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Published on: November 1, 2017
Sequentially dual-targeting vector with nano-in-micro structure for improved docetaxel oral delivery in vivo
Yurun Shen1, Mengying Hu2, Liyan Qiu1
1Ministry of Educational (MOE) Key Laboratory of Macromolecular Synthesis & Functionalization, Department of Polymer Science & Engineering, Zhejiang University, Hangzhou 310027, China.
Aim:
In this study, we constructed a novel vector (BioPf-M-loaded Alg-microparticles [Alg-BioPf-M]) with nano-in-micro structure to improve the oral absorption of docetaxel (DTX) by sequentially dual-targeting functions toward intestine and sodium-dependent multivitamin transporter based on entrapping biotin-modified micelles into alginate microparticles.
Methods:
A series of characteristics of this system was investigated, such as drug release, cellular uptake, transport pathway and the comprehensive in vivo studies including pharmacokinetic studies, anti-tumor activity and toxicity study.
Results:
The bioavailability of DTX-loaded Alg-BioPf-M was 27.4-fold higher than that of free DTX after oral administration and achieved superior tumor inhibition of 84.6% against sarcoma 180 tumors.
Conclusion:
These results demonstrated that the Alg-BioPf-M was a promising vector for oral delivery of DTX.
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