Pharmacokinetics and targeting property of TFu-loaded liposomes with different sizes after intravenous and oral administration
Pharmacokinetics and targeting property of TFu-loaded liposomes with different sizes after intravenous and oral administration
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DOI：
10.1080/10611860801927598
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发表时间：
2008-01-01
影响因子：
4.5
通讯作者：
Zhang, Na
中科院分区：
文献类型：
--
作者：
Sun, Weitong;Zou, Weiwei;Zhang, Na
本研究的目的是开发用于口服和静脉内（i. v.）给药后，阐明了载TFu脂质体的生物分布特征和体内药代动力学行为。制备并表征了四种不同大小的载TFu脂质体。研究了不同粒径的TFu脂质体在小鼠体内的药代动力学和生物分布。药物动力学研究表明，不同粒径的脂质体口服给药后的生物利用度均高于混悬液，且随着脂质体粒径的减小，胃肠道吸收增加。静脉注射给药后，较大的载TFu脂质体（530和400 nm）显示出较高的肝和脾靶向特性和较低的心脏和肾脏蓄积，而较小尺寸的脂质体（180 nm）显着提高药物血浆浓度，生物利用度和延长的保留时间在循环中。因此，可以得出结论，口服和可注射的载TFu的脂质体都是有前途的抗癌制剂，可提高生物利用度;较大尺寸的脂质体是通过静脉内给药用于肝癌和脾瘤的潜在被动靶向治疗剂，而较小的脂质体由于其增强口服吸收的可能性而可能优选用于口服给药。因此，不同大小的载TFu脂质体可能根据不同的治疗目的而具有不同的临床应用。
The purpose of the study was to develop the liposomal formulations of TFu for oral and intravenous (i.v.) administration, clarify the biodistribution characteristics and in vivo pharmacokinetic behaviors of TFu-loaded liposomes. Four TFu-loaded liposomes of different sizes were prepared and characterized. The pharmacokinetic characteristics and the biodistribution of TFu-loaded liposomes with different sizes were investigated after i.v. or oral administration to mice. The pharmacokinetic studies indicated that TFu-loaded liposomes with different sizes all resulted in higher bioavailabilities than the TFu suspension after oral administration, and the gastrointestinal absorption increased with the reduction in liposome sizes. Following i.v. administration to mice, larger TFu-loaded liposomes (530 and 400 nm) showed higher hepatic and splenic targeting properties and lower cardiac and renal accumulations, while smaller sized liposomes (180 nm) significantly enhanced drug plasma concentration, bioavailability and prolonged retention time in circulation. Therefore, it can be concluded that both the oral and the injectable TFu-loaded liposomes are promising anticancer formulations for improved bioavailability; larger sized liposomes are potential passive targeting therapeutic agents for hepatoma and splenoma through i.v. administration while smaller liposomes might be preferable for oral administration due to its enhancing oral absorption possibility. Consequently, TFu-loaded liposomes with different sizes might have different clinical applications according to different goals of treatment.