Preparation and in vivo evaluation of mucoadhesive microparticles containing amoxycillin-resin complexes for drug delivery to the gastric mucosa.

摘要

In this work, microparticles consisting of amoxycillin-loaded ion-exchange resin encapsulated in mucoadhesive polymers (polycarbophil and Carbopol 934) were prepared with the aim of increasing the efficacy of amoxycillin in the treatment of peptic ulcers by achieving targeted delivery to the gastric mucosa and prolonged drug release. An oil-in-oil solvent evaporation technique was conveniently modified in order to obtain polymer microparticles containing multiple amoxycillin-resin cores. Polycarbophil microparticles were spherical, Carbopol 934 microparticles irregular. In vitro release of amoxycillin was rapid with or without a polymer coating. Gastrointestinal transit in rats was investigated by fluorescence microscopy using particles loaded with fluorescein instead of amoxycillin: gastric residence time was longer, and the distribution of the particles on the mucosa apparently better, without any polymer coating.