Preparation, Optimization and In vitro Evaluation of Glipizide Nanoparticles Integrated with Eudragit RS-100.

Abstract

Background: Solubility is an important criterion for drug efficacy, independent of the route of administration. It also poses a major challenge for pharmaceutical indus-tries, which are developing new pharmaceutical products, since 40% of the active sub-stances being identified are either insoluble or poorly soluble in aqueous media. Objective: The objective of this study was to develop nanoformulation of glipizide drug-loaded nanoparticles providing controlled release formulation. Method: Nanoparticles were prepared by the solvent evaporation method. Eudragit RS100, a nonbiodegradable polymer with varying ratios was used for making the formula-tion. The effect of key formulation variables on the particle size and entrapment efficien-cy and drug loading of nanoparticles were studied by using factorial design. Results: DSC thermograms indicate that glipizide was dispersed in an amorphous state in the polymer. TEM study indicates that the nanoparticles were in spherical shape. The mean diameter was dependent on the presence of the amount of Eudragit RS100 and vis-cosity of the organic phase. The in vitro study showed that the cumulative drug release was from 69.52-81.44% in 10 hrs at pH 6.8 in phosphate buffer respectively. Conclusion: The developed NPs could reduce dose frequency, decrease side effects, and improve patient compliance. Using factorial design, maximum entrapment efficiency with minimum particle size could be achieved with a few experiments.