title: Development of Polysorbate 80/Phospholipid mixed micellar formation for docetaxel and assessment of its in vivo distribution in animal models.
abstract: Docetaxel (DTX) is a very important member of taxoid family. Despite several alternative delivery systems reported recently, DTX formulated by Polysorbate 80 and alcohol (Taxotere®) is still the most frequent administration in clinical practice. In this study, we incorporated DTX into Polysorbate 80/Phospholipid mixed micelles and compared its structural characteristics, pharmacokinetics, biodistribution, and blood compatibility with its conventional counterparts. Results showed that the mixed micelles loaded DTX possessed a mean size of approximately 13 nm with narrow size distribution and a rod-like micelle shape. In the pharmacokinetics assessment, there was no significant difference between the two preparations (P > 0.05), which demonstrated that the DTX in the two preparations may share a similar pharmacokinetic process. However, the Polysorbate 80/Phospholipid mixed micelles can increase the drug residence amount of DTX in kidney, spleen, ovary and uterus, heart, and liver. The blood compatibility assessment study revealed that the mixed micelles were safe for intravenous injection. In conclusion, Polysorbate 80/Phospholipid mixed micelle is safe, can improve the tumor therapeutic effects of DTX in the chosen organs, and may be a potential alternative dosage form for clinical intravenous administration of DTX.
authors.affiliation: National Key Laboratory of Nano/Micro Fabrication Technology, Key Laboratory for Thin Film and Microfabrication of Ministry of Education, Department of Bio-Nano Science and Engineering, Institute of Micro-Nano Science and Technology, Shanghai Jiao Tong University, 800 Dongchuan Road, Shanghai 200240, People's Republic of China. dxcui@sjtu.edu.cn.
authors.forename: Hua
authors.initials: H
authors.lastname: Song
authors.forename: Hongquan
authors.initials: H
authors.lastname: Geng
authors.forename: Jing
authors.initials: J
authors.lastname: Ruan
authors.forename: Kan
authors.initials: K
authors.lastname: Wang
authors.forename: Chenchen
authors.initials: C
authors.lastname: Bao
authors.forename: Juan
authors.initials: J
authors.lastname: Wang
authors.forename: Xia
authors.initials: X
authors.lastname: Peng
authors.forename: Xueqing
authors.initials: X
authors.lastname: Zhang
authors.forename: Daxiang
authors.initials: D
authors.lastname: Cui