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Formulation and Evaluation of Fast Dissolving Tablet Containing Vilazodone Nanocrystals for Solubility and Dissolution Enhancement Using Soluplus: In vitro- In vivo Study

SURENDRA GATTANI, RAJKUMAR SUKDEO MOON.


Abstract

Major problem to the development of highly effective formulation is the poor aqueous solubility of many drugs which affects stability and bioavailability of drug formulation. There is need of systematic formulation approaches to make poorly soluble drugs bioavailable. The objective of present investigation is to increase the solubility and dissolution rate of Vilazodone (VLZ) an antidepressant drug by preparing its nanoparticles using graft copolymer Soluplus and polyvinyl pyrrolidone K-30 (PVP K 30) by evaporative precipitation into aqueous solution method. The prepared nanoparticles were characterized by FTIR, DSC, XRD, SEM, Particle size by DLS and saturation solubility. The nanoparticles showed remarkable increase in the aqueous saturation solubility i.e., NP1, NP2, NP3 and NP4 shows 4.4, 4.6, 7.7 and 7.8 folds respectively increase in aqueous solubility as compared to VLZ. The nanoparticles NP4 batch with highest solubility is converted into fast dissolving tablet. The tablets were evaluated for different parameters and found to possess more dissolution (89.386% release) as compared to pure drug (51.652%). The rise in solubility and dissolution may be due to either increase in surface area due to reduction in particle size or micelles formation by Soluplus and reduction in crystallinity of drug. In vivo study reveals that optimized Vilazodone nanoparticles (VLZNP) elicited significant antidepressant like activity.

Key words: Fast dissolving tablet, Vilazodone, nanocrystals, Soluplus, solubility






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