Journal
MACROMOLECULAR BIOSCIENCE
Volume 9, Issue 11, Pages 1059-1068Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/mabi.200900134
Keywords
endocytosis; folic acid; micelles; receptor; targeting
Funding
- National Natural Science Foundation of China [20674084, 20774093]
- National Fund for Distinguished Young Scholars [50425309]
- Ministry of Science and Technology of China [2009CB930102]
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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.
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