期刊
JOURNAL OF COLLOID AND INTERFACE SCIENCE
卷 354, 期 1, 页码 202-209出版社
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.jcis.2010.10.054
关键词
Poly(epsilon-caprolactone-co-4-maleate-epsilon-caprolactone); Nanoparticles; Folate; 5-Fluorouracil; Anti-tumor effect
资金
- Fundamental Research Funds for the Central Universities
- National Natural Science Foundation of China [20804015]
- Specialized Research Fund for the Doctoral Program of Higher Education [200802511021]
- Natural Science Foundation of Shanghai [08ZR1406000]
- Shanghai Key Laboratory [08DZ2230500]
- Program for Changjiang Scholars and Innovative Research Team in University [IRT0825]
In this paper, folate conjugated poly(epsilon-caprolactone-co-4-maleate-epsilon-caprolactone) (P(CL-co-MCL)-folate) was prepared by a carbodiimide coupling reaction, i.e., the vitamin folic acid (FA) was covalently linked to the main chain of the maleate-functionalized polymer, poly(epsilon-caprolactone-co-4-maleate-epsilon-caprolactone) (P(CL-co-MCL)). Then the 5-Fluorouracil (5-FU) loaded nanoparticles of P(CL-co-MCL)-folate were achieved by solvent-evaporation method. Their properties were extensively studied by dynamic light scattering (DLS) and scan electron microscopy (SEM). DLS and SEM showed that the nanoparticles were in a well-defined spherical shape with a uniform size distribution. We also investigated the entrapment and in vitro release behavior, which indicated that the release speed of 5-FU could be well controlled and the release half-life period could reach 16.86 h, which was 26.4 times longer than that of pure 5-FU. The in vitro targeting test displayed that the 5-FU loaded P(CL-co-MCL)-folate nanoparticles exhibited an enhanced cell inhibition because folate targeting increased the concentration of 5-FU loaded P(CL-co-MCL)-folate nanoparticles in the tumor cells with folate receptor overexpressed. Meanwhile, the tumor inhibition of 5-FU loaded P(CL-co-MCL)-folate nanoparticles was much higher than that of pure 5-FU and that of 5-FU loaded P(CL-co-MCL) nanoparticles. Therefore, P(CL-co-MCL)-folate nanoparticles would be highly beneficial for biomedical and pharmaceutical applications. (C) 2010 Elsevier Inc. All rights reserved.
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