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-NH(2) 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.
Esmaeili
Farnaz
F
Novel Drug Delivery Systems Laboratory, Faculty of Pharmacy, Medical Sciences, University of Tehran, Tehran, Iran.
Ghahremani
Mohammad Hossein
MH
Ostad
Seyed Nasser
SN
Atyabi
Fatemeh
F
Seyedabadi
Mohammad
M
Malekshahi
Mazda Rad
MR
Amini
Mohsen
M
Dinarvand
Rassoul
R
D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D002352:Carrier Proteins / Q000378:metabolism*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D002851:Chromatography, High Pressure Liquid; D000077143:Docetaxel; D004337:Drug Carriers; D004705:Endocytosis / Q000502:physiology; D005079:Excipients; D058973:Folate Receptors, GPI-Anchored; D005492:Folic Acid / Q000737:chemistry*; D006801:Humans; D019344:Lactic Acid / Q000737:chemistry*; D053758:Nanoparticles; D011092:Polyethylene Glycols / Q000737:chemistry*; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011956:Receptors, Cell Surface / Q000378:metabolism*; D043823:Taxoids / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology
D000970:Antineoplastic Agents; D002352:Carrier Proteins; D004337:Drug Carriers; D005079:Excipients; D058973:Folate Receptors, GPI-Anchored; D011956:Receptors, Cell Surface; D043823:Taxoids; D000077143:Docetaxel; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D011092:Polyethylene Glycols; D005492:Folic Acid