PMID- 11166408 OWN - NLM STAT- MEDLINE DCOM- 20010510 LR - 20220318 IS - 0168-3659 (Print) IS - 0168-3659 (Linking) VI - 70 IP - 1-2 DP - 2001 Jan 29 TI - Biodegradable polymeric micelles composed of doxorubicin conjugated PLGA-PEG block copolymer. PG - 63-70 AB - 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. FAU - Yoo, H S AU - Yoo HS AD - Department of Biological Sciences, Korea Advanced Institute of Science and Technology, Taejon 305-701, South Korea. FAU - Park, T G AU - Park TG LA - eng PT - Journal Article PT - Research Support, Non-U.S. Gov't PL - Netherlands TA - J Control Release JT - Journal of controlled release : official journal of the Controlled Release Society JID - 8607908 RN - 0 (Antibiotics, Antineoplastic) RN - 0 (Micelles) RN - 0 (poly(lactic-glycolic acid)-poly(ethyleneglycol) copolymer) RN - 34346-01-5 (Polyglactin 910) RN - 3WJQ0SDW1A (Polyethylene Glycols) RN - 80168379AG (Doxorubicin) SB - IM MH - Antibiotics, Antineoplastic/*administration & dosage MH - Doxorubicin/*administration & dosage/pharmacokinetics/pharmacology MH - Flow Cytometry MH - Humans MH - Micelles MH - Polyethylene Glycols/*administration & dosage MH - Polyglactin 910/*administration & dosage MH - Tumor Cells, Cultured EDAT- 2001/02/13 11:00 MHDA- 2001/05/22 10:01 CRDT- 2001/02/13 11:00 PHST- 2001/02/13 11:00 [pubmed] PHST- 2001/05/22 10:01 [medline] PHST- 2001/02/13 11:00 [entrez] AID - S0168365900003400 [pii] AID - 10.1016/s0168-3659(00)00340-0 [doi] PST - ppublish SO - J Control Release. 2001 Jan 29;70(1-2):63-70. doi: 10.1016/s0168-3659(00)00340-0.