Premium
Folate‐Conjugated Micelles and Their Folate‐Receptor‐Mediated Endocytosis
Author(s) -
Lu Tiancheng,
Sun Jing,
Chen Xuexi,
Zhang Peibiao,
Jing Xiabin
Publication year - 2009
Publication title -
macromolecular bioscience
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.924
H-Index - 105
eISSN - 1616-5195
pISSN - 1616-5187
DOI - 10.1002/mabi.200900134
Subject(s) - micelle , folate receptor , endocytosis , chemistry , conjugated system , hela , biophysics , drug delivery , peg ratio , cationic polymerization , prodrug , cell , cancer cell , biochemistry , organic chemistry , cancer , biology , aqueous solution , finance , economics , genetics , polymer
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 r e sults 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.