In vivo evaluation of a novel zero order drug releasing transdermal system of rotigotine
A. R. Sravanthi, S. Mallikarjun Reddy, Albert Jaswanth · Asian Journal of Pharmacy and Pharmacology · 2021
Background: Rotigotine is a new non-ergolinic dopamine agonist used in the treatment of Parkinson's disorder and restless legs syndrome.It has extensive pre-systemic metabolism and administration of rotigotine through transdermal route is the best way to avoid pre-systemic metabolism and thereby to increase the bioavailability and to deliver the drug in a controlled order.A controlled release transdermal system was developed using a novel hybrid Objective: technique including a combination of micro reservoir and adhesive dispersion system.Materials and Methods: Transdermal system was prepared by incorporating rotigotine drug in adhesive matrix layer in which microspheres loaded with rotigotine were dispersed.Microspheres were prepared by spray drying technique using poly-ecaprolactone and maltodextrin (1:1 ratio) as carriers in various drug to polymer ratios.Microsphere Results: composition comprising drug to polymer ratio 1:9 was found optimal for designing transdermal system.The optimized transdermal formulation comprised of 80 mg of silicon adhesive with 2.5 mg of rotigotine along with 20.1 mg of microspheres containing 2 mg of rotigotine.From the PK study conducted in male wistar rats, it was Conclusion: observed that there was 1.679 folds improvement in bioavailability of test formulation when compared to reference (contains 4.5 mg of rotigotine pure crystalline drug in adhesive matrix layer) formulation.