Comparison in docetaxel-loaded nanoparticles based on three different carboxymethyl chitosans

Abstract

In this study, three different carboxymethyl chitosans (CMCs), namely O-carboxymethyl chitosan (OC), N-carboxymethyl chitosan (NC) and N,O-carboxymethyl chitosan (NOC), were prepared as nano-carriers for an anti-tumor drug, docetaxel (DCT). Three CMCs were fabricated into drug-loading nanoparticles under different preparing conditions respectively. A series of characterization parameters were determined including drug loading capacity (DC), entrapment efficiency (EE), particle size distribution, zeta potential, and morphology, which were used to find the optimized preparing condition for three kinds of nanoparticles (NPs). Furthermore, the in vitro drug release profiles of all the three kinds of nanoparticles showed a sustained release behavior and the release rate of OC-NPs was the fastest. Moreover, compared with NC-NPs and NOC-NPs, OC-NPs exhibited more cellular accumulation in the human gastric carcinoma cells (SGC 7901) as quantitatively determined by the flow cytometry and also much stronger cytotoxicity against these cells. Accordingly, our results showed that drug-loaded nanoparticles formed by different CMCs have dissimilar physiochemical characteristics which subsequently influence their therapeutic effects. We suggest that OC-based nanoparticle is a more desirable anti-tumor drug delivery system than NC-NP and NOC-NP.

Keywords: Anti-tumor; Carboxymethyl chitosan; Nanoparticle.