Conception of Cellulose/Alginate/Mesalazine microspheres by solvent evaporation technique for drug release: Experimental and theoretical investigations

Abstract

Preparation of microspheres containing Mesalazine referred to as 5-aminosalicylic acid (5-ASA) for colon targeting drug was carried out using the emulsion solvent evaporation technique. The formulation was based on 5-ASA as the active agent, sodium Alginate (SA) andEthylcellulose (EC) as encapsulating agents, with polyvinyl alcohol (PVA) as emulsifier. The effects ofthe following processing parameters, 5-ASA %, EC:SA ratio and stirring rate on the properties of the resulting products in the form microspheres were considered. The samples were characterized using Optical microscopy, SEM, PXRD, FTIR, TGA, and DTG.In vitro release of 5-ASA from the different batches of microspheres was tested in biologically simulated fluids, (gastric; SGF, pH 1.2 for 2 h), then (intestinal fluid SIF, pH 7.4for 12 h) at 37 °C. The release kinetic results have been treated mathematically relaying on Higuchi's and Korsmeyer–Peppas' models for drug liberation. DOE study was performed to evaluate the interactive effects of variables on the drug entrapment and microparticle sizes. Molecular chemical interactions in structures were optimized using DFT analysis.