OPTIMIZATION AND EVALUATION OF NANOPARTICULATE SUSTAINED RELEASE DOSAGE FORM OF ANTISPASMODIC DRUG

Abstract

This study aimed to select or modify the polymer matrix composition to achieve high entrapment of hydrophilic drugs in polymeric nanoparticles (NPs). Alverine Citrate, the bioactive drug, was selected as a representative hydrophilic drug. The nanoprecipitation method was used for the preparation of Alverine Citrate -loaded NPs. Concentrations of polymers were optimized by a 3-level factorial design, which affected the particle size and encapsulation efficiency. The formulation was subjected to morphological, physicochemical, and in vitro drug release studies. The mean particle size of nanoparticles was around 114.8 nm, as estimated with a particle size analyzer. TEM observations revealed a spherical shape. Fourier transform infrared analysis did not reveal any chemical interaction between the drug and polymers used for the nano-formulation. A release study conducted in vitro over a period of 24 h indicated primarily burst release after that sustained release of Alverine Citrate from the formulation. The release kinetics studies revealed that drug release from the nanoparticles follows the Korsmeyer Peppas model. The study demonstrates the benefit of excipient screening techniques in improving entrapment efficiency of a hydrophilic drug.