Preparation and characterization of mPEG grafted chitosan micelles as 5-fluorouracil carriers for effective anti-tumor activity

The objective of this study was to investigate the potential of methoxy polyethylene glycol (mPEG) grafted chitosan (mPEG-g-CS) to be used as a drug carrier. mPEG-g-CS was successfully synthesized by one-step method with formaldehyde. The substitution degree of mPEG on chitosan was calculated by elemental analysis and was found to be (3.23 +/- 0.25)%. mPEG-g-CS self-assembled micelles were prepared by ultrasonic method with the controlled size of 178.5-195.1 nm and spherical morphology. Stable dispersion of the micelles was formed with the zeta potential of 2.3-30.2 mV. 5-Fluorouracil (5-FU), an anticancer chemotherapy drug, was used as a model drug to evaluate the efficiency of the new drug delivery carrier. The loading efficiency of 5-FU was (4.01 +/- 0.03)%, and the drug-loaded mPEG-g-CS self-assembled micelle showed a controlled-release effect. In summary, the mPEG-g-CS self-assembled micelle is proved to be a promising carrier with controlled particle size and controlled-release effect. Therefore, it has great potential for the application as 5-FU carriers for effective anti-tumor activity. (C) 2014 Feng Gao. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved.