Effects of the characteristics of chitosan on controlling drug release of chitosan coated PLLA microspheres.

Chitosan has been shown to be a biomaterial with good biocompatibility, and is highly biodegradable. This study investigated the effect of post-coating PLLA microspheres with different chitosans on the initial burst and controlling the drug release of the microspheres. Without chitosan, 19.2% of encapsulated lidocaine would release from PLLA microspheres within the first hour (R1), and the time of 50% release (T50) was 25 h. After the microspheres were coated with chitosan of viscosity (eta) 384 +/- 10cp, R1 and T50 could be reduced and prolonged to 14.6% and 90 h, respectively, for all tested molecular weights (Mw) of chitosan. In the case of the same Mw of chitosan being applied, the efficacy of reducing the initial burst of drug release was higher for a lower degree of deacetylation (D.D.). With chitosan in acetic acid solution, coating the microspheres with high Mw and high viscosity could most effectively reduce the initial burst and control drug release of PLLA microspheres. For example, the microspheres coated with chitosan solution of Mw 800 kDa and eta of 1479 cp, R1 and T50 could be reduced and prolonged to 7.4% and 245 h, respectively. The study indicated that manipulating the viscosity of the chitosan solution was the most important factor in contributing to controlling the drug release of chitosan post-coated PLLA microspheres.