Development of new chitosan-cellulose multicore microparticles for controlled drug delivery

Chitosan (CS) is a very interesting biomaterial for drug delivery; however its use in oral administration is restricted by its fast dissolution in the stomach and limited capacity for controlling the release of drugs. To address this limitation, a new microparticulate CS controlled release system, consisting of hydrophilic CS microcores entrapped in a hydrophobic cellulosic polymer, such as cellulose acetate butyrate (CAB) or ethyl cellulose (EC) was proposed. These microparticles were obtained with different types of CS and various core/coat ratios, with the particle size in all cases being smaller that 70 microns. Using sodium diclofenac (SD) and fluorescein isothiocyanate-labeled bovine serum albumin (FITC-BSA) as model compounds, the properties of these new microparticles for the entrapment and controlled release of drugs and proteins were investigated. Results showed that the entrapment efficiency of SD was very high irrespective of the processing conditions. Furthermore, for both model compounds (SD and FITC-BSA) it was possible to modulate the in vitro release of the encapsulated molecules by changing the core properties (CS salt, Mw, core/coat ratio) or the coating polymer. The microparticles were stable at low pH and thus, suitable for oral delivery without requiring any harmful cross-linkage treatment.