Abstract
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.
Publication types
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Evaluation Study
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Biocompatible Materials / chemistry
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Biocompatible Materials / metabolism
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CHO Cells
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Carrier Proteins / metabolism*
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Cricetinae
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Cricetulus
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Drug Carriers* / chemistry
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Drug Carriers* / metabolism
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Drug Delivery Systems
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Endocytosis / physiology*
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Folate Receptors, GPI-Anchored
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Folic Acid* / chemistry
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Folic Acid* / metabolism
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Folic Acid* / therapeutic use
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HeLa Cells
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Humans
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Materials Testing
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Mice
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Micelles*
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Molecular Structure
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Neoplasms / drug therapy
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Neoplasms / pathology
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Polymers / chemistry
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Polymers / metabolism
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Receptors, Cell Surface / metabolism*
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Vitamin B Complex* / chemistry
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Vitamin B Complex* / metabolism
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Vitamin B Complex* / therapeutic use
Substances
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Biocompatible Materials
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Carrier Proteins
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Drug Carriers
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Folate Receptors, GPI-Anchored
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Micelles
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Polymers
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Receptors, Cell Surface
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Vitamin B Complex
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Folic Acid