Open AccessPharmacokinetics and biodistribution of polymeric micelles of paclitaxel with Pluronic P123 1
Author(s) -
HAN Limei,
GUO Jie,
ZHANG Lijun,
WANG Qingsong,
FANG Xiaoling
Publication year - 2006
Publication title -
acta pharmacologica sinica
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.514
H-Index - 90
eISSN - 1745-7254
pISSN - 1671-4083
DOI - 10.1111/j.1745-7254.2006.00340.x
Subject(s) - biodistribution , micelle , pharmacokinetics , poloxamer , bioavailability , paclitaxel , chemistry , in vivo , pharmacology , chromatography , materials science , in vitro , medicine , biochemistry , copolymer , organic chemistry , aqueous solution , polymer , surgery , chemotherapy , microbiology and biotechnology , biology
Aim: To investigate the preparation, in vitro release, in vivo pharmacokinetics and tissue distribution of a novel polymeric micellar formulation of paclitaxel (PTX) with Pluronic P123. Methods : The polymeric micelles of paclitaxel with Pluronic P123 were prepared by a solid dispersion method. The characteristics of micelles including particle size distribution, morphology and in vitro release of PTX from micelles were carried out. PTX‐loaded micellar solutions were administered through the tail vein to healthy Sprague‐Dawley rats and Kunming strain mice to assess the pharmacokinetics and tissue distribution of PTX, respectively. Taxol, the commercially available intravenous formulation of PTX, was also administered as control. Results : By using a dynamic light scattering sizer and a transmission electron microscopy, it was shown that the PTX‐loaded micelles had a mean size of approximately 25 nm with narrow size distribution and a spherical shape. PTX was continuously released from Pluronic P123 micelles in release medium containing 1 mol/L sodium salicylate for 24 h at 37°C. In the pharmacokinetic assessment, t 1/2β and AUC of micelle formulation were 2.3 and 2.9‐fold higher than that of Taxol injection. And the PTX‐loaded micelles increased the uptake of PTX in the plasma, ovary and uterus, lung, and kidney, but decreased uptake in the liver and brain in the biodistribution study. Conclusion : Polymeric micelles using Pluronic P123 can effectively solubilize PTX, prolong blood circulation time and modify the biodistribution of PTX.