title: Body distributioin of RGD-mediated liposome in brain-targeting drug delivery.
abstract: RGD conjugation liposomes (RGD-liposomes) were evaluated for brain-targeting drug delivery. The flow cytometric in vitro study demonstrated that RGD-liposomes could bind to monocytes and neutrophils effectively. Ferulic acid (4-hydroxy-3-methoxycinnamic, FA) was loaded into liposomes. Rats were subjected to intrastriatal microinjections of 100 units of human recombinant IL-1beta to produce brain inflammation and caudal vein injection of three formulations (FA solution, FA liposome and RGD-coated FA liposome). Animals were sacrificed 15, 30, 60 and 120 min after administration to study the body distribution of the FA in the three formulations. HPLC was used to determine the concentration of FA in vivo with salicylic acid as internal standard. The results of body distribution indicated that RGD-coated liposomes could be mediated into the brain with a 6-fold FA concentration compared to FA solution and 3-fold in comparison to uncoated liposome. Brain targeted delivery was achieved and a reduction in dosage might be allowed.
authors.affiliation: Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, Liaoning, PR China.
authors.forename: Jing
authors.initials: J
authors.lastname: Qin
authors.forename: DaWei
authors.initials: D
authors.lastname: Chen
authors.forename: Haiyang
authors.initials: H
authors.lastname: Hu
authors.forename: MingXi
authors.initials: M
authors.lastname: Qiao
authors.forename: XiuLi
authors.initials: X
authors.lastname: Zhao
authors.forename: Baoyu
authors.initials: B
authors.lastname: Chen
mesh_terms: D000818:Animals; D001812:Blood-Brain Barrier; D001921:Brain / Q000378:metabolism*; D002478:Cells, Cultured; D003373:Coumaric Acids / Q000008:administration & dosage* / Q000378:metabolism; D004337:Drug Carriers; D016503:Drug Delivery Systems; D005434:Flow Cytometry; D006801:Humans; D008081:Liposomes; D008297:Male; D009000:Monocytes / Q000378:metabolism; D009504:Neutrophils / Q000378:metabolism; D009842:Oligopeptides; D051381:Rats; D017208:Rats, Wistar; D013387:Succinic Anhydrides; D014018:Tissue Distribution