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KMID : 0043320120350020333
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Archives of Pharmacal Research
2012 Volume.35 No. 2 p.333 ~ p.341
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Anti-glioma effect and safety of docetaxel-loaded nanoemulsion
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Gaoe Huil
Pang Zhiqing
Pan Shuaiqi
Cao Shijie
Yang Zhi
Chen Chen
Jiang Xinguo
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Abstract
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Docetaxel, an inhibitor of microtubule depolymerization, has been used for many malignancies. Due to its toxicity and the non-selective distribution of its commercial formulation, Taxotere®, new formulations with less toxicity and tumor targeting need to be explored. For its safety and ease of factory scale production, nanoemulsion, was selected to encapsulate docetaxel. The particle size of docetaxel loaded nanoemulsion (DNE) was 72.3 nm, the average zeta potential was ?6.38 mV, the encapsulation efficiency was 93.1% and the drug loading capacity was 2.87%. Although DNE presented similar antiproliferation effects on both U87 cells and bEnd.3 cells, its in vivo toxicity was significantly lower than Taxotere®. In vivo fluorescent imaging suggested nanoemulsions loaded with a fluorescent probe could distribute to the brain and accumulate at the glioma site. The pharmacological experiments also confirmed that the DNE could target glioma sites and prolong the median survival time of mice with gliomas. In conclusion, DNE is a new, less toxic, drug formulation that is effective for brain glioma therapy.
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KEYWORD
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Docetaxel, Nanoemulsion, Glioma, Toxicity
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