title: Preparation of the thienopyridine derivatives loaded liposomes and study on the effect of compound-lipid interaction on release behavior.
abstract: The article describes characterization of two liposome formulations containing thienopyridine derivatives, namely TP-58 and TP-67. By preparing the liposomes, the concentration of the two compounds in ultrapure water was increased up to three orders of magnitude. After i.v. administration of the liposomes in rats, the initial compound plasma concentrations were enhanced more than fifty times relative to that after i.g. administration of the compound suspensions. It was found out that the release rate of TP-67 from the liposome both in vitro and in vivo was not significantly different from that of TP-58. TP-58 was more lipophilic than TP-67 according to partition coefficiency, and TP-67 had greater polarity than TP-58 based on polar surface area (PSA). With DSC, it was found out that the interaction magnitude between TP-67 and the lipid bilayer was not significantly different from that between TP-58 and the lipid bilayer, which accounted for the similarity of the two compounds in release rate both in vitro and in vivo. It indicated liposome can be used as a potential carrier for broading the application of TP-58 and TP-67. Interaction between the thienopyridine derivatives and the lipid bilayer is probably the decisive factor for compound release from the liposomes.
authors: State Key Laboratory of Biotherapy, West China Hospital, Sichuan University, Chengdu, Sichuan, China.
authors: Jing
authors: J
authors: Liu
authors: Jie
authors: J
authors: Tang
authors: Haiyun
authors: H
authors: He
authors: Lu-Lu
authors: LL
authors: Cai
authors: Yimei
authors: Y
authors: Huang
authors: Xiawei
authors: X
authors: Wei
authors: Min
authors: M
authors: Luo
authors: Bilan
authors: B
authors: Wang
authors: Xiang
authors: X
authors: Gao
authors: Chengli
authors: C
authors: Yang
authors: Tingting
authors: T
authors: Hu
authors: Xiangrong
authors: X
authors: Song
authors: Tao
authors: T
authors: Yi
authors: Li
authors: L
authors: Yang
authors: Yongmei
authors: Y
authors: Xie
authors: Aiping
authors: A
authors: Tong
authors: Lantu
authors: L
authors: Gou
authors: Yinglan
authors: Y
authors: Zhao
authors: Yu
authors: Y
authors: Zheng
mesh_terms: D000818:Animals; D002626:Chemistry, Pharmaceutical / Q000379:methods; D005260:Female; D008051:Lipid Bilayers / Q000737:chemistry*; D008081:Liposomes / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D051379:Mice; D051381:Rats; D017207:Rats, Sprague-Dawley; D058924:Thienopyridines / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics
chemical_list: D008051:Lipid Bilayers; D008081:Liposomes; D058924:Thienopyridines