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.
Highlights
As the most successful chemotherapeutic drugs currently available, Taxanes play an important role in the treatment of various solid tumors [1]
There was no significant difference in particle size of these three types of micelles
The DTX-loaded Polysorbate 80/Phospholipid mixed micelles were dispersed in pure water and the morphology was investigated by transmission electron microscope (TEM)
Summary
As the most successful chemotherapeutic drugs currently available, Taxanes play an important role in the treatment of various solid tumors [1]. DTX and 1040-mg Tween® 80 (Polysorbate 80) per mL This concentrated solution has to be carefully diluted with solvent containing 13% ethanol in saline before administration, and has to be used within 4 h for its limited stability. Various drug delivery systems have been reported recently, such as DTX loaded nanoparticles [4], liposomes [5], N-palmitoyl chitosan anchored DTX liposomes [6], self-emulsified DTX [7], PEGylated liposomes [8], PEGylated immunoliposomes [9], and PEG-liposomes-folic acid bioconjugates [10] They have their advantages, respectively, each of the above is hampered by one or more problems, such as complicated preparation process, high cost, and low stability of the formulation. There is an urgent need for a pharmaceutical composition comprising DTX, which should have high solubility and stability, simplified preparation process, and the same pharmacokinetics as Taxotere®
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