RASAGILINE MESYLATE, A BCS CLASS III DRUG; EX-VIVO PERMEATION ENHANCEMENT STUDY THROUGH EXCISED RAT ABDOMINAL SKINAbstract
Rasagiline Mesylate (RM), an antiparkinson drug, belongs to BCS class III drug having high solubility with low permeability. It undergoes extensive first-pass metabolism with oral bioavailability of only 35%. In the present research work, efforts were made to improve its permeation as requisite for the transdermal drug delivery system. RM was authenticated by determination of melting point. Further confirmed by ATR-FTIR, DSC and XRD. The solubility and pH dependant solubility profile was established. The purity of the received drug and estimation of the drug during the study was performed by an in-house developed novel RP-HPLC method. To determine the drug flux, permeation experiments were performed in modified Franz diffusion cells using dialysis membrane and excised rat abdominal skin as a barrier and the flux found to be 45.4 and 29.9 µg/cm2 / h, respectively. To increase flux and permeation, permeation enhancers with different mechanisms like Isopropyl myristate (IPM), Hyaluronidase, Ethanol, Oleic acid, Dimethyl sulfoxide (DMSO), Polyethylene glycol (PEG 400) and Propylene glycol (PG) were employed in the concentration of 5%. The flux, permeability coefficient, and enhancement ratio of solutions were determined. IPM improved the drug permeation among all the permeation enhancers by 3.3 folds higher than the pure drug alone. The order of enhancing the permeation by all the permeation enhancers used was in the order PG <PEG 400<DMSO<Oleic acid <Ethanol<Hyaluronidase<IPM. This research study concluded that the IPM was selected from all the permeation enhancers used for the transdermal drug delivery system of RM.
B. K. Satheeshababu *, G. Rohith, V. G. Joshi and R. Sadashivaiah
Department of Pharmaceutics, Government College of Pharmacy, P Kalinga Rao Road, Subbaiah Circle, Bengaluru, Karnataka, India.
11 November 2020
04 March 2021
29 June 2021
01 October 2021