Biodistribution and biological evaluation of paclitaxel polymer micelles

Abstract

Abstract:

AIM: The biodistribution in tumor-bearing mice and biosafety of paclitaxel (PTX) polymer micelles were investigated. METHODS: The pharmacokinetic study, tissue distribution and antineoplastic effect of PTX polymer micelles and Taxol were evaluated on S180 tumor-bearing mice after intravenous injection. Animals were used to research the acute toxicity, hemolysis and venous irritation of PTX polymer micelle. RESULTS:The t1/2 and MRT of PTX polymer micelles were 3.52 and 4.55 times of Taxol, respectively. Tissue distribution studies showed that the relative uptake rate of PTX polymer micelles at tumor sites was 2.31. The results indicated that PTX polymer micelles improved the circulation time and tumor targeting. The antitumor efficacy of PTX polymer micelles was significantly higher than Taxol. Maximum tolerated dose and LD50 of PTX polymer micelles were significantly improved. PTX polymer micelles had no obvious vascular irritation to ear vein of rabbits. CONCLUSION: The circulation time, tumor targeting, antineoplastic effect and biosafety of PTX polymer micelles were improved, which might turn into a promising tumor targeting paclitaxel polymer micelle preparations in clinic with maximum effect and minmum toxicity.

Key words: paclitaxel, polymer micelles, biodistribution, antitumor efficacy, safety study

CLC Number:

R965.2

YAO Tianyi, YIN Shaoping, LIU Wen, ZHAO Yanlei, WANG Guangji, LI Juan. Biodistribution and biological evaluation of paclitaxel polymer micelles[J]. Chinese Journal of Clinical Pharmacology and Therapeutics, 2017, 22(11): 1207-1214.

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