title: 5-Fluorouracil-loaded PLA/PLGA PEG-PPG-PEG polymeric nanoparticles: formulation, in vitro characterization and cell culture studies.
abstract: In this study, 5-FU, a potent anticancer drug, is planned to be delivered via a new and promising drug delivery system, nanoparticles formed with hydrophobic core polymer and triblock copolymers; Poly(DL-lactic acid), Poly(ethylene glycol)-block-poly(propylene glycol)-block-poly(ethylene glycol) copolymer (PLA/PEG-PPG-PEG) and Poly(D,L-lactide-co-glycolide)/Poly(ethylene glycol)-block-poly(propylene glycol)-block-poly(ethylene glycol) copolymer (PLGA/PEG-PPG-PEG) nanoparticles. Particle size range of nanoparticles was found to be between 145 and 198 nm, which would promote the passive targeting of the nanoparticles to tumor cells based on the enhanced permeability and retention (EPR) effect. SEM images revealed all nanoparticles formulations to be spherical and without pores. Zeta potential, yield value and encapsulation efficiencies of 5-FU-loaded nanoparticles were within the range of -11.1 and -13.7 mV, 72.7-87.7% and 83.6-93.9%, respectively. Cumulative release of 5-FU was observed between 90% and 94.4% in all nanoparticle formulations by the end of 72 h, and fitness of release profiles to Higuchi model indicated matrix-controlled diffusion of the 5-FU from polymeric nanoparticles. Cell viability values of the cells treated with 5-FU-loaded nanoparticles were obtained as low as 47% and 52% with tetrazolium dye assay, suggesting that delivery of 5-FU via amphiphilic triblock copolymer nanoparticles would be a promising delivery system because of the EPR effect.
authors.affiliation: Department of Pharmaceutical Technology, Faculty of Pharmacy, Hacettepe University , Sıhhiye-Ankara , Turkey and.
authors.forename: Harika
authors.initials: H
authors.lastname: Ocal
authors.forename: Betül
authors.initials: B
authors.lastname: Arica-Yegin
authors.forename: Imran
authors.initials: I
authors.lastname: Vural
authors.forename: Katerina
authors.initials: K
authors.lastname: Goracinova
authors.forename: Sema
authors.initials: S
authors.lastname: Caliş
mesh_terms: D000964:Antimetabolites, Antineoplastic / Q000008:administration & dosage* / Q000494:pharmacology; D018938:Caco-2 Cells; D002470:Cell Survival / Q000187:drug effects; D002626:Chemistry, Pharmaceutical / Q000379:methods; D004337:Drug Carriers / Q000737:chemistry; D016503:Drug Delivery Systems; D005472:Fluorouracil / Q000008:administration & dosage* / Q000494:pharmacology; D006801:Humans; D019344:Lactic Acid / Q000737:chemistry; D008855:Microscopy, Electron, Scanning; D053758:Nanoparticles; D010316:Particle Size; D011091:Polyesters; D011092:Polyethylene Glycols / Q000737:chemistry; D011100:Polyglycolic Acid / Q000737:chemistry; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011108:Polymers / Q000737:chemistry*; D011409:Propylene Glycols / Q000737:chemistry
chemical_list: D000964:Antimetabolites, Antineoplastic; D004337:Drug Carriers; D011091:Polyesters; D011108:Polymers; D011409:Propylene Glycols; C528875:poly(ethylene glycol)-block-poly(propylene glycol)-block-poly(ethylene glycol) copolymer; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D011092:Polyethylene Glycols; C033616:poly(lactide); D005472:Fluorouracil