Folate-conjugated Micelles Based on Star-shaped PLGA-PEG-NH2 Copolymers as Novel Tumor-targeted Nanocarriers

doi:10.3969/j.issn.0251-0790.2012.08.039

Abstract

Abstract: A new type of folic acid(FA)-conjugated amphiphilic 4-arm star-shaped PLGA-PEG-NH₂(4s-PLGA-PEG-NH₂) micelles was prepared as a doxorubicin(DOX)-loaded nanocarrier for tumor-targeted drug delivery. The 4s-PLGA-PEG-NH₂ micelles were prepared by a solvent evaporation method; then, FA was conjugated onto the surface of the micelles using 1-ethyl-3-(3-dimethylaminopropyl)-carbodiimide hydrochloride(EDC) conjugation chemistry. The structure of the synthesized 4s-PLGA-PEG-NH₂ copolymer was characterized by ¹H NMR and gel permeation chromatography(GPC). The prepared micelles properties were determined by dynamic light scattering, UV spectra and TEM observation. The cellular uptake and cytotoxicity of FA-conjugated DOX-4s-PLGA-PEG-NH₂ micelles were assessed using confocal laser scanning microscopy(CLSM) and the cell counting kit-8 assay. The results show that compared with the nontargeted DOX-micelles, FA-DOX-micelles have higher cellular uptake of DOX, and subsequently a higher cytotoxicity to tumor cells. In conclusion, the FA-conjugated 4s-PLGA-PEG-NH₂ micelles could be an excellent nanocarrier to deliver anticancer drugs specifically inside the cell via FA-receptor-medicated endocytosis.

Key words: Star-shaped copolymer, PLGA-PEG-NH₂, Nano-micelle, Folic acid, Targeted carrier

CLC Number:

O631

TrendMD:

MA Gui-Lei, ZHAO Shun-Xin, JIN Xu, CHEN Min-Min, ZHANG Zheng-Pu, SONG Cun-Xian. Folate-conjugated Micelles Based on Star-shaped PLGA-PEG-NH₂ Copolymers as Novel Tumor-targeted Nanocarriers[J]. Chem. J. Chinese Universities, 2012, 33(08): 1854.

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Folate-conjugated Micelles Based on Star-shaped PLGA-PEG-NH₂ Copolymers as Novel Tumor-targeted Nanocarriers

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