revealed that
the drug release from formulations F4 and F5 followed Higuchi kinetics. Skin irritation test performed on rats did
not show any erythema/edema for transdermal patches.
Keywords: Carvedilol, Transdermal patches, PVPK30, Ethyl cellulose, HPMCK15M, Release kinetics, In- Vivo, Skin irritation test.
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