Sravanthi A.*, Sunitha M. Reddy, Jaswanth A.
Officer, Department of QA, Natco Pharma Limited, Kotthur, Ranga Reddy District, Telangana, India 509228
*Corresponding author
Sravanthi A
Officer, Department of QA, Natco Pharma Limited, Kotthur, Ranga Reddy District, Telangana, India 509228
Abstract
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. Objective: A controlled release transdermal system was developed using a novel hybrid 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-e-caprolactone and maltodextrin (1:1 ratio) as carriers in various drug to polymer ratios. Results: Microsphere 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 mg of microspheres containing 2 mg of rotigotine. Conclusion: From the PK study conducted in male wistar rats, it was 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.
Keywords: Rotigotine, pre-systemic, transdermal, maltodextrin, poly-e-caprolactone,microspheres, bioavailability
