Disigning sustained release formulation of microsphere drug delivery systems by using tropisetron as a model drug

Abstract

Tropisetron is a 5-HT₃ (5-hydroxytrypamine₃) receptor antagonist used for prevention of chemotherapy-induced nausea and vomiting. The ethyl-cellulose, sodium alginate and HPMC K15M loaded microspheres were successfully prepared by using ionic gelation technique. All the formulations were evaluated for various parameters such as particle size analysis, drug content, drug entrapment efficiency, compatibility study, in vitro dissolution study, release kinetic study and stability study. The prepared microspheres had good spherical geometry with smooth and the particle size of a microsphere was determined by optical microscopy technique and all the batches of microspheres showed uniform size distribution. The in vitro dissolution studies showed that Tropisetron microspheres formulation F₁₀ showed better sustained release effect over a period of 12 hours that contains 30% of all the three polymer. The mechanism of release was determined by fitting the release data to the various kinetic equations such as zero-order, first-order, Higuchi model, Korse meyer Peppas and finding the R² values it was observed that in present study in vitro drug release kinetic of the best formulation followed zero-order release kinetic model and drug release mechanism is anomalous diffusion coupled with erosion. Thus, from the results of the current study clearly indicate a promising potential of the tropisetron microspheres as an alternative to the conventional dosage form and can fullfil patient need by once daily medication.