Folate-conjugated micelles and their folate-receptor-mediated endocytosis.
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.
Lu
Tiancheng
T
State Key Laboratory of Polymer Physics and Chemistry, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun 130022, China.
Sun
Jing
J
Chen
Xuexi
X
Zhang
Peibiao
P
Jing
Xiabin
X
D000818:Animals; D001672:Biocompatible Materials / Q000737:chemistry / Q000378:metabolism; D016466:CHO Cells; D002352:Carrier Proteins / Q000378:metabolism*; D006224:Cricetinae; D003412:Cricetulus; D004337:Drug Carriers / Q000737:chemistry / Q000378:metabolism; D016503:Drug Delivery Systems; D004705:Endocytosis / Q000502:physiology*; D058973:Folate Receptors, GPI-Anchored; D005492:Folic Acid / Q000737:chemistry / Q000378:metabolism / Q000627:therapeutic use; D006367:HeLa Cells; D006801:Humans; D008422:Materials Testing; D051379:Mice; D008823:Micelles; D015394:Molecular Structure; D009369:Neoplasms / Q000188:drug therapy / Q000473:pathology; D011108:Polymers / Q000737:chemistry / Q000378:metabolism; D011956:Receptors, Cell Surface / Q000378:metabolism*; D014803:Vitamin B Complex / Q000737:chemistry / Q000378:metabolism / Q000627:therapeutic use
D001672:Biocompatible Materials; D002352:Carrier Proteins; D004337:Drug Carriers; D058973:Folate Receptors, GPI-Anchored; D008823:Micelles; D011108:Polymers; D011956:Receptors, Cell Surface; D014803:Vitamin B Complex; D005492:Folic Acid