Folate-receptor-targeted delivery of docetaxel nanoparticles prepared by PLGA-PEG-folate conjugate

For folate-receptor-targeted anticancer therapy, docetaxel (DTX) nanoparticles (NPs) were produced employing polylactide-co-glycolide-polyethylene glycol-folate (PLGA-PEG-FOL) conjugate. The FOL-conjugated di-block copolymer was synthesized by coupling the PLGA-PEG-NH2 di-block copolymer with an act...

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Bibliographic Details
Published in:Journal of drug targeting 2008-01, Vol.16 (5), p.415-423
Main Authors: Esmaeili, Farnaz, Ghahremani, Mohammad Hossein, Ostad, Seyed Nasser, Atyabi, Fatemeh, Seyedabadi, Mohammad, Malekshahi, Mazda Rad, Amini, Mohsen, Dinarvand, Rassoul
Format: Article
Language:English
Subjects:
Antineoplastic Agents - administration & dosage
Antineoplastic Agents - pharmacokinetics
Antineoplastic Agents - pharmacology
Biological and medical sciences
Carrier Proteins - metabolism
Cell Line, Tumor
Cell Survival - drug effects
Chromatography, High Pressure Liquid
docetaxel
Drug Carriers
Endocytosis - physiology
Excipients
Folate
Folate Receptors, GPI-Anchored
Folic Acid - chemistry
General pharmacology
Humans
Lactic Acid - chemistry
Medical sciences
nanoparticle
Nanoparticles
nanotechnology
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
PLGA
Polyethylene Glycols - chemistry
Polyglycolic Acid - chemistry
Receptors, Cell Surface - metabolism
targeted delivery
Taxoids - administration & dosage
Taxoids - pharmacokinetics
Taxoids - pharmacology
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Summary:For folate-receptor-targeted anticancer therapy, docetaxel (DTX) nanoparticles (NPs) were produced employing polylactide-co-glycolide-polyethylene glycol-folate (PLGA-PEG-FOL) conjugate. The FOL-conjugated di-block copolymer was synthesized by coupling the PLGA-PEG-NH2 di-block copolymer with an activated folic acid. It was expected that FOL moieties were exposed on the micellar surface. The conjugates assisted in the formation of DTX NPs with an average size of 200 nm in diameter through an emulsification/solvent diffusion method. The FOL-targeted NPs showed a greater extent of intracellular uptake in FOL-receptor-positive cancer cells (SKOV3) in comparison with the non-targeted NPs, indicating that the FOL-receptor-mediated endocytosis mechanism could have a role in the cellular uptake of NPs. These results suggested that FOL-targeted DTX NPs could be a potentially useful delivery system for FOL-receptor-positive cancer cells.
ISSN:1061-186X
1029-2330
DOI:10.1080/10611860802088630