title: Characterization, blood profile and biodistribution properties of surface modified PLGA nanoparticles of SN-38.
abstract: SN-38, the active metabolite of irinotecan, poses a challenge in terms of drug delivery due to its low solubility and labile lactone ring. The aim of this study was to develop a SN-38 nanoparticulate delivery system to evaluate the in vivo blood profile and biodistribution properties of nanoparticles (NPs). Poly lactide-co-glycolide (PLGA) NPs that were covalently bound to polyethylene glycol-folate (PEG-FOL) were prepared, and their in vivo biodistribution in rats was investigated. Either the SN-38 solution or SN-38 NP suspension was administered intravenously into the tail vein at a dose of 2mg SN-38 eq./kg. As expected, SN-38 NPs showed a higher plasma concentration in vivo when compared with free SN-38 during a 24h period. Compared with the SN-38 solution, both folate targeted and non-targeted NPs exhibited superior drug concentration in body organs such as the liver, spleen, and lung at 1 and 8h post-administration.
authors.affiliation: Department of Pharmaceutics, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, PO Box 14159-6451, Iran.
authors.forename: Pedram
authors.initials: P
authors.lastname: Ebrahimnejad
authors.forename: Rassoul
authors.initials: R
authors.lastname: Dinarvand
authors.forename: Mahmoud Reza
authors.initials: MR
authors.lastname: Jafari
authors.forename: Seyed Abolghasem Sajadi
authors.initials: SA
authors.lastname: Tabasi
authors.forename: Fatemeh
authors.initials: F
authors.lastname: Atyabi
mesh_terms: D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000008:administration & dosage / Q000097:blood*; D002166:Camptothecin / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000097:blood; D002626:Chemistry, Pharmaceutical; D004337:Drug Carriers / Q000138:chemical synthesis / Q000737:chemistry*; D005492:Folic Acid / Q000031:analogs & derivatives* / Q000737:chemistry; D007275:Injections, Intravenous; D000077146:Irinotecan; D019344:Lactic Acid / Q000737:chemistry*; D015394:Molecular Structure; D053758:Nanoparticles / Q000737:chemistry*; D011092:Polyethylene Glycols / Q000737:chemistry*; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D051381:Rats; D017208:Rats, Wistar; D013499:Surface Properties; D014018:Tissue Distribution
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D004337:Drug Carriers; C552831:poly(ethylene glycol)-folate; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D011092:Polyethylene Glycols; D000077146:Irinotecan; D005492:Folic Acid; D002166:Camptothecin