LOPERAMIDE LOADED POLYMERIC NANOSPONGES FOR ENHANCED BIOAVAILABILITY: FORMULATION DEVELOPMENT AND IN-VITRO EVALUATION

Abstract

Loperamide HCl belongs to antidiarrheals group used for the treatment of variety of acute, chronic or traveler’s diarrhea by slowing down an overactive bowel leading to the decreased number of bowel movements. This study involved loperamide loaded beta cyclodextrin-based nano sponges that were found to be effective for treating diarrhea. Beta-Cyclodextrin,  polyvinyl alcohol and dimethylsulfoxide are employed to fabricate nanosponges through emulsion solvent diffusion technology with little modifications. Antidiarrheal drug loperamide HCl loaded beta cyclodextrin based nano sponges were formulated and evaluated for studying physiochemical characteristics. Fourier Transform Infrared spectroscopy and scanning electron microscopy were used for structural analysis. Drug compatibility with excipients used in the formulation was determined by FTIR analysis. The development of inclusion complexes with porous and spherical morphology was verified by FTIR without any chemical interaction between drug and polymer. Spherical, spongy, porous and nano sized three-dimensional structure was shown by scanning electron microscopy. Analysis of particle size, percent yield, drug loading and entrapment efficiency of nano sponges were also performed. The particle size of formulation was in nano size range. The percentage yield was in the range of 91 and 94%. The entrapment effectiveness and percent drug loading were between 89% and 90%. In the in-vitro release experiment, loperamide loaded beta cyclodextrin based nanosponge formulations revealed continuous drug release profile with the absence of burst release phenomenon. The findings of all the studies confirmed that encapsulation of drug in nanosponges led to improvement in its efficacy in terms of its solubility, dissolution , release and therapeutic applications.