PMID- 15081218
OWN - NLM
STAT- MEDLINE
DCOM- 20050125
LR  - 20220309
IS  - 0168-3659 (Print)
IS  - 0168-3659 (Linking)
VI  - 96
IP  - 2
DP  - 2004 Apr 28
TI  - Folate receptor targeted biodegradable polymeric doxorubicin micelles.
PG  - 273-83
AB  - Biodegradable polymeric micelles, self-assembled from a di-block copolymer of 
      poly(D,L-lactic-co-glycolic acid) (PLGA) and poly(ethylene glycol) (PEG), were 
      prepared to achieve folate receptor targeted delivery of doxorubicin (DOX). In 
      the di-block copolymer structure of PLGA-b-PEG, DOX was chemically conjugated to 
      a terminal end of PLGA to produce DOX-PLGA-mPEG, and folate was separately 
      conjugated to a terminal end of PEG to produce PLGA-PEG-FOL. The two di-block 
      copolymers with different functional moieties at their chains ends were 
      physically mixed with free base DOX in an aqueous solution to form mixed 
      micelles. It was expected that folate moieties were exposed on the micellar 
      surface, while DOX was physically and chemically entrapped in the core of 
      micelles. Flow cytometry and confocal image analysis revealed that folate 
      conjugated mixed micelles exhibited far greater extent of cellular uptake than 
      folate unconjugated micelles against KB cells over-expressing folate receptors on 
      the surface. They also showed higher cytotoxicity than DOX, suggesting that 
      folate receptor medicated endocytosis of the micelles played an important role in 
      transporting an increased amount of DOX within cells. In vivo animal experiments, 
      using a nude mice xenograft model, demonstrated that when systemically 
      administered, tumor volume was significantly regressed. Biodistribution studies 
      also indicated that an increased amount of DOX was accumulated in the tumor 
      tissue.
FAU - Yoo, Hyuk Sang
AU  - Yoo HS
AD  - Department of Biological Sciences, Korea Advanced Institute of Science and 
      Technology, Daejeon 305-701, South Korea.
FAU - Park, Tae Gwan
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 (Carrier Proteins)
RN  - 0 (Folate Receptors, GPI-Anchored)
RN  - 0 (Micelles)
RN  - 0 (Polyesters)
RN  - 0 (Polymers)
RN  - 0 (Receptors, Cell Surface)
RN  - 0 (methoxypolyethyleneglycol-poly(lactic-co-glycolic acid))
RN  - 1SIA8062RS (Polylactic Acid-Polyglycolic Acid Copolymer)
RN  - 26009-03-0 (Polyglycolic Acid)
RN  - 33X04XA5AT (Lactic Acid)
RN  - 34346-01-5 (Polyglactin 910)
RN  - 3WJQ0SDW1A (Polyethylene Glycols)
RN  - 80168379AG (Doxorubicin)
SB  - IM
MH  - Animals
MH  - Antibiotics, Antineoplastic/administration & dosage/chemistry/*pharmacokinetics
MH  - Carrier Proteins/*metabolism
MH  - Doxorubicin/administration & dosage/chemistry/*pharmacokinetics
MH  - Female
MH  - Flow Cytometry
MH  - Folate Receptors, GPI-Anchored
MH  - Lactic Acid/*chemistry
MH  - Mice
MH  - Mice, Nude
MH  - Micelles
MH  - Microscopy, Confocal
MH  - Polyesters
MH  - Polyethylene Glycols/*chemistry
MH  - Polyglactin 910/*chemistry
MH  - Polyglycolic Acid/*chemistry
MH  - Polylactic Acid-Polyglycolic Acid Copolymer
MH  - Polymers/*chemistry
MH  - Receptors, Cell Surface/*metabolism
MH  - Time Factors
MH  - Tissue Distribution
MH  - Xenograft Model Antitumor Assays
EDAT- 2004/04/15 05:00
MHDA- 2005/01/26 09:00
CRDT- 2004/04/15 05:00
PHST- 2003/11/12 00:00 [received]
PHST- 2004/02/03 00:00 [accepted]
PHST- 2004/04/15 05:00 [pubmed]
PHST- 2005/01/26 09:00 [medline]
PHST- 2004/04/15 05:00 [entrez]
AID - S0168365904000811 [pii]
AID - 10.1016/j.jconrel.2004.02.003 [doi]
PST - ppublish
SO  - J Control Release. 2004 Apr 28;96(2):273-83. doi: 10.1016/j.jconrel.2004.02.003.