Development of drug delivery systems for taxanes using ionic gelation of carboxyacyl derivatives of chitosan.

ABSTRACT

Nanoparticles of two chitosan derivatives - N-succinyl-chitosan (SC) and N-glutaryl-chitosan (GC) - were developed as passive transport systems for taxanes (paclitaxel and docetaxel) using an ionic gelation technique with sodium tripolyphosphate. These nanoparticles had an apparent hydrodynamic diameter of 300-350nm, a ζ-potential of 25-31mV, an encapsulation efficiency of 21-26%, and a drug loading efficiency of 6-13%. DLS and SLS analysis shows that the nanoparticles have a unimodal size distribution and spherical form. Drug release kinetics of the taxane-loaded nanoparticles demonstrates that more than 50% of the loaded taxane could be released upon the degradation of the nanoparticles after targeted delivery. The drug-loaded SC and GC nanoparticles exhibit high cytotoxicity towards AGS cancer cell lines and their antitumor activity is consequently enhanced when compared with free taxanes.