Čes. slov. farm. 2014, 63(3):127-135 | DOI: 10.36290/csf.2014.026

Impact of formulation and process parameters on the properties of chitosan-based microspheres prepared by external ionic gelation

Romana Kubánková, Jakub Vysloužil, Martina Kejdušová, David Vetchý, Kateřina Dvořáčková^*

Veterinární a farmaceutická univerzita Brno, Farmaceutická fakulta, Ústav technologie léků, Brno

The aim of this experimental study was to optimize a preparation of microspheres from high viscosity chitosan by external ion gelation and to evaluate selected aspects of their preparation. For drug-free microparticles, the concentration of chitosan dispersions was chosen as a formulation variable; the position of instrument for a dispersion extrusion (horizontal vs. vertical) was evaluated as a process variable. On the basis of sphericity and equivalent diameter results, three different concentrations of chitosan dispersions were used for 5-aminosalicylic acid (5-ASA) encapsulation with the extrusion instrument in horizontal position, which was considered as the optimal. In consequent drug-loaded microparticle preparation, the influence of the concentration of chitosan dispersions and composition of hardening solution (10% sodium tripolyphosphate (TPP) vs. 10% TPP containing drug) was evaluated. In prepared 5-ASA microspheres it was found that the equivalent diameter increased with increasing chitosan concentration. In the case of sphericity, significant differences were not found. Samples prepared with the drug in both chitosan dispersion and hardening solution had a higher drug content, a smaller equivalent diameter and they showed a faster in vitro drug release in comparison with the samples prepared with the drug in chitosan dispersion only.

Keywords: microparticles; external ionic gelation; chitosan; formulation and process parameters; dissolution profile

Received: May 21, 2014; Accepted: May 30, 2014; Published: March 1, 2014  Show citation