A COMPARATIVE EVALUATION OF PERMEATION ENHANCERS FOR ROPINIROLE HYDROCHLORIDE A BCS CLASS III DRUG TO BE FORMULATED AS TRANSDERMAL DRUG DELIVERY SYSTEMAbstract
Ropinirole hydrochloride, a non-ergoline dopamine agonist, administered orally for the treatment of Parkinson’s disease and restless leg syndrome and belonged to BCS class III drug having high solubility and low permeability. The objective of the present research study was to enhance the permeability of ropinirole hydrochloride by selecting a suitable permeation enhancing agent from different classes of permeation enhancers. Received pure drug was authenticated by determining its melting point, solubility, stability, apparent partition coefficient and using analytical tools like FTIR, DSC, PXRD and RP-HPLC. The permeation enhancing activity of eight different permeation enhancers was determined in a modified Franz-diffusion cell, the barrier used was rat abdominal skin. The donor compartment consists of an aqueous solution of drug alone, and with a 5% w/v permeation enhancer, and the receptor compartment consists of phosphate-buffered saline pH 7.4. The results of the research study suggested that the received drug was authentic and its purity at par with official pharmacopeia. The ex-vivo permeation kinetic studies showed that all the permeation enhancers are enhancing the drug permeation rate. The enhancement effect of different enhancers was in the following order of isopropyl myristate > dimethyl sulfoxide > groundnut oil > ethanol > β-cyclodextrin > oleic acid > tween 80 > hyaluronidase. Isopropyl myristate has got high permeation enhancing activity with the highest steady-state flux of 22.846 ± 0.549 μg/cm2/h, and permeation enhancement rate was 4.16 folds higher than the pure drug with no enhancer, indicating isopropyl myristate is to be the best permeation enhancers than others. The study reveals that isopropyl myristate was a suitable permeation enhancer to formulate a transdermal drug delivery system of ropinirole hydrochloride.
R. Sadashivaiah, B. K. S. Babu * and G. Rohith
Department of Pharmaceutics, Government College of Pharmacy, Bengaluru, Karnataka, India.
25 November 2019
24 February 2020
11 March 2020
01 December 2020