Preparation of the thienopyridine derivatives loaded liposomes and study on the effect of compound-lipid interaction on release behavior.

State Key Laboratory of Biotherapy, West China Hospital, Sichuan University, Chengdu, Sichuan, China.

Drug delivery 2012 Jun-Jul

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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.

Citation

Jing Liu, Jie Tang, Haiyun He, Lu-Lu Cai, Yimei Huang, Xiawei Wei, Min Luo, Bilan Wang, Xiang Gao, Chengli Yang, Tingting Hu, Xiangrong Song, Tao Yi, Li Yang, Yongmei Xie, Aiping Tong, Lantu Gou, Yinglan Zhao, Yu Zheng. Preparation of the thienopyridine derivatives loaded liposomes and study on the effect of compound-lipid interaction on release behavior. Drug delivery. 2012 Jun-Jul;19(5):247-54