DESIGN AND CHARECTERIZATION OF NOVEL TRANSDERMAL THERAPEUTIC SYSTEMS OF FELODIPINE
Abstract
Felodipine is an effective calcium channel blocker, mainly used in the treatment of hypertension and angina pectoris. To overcome the low oral bioavailability of felodipine, the present work was designed to develop transdermal therapeutic system for felodipine using the polymer blend of eudragit RL 100 (ERL) / RS 100 (ERS) by solvent casting method and to study the effect of polymer composition, plasticizer and permeation enhancer on the physico-mechanical and in-vitro drug release characteristics of the film. Dibutyl phthalate (DBP) and oleic acid (OA) were used as plasticizer and permeation enhancer respectively. Different formulations with varied concentration of polymers, plasticizers and permeation enhancers were done and optimization of the concentration of formulation components was performed. Incorporation of DBP improved the flexibility, folding endurance and handling properties of the films. There was no significant difference in the drug content among patches indicating the uniformity in drug content. Increasing the concentration of ERL, and the presence of plasticizer were found to increase the in vitro drug release of the films.  The patches were also evaluated for ex vivo skin permeation using human cadaver skin. The presence of OA produced significant increase in the flux and permeability constant. The formulation with ERL: ERS ratio 1:4, 2% w/w OA as permeation enhancer and 20% w/w DBP as plasticizer showed the best results which exhibited the cumulative percentage of drug release of 75.73 ± 2.179 % and the cumulative amount of drug permeation across skin of 4321 ± 11.533 µg/cm2 in 24 hrs. Drug-excipient interaction studies were carried out using DSC and IR technique; films indicated no chemical interaction between drug and excipient. The results of the skin irritation studies showed no noticeable irritancy on rabbit skin indicating the skin compatibility of the drug as well as polymer. An attempt was made to develop the complete transdermal system of the drug by using backing membrane and release liner.
Key-words: Transdermal Therapeutic System, Felodipine, Eudragit, Dibutyl Phthalate, Skin Permeation
DOI
https://doi.org/10.22270/jddt.v2i6.306
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