Formulation and evaluation of ritonavir mucoadhesive microspheres.

Sellappan Velmurugan and Moham

Abstract

The aim of the present research was to formulate and evaluate Xanthan gum and Carbopol 940 mucoadhesive microspheres for controlled release of Ritonavir. The mucoadhesive microspheres were formulated by Ionotropic gelation technique, using sodium alginate, Xanthan gum and carbopol as mucoadhesive polymer in various proportions in combination. Further, the prepared Ritonavir mucoadhesive microspheres were characterized for particle size, morphology, entrapment efficiency, mucoadhesion, in vitro drug release, ritonavir release kinetics and compatability studies (FTIR &DSC). The Ritonavir Microspheres were free-flowing and discrete. The mean particle size ranged from 772.71 ± 4.77 µm to 941.50 ± 3.13 µm and the entrapment efficiencies ranged from 72.93 to 96.86 %. The Ritonavir entrapment efficiency was found to be dependent on type and concentration of mucoadhesive polymer used for formulation. Scanning electron microscopy revealed the surface morphology of microspheres .The FTIR & DSC study confirmed stable character of Ritonavir in the drug-loaded mucoadhesive microspheres. The crystallinity of ritonavir was found to be reduced in prepared mucoadhesive microspheres, which were confirmed by XRD studies. The mechanism of Ritonavir release from the mucoadhesive microsphere was found to be anomalous and super case-II transport type. Stability studies were done for the best formulation F8 indicates that there is no change in entrapment efficiency and percentage mucoadhesion of the formulation.

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