Folate-Conjugated Micelles and Their Folate-Receptor-Mediated Endocytosis

被引：51

作者：

Lu, Tiancheng ^{[1
,2
,3
]}

Sun, Jing ^{[1
,3
]}

Chen, Xuexi ^{[1
]}

Zhang, Peibiao ^{[1
]}

Jing, Xiabin ^{[1
]}

机构：

[1] Chinese Acad Sci, State Key Lab Polymer Phys & Chem, Changchun Inst Appl Chem, Changchun 130022, Peoples R China

[2] Jilin Agr Univ, Sch Life Sci, Changchun 130118, Peoples R China

[3] Chinese Acad Sci, Grad Sch, Beijing 100039, Peoples R China

来源：

MACROMOLECULAR BIOSCIENCE | 2009年 / 9卷 / 11期

基金：

中国国家自然科学基金;

关键词：

endocytosis; folic acid; micelles; receptor; targeting; BLOCK-COPOLYMER MICELLES; ANTICANCER DRUG-DELIVERY; BRAIN ENDOTHELIAL-CELLS; POLYMERIC MICELLES; TUMOR-CELLS; CANCER-CELLS; IN-VITRO; DOXORUBICIN; NANOPARTICLES; PH;

D O I：

10.1002/mabi.200900134

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

070307 [化学生物学]; 071010 [生物化学与分子生物学];

摘要：

A folate-conjugated copolymer PEG-PLA-PLL/folate was synthesized and mixed with pure PEG-PLA-PLL and a fluorescent model drug mFITC to prepare folate-conjugated micelles. The distribution of micelles was studied on cancer-cell-bearing mice via frozen slicing. The results show that mFITC is successfully encapsulated into folate(+) and folate(-)micelles; PEG-PLA-PLL micelles the latter can be internalized by both HeLa and CHO cells without selectivity due to their cationic surface charges, while folate(+)micelles exhibit more preferential endocytosis by HeLa cells than by CHO cells. The folate(-)micelles showed retention in both organs and tumors. The folate(+)micelles are a promising active targeting drug delivery system for FR over-expressing cells and they accumulate in tumor beds.

引用

页码：1059 / 1068

页数：10

共 40 条

[1]

Bae Y, 2005, MOL BIOSYST, V1, P242, DOI 10.1039/b500266d

[2]

BIRN H, 1997, AM J PHYSIOL-RENAL, V272, P70

[3]

CAMPBELL IG, 1991, CANCER RES, V51, P5329

[4]

STUDIES ON THE INVIVO DISPOSITION OF ADRIAMYCIN IN HUMAN-TUMORS WHICH EXHIBIT DIFFERENT RESPONSES TO THE DRUG [J].