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CLC number: R944.9

On-line Access: 2012-12-07

Received: 2012-03-27

Revision Accepted: 2012-11-11

Crosschecked: 2012-11-14

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Journal of Zhejiang University SCIENCE B 2012 Vol.13 No.12 P.981-989

http://doi.org/10.1631/jzus.B1200098


Docetaxel-loaded liposomes: preparation, pH sensitivity, pharmacokinetics, and tissue distribution


Author(s):  Hong Zhang, Rui-ying Li, Xia Lu, Zhen-zhen Mou, Gui-mei Lin

Affiliation(s):  School of Pharmaceutical Science, Shandong University, Jinan 250012, China

Corresponding email(s):   guimeilin@sdu.edu.cn

Key Words:  Docetaxel-loaded liposomes, pH sensitivity, Pharmacokinetics, Tissue distribution


Hong Zhang, Rui-ying Li, Xia Lu, Zhen-zhen Mou, Gui-mei Lin. Docetaxel-loaded liposomes: preparation, pH sensitivity, pharmacokinetics, and tissue distribution[J]. Journal of Zhejiang University Science B, 2012, 13(12): 981-989.

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author="Hong Zhang, Rui-ying Li, Xia Lu, Zhen-zhen Mou, Gui-mei Lin",
journal="Journal of Zhejiang University Science B",
volume="13",
number="12",
pages="981-989",
year="2012",
publisher="Zhejiang University Press & Springer",
doi="10.1631/jzus.B1200098"
}

%0 Journal Article
%T Docetaxel-loaded liposomes: preparation, pH sensitivity, pharmacokinetics, and tissue distribution
%A Hong Zhang
%A Rui-ying Li
%A Xia Lu
%A Zhen-zhen Mou
%A Gui-mei Lin
%J Journal of Zhejiang University SCIENCE B
%V 13
%N 12
%P 981-989
%@ 1673-1581
%D 2012
%I Zhejiang University Press & Springer
%DOI 10.1631/jzus.B1200098

TY - JOUR
T1 - Docetaxel-loaded liposomes: preparation, pH sensitivity, pharmacokinetics, and tissue distribution
A1 - Hong Zhang
A1 - Rui-ying Li
A1 - Xia Lu
A1 - Zhen-zhen Mou
A1 - Gui-mei Lin
J0 - Journal of Zhejiang University Science B
VL - 13
IS - 12
SP - 981
EP - 989
%@ 1673-1581
Y1 - 2012
PB - Zhejiang University Press & Springer
ER -
DOI - 10.1631/jzus.B1200098


Abstract: 
Docetaxel (DTX), as a member of taxoid family, has been widely used in the treatment of cancers. The present study prepared pH-sensitive DTX-loaded liposomes (DTX-Lips) by thin-film dispersion method and various physico-chemical and morphological properties were examined. The pH sensitivity of in vitro DTX release and the in vivo pharmacokinetics and tissue distribution using Kunming mice were also investigated. The mean particle size and zeta potential of DTX liposomes were (277±2) nm and (−32.60±0.26) mV, respectively. Additionally, in vitro drug release study showed that the cumulative release rate was 1.3 times more at pH 5.0 than at pH 7.4, suggesting a pH-dependent release ability of DTX-Lips. Pharmacokinetic and pharmaceutical studies in comparison with Duopafei® showed that the half-time period (t1/2) and area under the curve (AUC) of DTX-Lips in mouse plasma were 1.8 times longer and 2.6 times higher, respectively, and that DTX-Lips selectively accumulated in macrophage-rich organs such as liver and spleen. These results together suggest that the DTX-Lips could be a promising formulation for the clinical administration of DTX.

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