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Pharmacokinetics and targeting property of TFu-loaded liposomes with different sizes after intravenous and oral administration.

Abstract：

: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.

journal_name

J Drug Target

journal_title

Journal of drug targeting

authors

Sun W,Zou W,Huang G,Li A,Zhang N

doi

10.1080/10611860801927598

subject

Has Abstract

pub_date

2008-06-01 00:00:00

pages

357-65

issue

5

eissn

1061-186X

issn

1029-2330

pii

793648803

journal_volume

16

pub_type

杂志文章

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