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@article{Ye:2015:10.2147/IJN.S83508,
author = {Ye, YJ and Wang, Y and Lou, KY and Chen, YZ and Chen, R and Gao, F},
doi = {10.2147/IJN.S83508},
journal = {International Journal of Nanomedicine},
pages = {4309--4319},
title = {The preparation, characterization, and pharmacokinetic studies of chitosan nanoparticles loaded with paclitaxel/dimethyl-β-cyclodextrin inclusion complexes.},
url = {http://dx.doi.org/10.2147/IJN.S83508},
volume = {10},
year = {2015}
}

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TY  - JOUR
AB  - A novel biocompatible and biodegradable drug-delivery nanoparticle (NP) has been developed to minimize the severe side effects of the poorly water-soluble anticancer drug paclitaxel (PTX) for clinical use. PTX was loaded into the hydrophobic cavity of a hydrophilic cyclodextrin derivative, heptakis (2,6-di-O-methyl)-β-cyclodextrin (DM-β-CD), using an aqueous solution-stirring method followed by lyophilization. The resulting PTX/DM-β-CD inclusion complex dramatically enhanced the solubility of PTX in water and was directly incorporated into chitosan (CS) to form NPs (with a size of 323.9-407.8 nm in diameter) using an ionic gelation method. The formed NPs had a zeta potential of +15.9-23.3 mV and showed high colloidal stability. With the same weight ratio of PTX to CS of 0.7, the loading efficiency of the PTX/DM-β-CD inclusion complex-loaded CS NPs was 30.3-fold higher than that of the PTX-loaded CS NPs. Moreover, it is notable that PTX was released from the DM-β-CD/CS NPs in a sustained-release manner. The pharmacokinetic studies revealed that, compared with reference formulation (Taxol(®)), the PTX/DM-β-CD inclusion complex-loaded CS NPs exhibited a significant increase in AUC0→24h (the area under the plasma drug concentration-time curve over the period of 24 hours) and mean residence time by 2.7-fold and 1.4-fold, respectively. Therefore, the novel drug/DM-β-CD inclusion complex-loaded CS NPs have promising applications for the significantly improved delivery and controlled release of the poorly water-soluble drug PTX or its derivatives, thus possibly leading to enhanced therapeutic efficacy and less severe side effects.
AU  - Ye,YJ
AU  - Wang,Y
AU  - Lou,KY
AU  - Chen,YZ
AU  - Chen,R
AU  - Gao,F
DO  - 10.2147/IJN.S83508
EP  - 4319
PY  - 2015///
SN  - 1178-2013
SP  - 4309
TI  - The preparation, characterization, and pharmacokinetic studies of chitosan nanoparticles loaded with paclitaxel/dimethyl-β-cyclodextrin inclusion complexes.
T2  - International Journal of Nanomedicine
UR  - http://dx.doi.org/10.2147/IJN.S83508
UR  - http://hdl.handle.net/10044/1/25099
VL  - 10
ER  -

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