In vitro and in vivo Evaluation of Pramipexole HCl Mucoadhesive Microspheres

Abstract

The study was aimed to design and develop the novel gastro retentive mucoadhesive Pramipexole microspheres using ionotropic gelation technique. Based on the results of Micromeretic properties confirmed that microspheres were free flowing with good pack ability. The optimized M13 formulation displayed the % entrapment efficiency 96.07%, % yield 98.01%, swelling index 96.08% and Mucoadhesiveness was 95.42%. The in vitro drug release showed the sustained release of Pramipexole up to 99.16 ± 5.12% within 12 h. FTIR studies revealed incompatibility was not found between drug and excipients. SEM confirmed the particles were of spherical in shape. Optimized formulation (M13) were stable at 40°C ± 2°C/75% RH ± 5% RH for 6 months. In vivo studies were performed and kinetic parameters like Cmax, Tmax, AUC0-t, AUC0-∞ and t1/2 were calculated. The marketed product Cmax (2.19 ± 0.01 ng/ml) was higher than optimized formulation (2.0 ± 0.01 ng/ml). The optimized formulation AUC0-t (20.15 ± 1.12 ng.hr/ml), AUC0-∞ (27.42 ± 1.16 ng.hr/ml) was significantly higher than that of marketed product AUC0-t (13.21 ± 1.26 ng.hr/ml) and AUC0-∞ (19.15 ± 1.13 ng.hr/ml) respectively. Which indicated the optimized formulation bioavailability was higher than marketed product. Microspheres would be a promising drug delivery system which plays potentially significant role in pharmaceutical drug delivery in the efficient management of Parkinson’s disease.