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Int J Pharm. 2016 Dec 30;515(1-2):506-514. doi: 10.1016/j.ijpharm.2016.10.026. Epub 2016 Oct 13.

Nanoemulsion enhances α-tocopherol succinate bioavailability in rats.

Author information

1
Department of Pharmaceutics, School of Pharmacy, Harbin Medical University, Harbin, 150086, PR China.
2
Department of Pharmacy, The Second Affiliated Hospital, Harbin Medical University, Harbin, 150086, PR China.
3
Department of Pharmaceutics, School of Pharmacy, Harbin Medical University, Harbin, 150086, PR China; Department of Pharmacy, The Second Affiliated Hospital, Harbin Medical University, Harbin, 150086, PR China.
4
Department of Pharmaceutics, School of Pharmacy, Harbin Medical University, Harbin, 150086, PR China. Electronic address: tangjl430@hotmail.com.

Abstract

The vitamin E analogue, α-tocopherol succinate (α-TOS), has a broad anti-tumor effect. α-TOS can induce cancer cells apoptosis and suppress tumor growth by targeting mitochondria. Low bioavailability of α-TOS is the major problem encountered with formulation development. In our study, α-TOS nanoemulsion (α-TOS-NE) was demonstrated as a new drug delivery system of α-TOS to increase the bioavailability. MTT-based cytotoxicity assay and mitochondrial membrane potential (ΔY) 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 α-TOS-NE. In comparison with free α-TOS, α-TOS-NE exhibited a stronger cytotoxicity and decreased ΔΨ. Pharmacokinetic profiles of I.V. α-TOS-NE group, I.P. α-TOS-NE group, and I.P. free α-TOS group (7% DMSO/93% PEG) were drawn. First of all, nanoemultion (NE) enables the I.V. injection of α-TOS, make it possible to be an I.V. preparation. Second, compare to the I.P. free α-TOS group, I.P. α-TOS-NE group had a higher bioavailability. Thus, NE improved the strong anti-cancer efficacy of α-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 α-TOS by I.V administration.

KEYWORDS:

Bioavailability; Cancer; Mitochondria; Nanoemulsion; α-tocopherol succinate

PMID:
27746330
DOI:
10.1016/j.ijpharm.2016.10.026
[Indexed for MEDLINE]

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