Citation: Dong-Jun Fu, Yu Jin, Mu-Qing Xie, Ya-Jing Ye, Dong-Dong Qin, Kai-Yan Lou, Yan-Zuo Chen, Feng Gao. Preparation and characterization of mPEG grafted chitosan micelles as 5-fluorouracil carriers for effective anti-tumor activity[J]. Chinese Chemical Letters, ;2014, 25(11): 1435-1440. doi: 10.1016/j.cclet.2014.06.027 shu

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

Dong-Jun Fu ^a ,
Yu Jin ^a ,
Mu-Qing Xie ^a ,
Ya-Jing Ye ^a ,
Dong-Dong Qin ^a ,
Kai-Yan Lou ^a,b,c ,
Yan-Zuo Chen ^a ,
Feng Gao ^a,b,c,,

1.
a Department of Pharmaceutics, School of Pharmacy, East China University of Science and Technology, Shanghai 200237, China;
2.
b Shanghai Key Laboratory of Functional Materials Chemistry, East China University of Science and Technology, Shanghai 200237, China;
3.
c Shanghai Key Laboratory of New Drug Design, East China University of Science and Technology, Shanghai 200237, China

Corresponding author: Feng Gao,
Received Date: 24 March 2014
Available Online: 5 June 2014

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.
- Self-assembled micelles,
- Methoxy polyethylene glycol grafted,
- chitosan,
- 5-Fluorouracil,
- Controlled-release
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