Biodegradable polymeric micelles composed of doxorubicin conjugated PLGA-PEG block copolymer

Hyuk Sang Yoo, Tae Gwan Park

Research output: Contribution to journalArticlepeer-review

519 Scopus citations

Abstract

Biodegradable polymeric micelles containing doxorubicin in the core region were prepared from a di-block copolymer composed of doxorubicin-conjugated poly(DL-lactic-co-glycolic acid) (PLGA) and polyethyleneglycol (PEG). The di-block copolymer of PLGA-PEG was first synthesized and the primary amino group of doxorubicin was then conjugated to the terminal hydroxyl group of PLGA, which had been pre-activated using p-nitrophenyl chloroformate. The resulting polymeric micelles in aqueous solution were characterized by measurement of size, drug loading, and critical micelle concentration. The micelles containing chemically-conjugated doxorubicin exhibited a more sustained release profile than PEG-PLGA micelles containing physically-entrapped doxorubicin. The cytotoxic activity of the micelles against HepG2 cells was greater than free doxorubicin, suggesting that the micelles containing conjugated doxorubicin were more effectively taken up cellularly, by an endocytosis mechanism rather than by passive diffusion. Confocal microscopic observation and flow cytometry analysis supported the enhanced cellular uptake of the micelles.

Original languageEnglish
Pages (from-to)63-70
Number of pages8
JournalJournal of Controlled Release
Volume70
Issue number1-2
DOIs
StatePublished - Jan 29 2001
Externally publishedYes

Funding

This study was supported by the Center for Advanced Functional Polymers, KAIST, Korea.

Keywords

  • Biodegradable
  • Doxorubicin
  • Endocytosis
  • Micelles
  • PLGA

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