Sequentially dual-targeting vector with nano-in-micro structure for improved docetaxel oral delivery in vivo.

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.