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

Int J Biol Macromol

Laboratory of Chemical Process Engineering, Department of Process Engineering, Faculty of Technology, Ferhat Abbas Sétif1University, 19000 Sétif, Algeria. Electronic address:

Published: July 2023

AI Article Synopsis

  • The study focused on creating microspheres containing Mesalazine (5-ASA) for targeted drug delivery to the colon, using an emulsion solvent evaporation method.
  • The formulation included sodium alginate and ethylcellulose as encapsulating agents and polyvinyl alcohol as an emulsifier while examining the impact of various processing parameters on the microspheres' properties.
  • Characterization methods included optical microscopy and spectroscopy, and drug release was tested in simulated gastric and intestinal fluids, with kinetic results analyzed under specific mathematical models to evaluate drug liberation.

Article 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.

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http://dx.doi.org/10.1016/j.ijbiomac.2023.124894DOI Listing

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