科研之友
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摘要
The vitamin E analogue, alpha-tocopherol succinate (alpha-TOS), has a broad anti-tumor effect. alpha-TOS can induce cancer cells apoptosis and suppress tumor growth by targeting mitochondria. Low bioavailability of alpha-TOS is the major problem encountered with formulation development. In our study, alpha-TOS nanoemulsion (alpha-TOS-NE) was demonstrated as a new drug delivery system of alpha-TOS to increase the bioavailability. MTT-based cytotoxicity assay and mitochondrial membrane potential (DY) were performed on human breast cancer cell lines MCF-7 and human oral epithelial cancer cell lines KB to evaluate in vitro anticancer efficacy of alpha-TOS-NE. In comparison with free alpha-TOS, alpha-TOS-NE exhibited a stronger cytotoxicity and decreased Delta Psi. Pharmacokinetic profiles of I.V. alpha-TOS-NE group, I.P. alpha-TOS-NE group, and I.P. free alpha-TOS group (7% DMSO/93% PEG) were drawn. First of all, nanoemultion (NE) enables the I.V. injection of alpha-TOS, make it possible to be an I.V. preparation. Second, compare to the I.P. free alpha-TOS group, I.P. alpha-TOS-NE group had a higher bioavailability. Thus, NE improved the strong anti-cancer efficacy of alpha-TOS while increasing its in vivo bioavailability in rats. In conclusion, our laboratory-made NE was a safe drug delivery system for clinical trials and could be a promising formulation for alpha-TOS by I.V administration.
- 出版日期2016-12-30
- 单位哈尔滨医科大学
