The teniposide cationic nanoemulsions (TCN) were prepared by a self-assembly technique with D-α-tocopherol polyethylene glycol 1000 succinate (TPGS), 12-hydroxystearic acid-polyethylene glycol copolymer (HS-15), octadecylamine and medium chain triglyceride. The product was nanometer-sized with the mean diameter of (61.9±4.5)nm and the ζ potential of (+8.38±3.34)mV. The MTT assay showed that the in vitro antitumor activity of teniposide in A549 cells was significantly increased by TCN. The distributions of teniposide from TCN in the intestinal tract and tissues such as heart, liver, spleen, lung and kidney of mice were obviously enhanced compared with teniposide solution. Moreover, the results of in vivo pharmacokinetic test in rats indicated that the cmax and AUC of teniposide from TCN were significantly enhanced. Compared with teniposide solution, the oral bioavailability of TCN was 380％.
Key words
teniposide /
self-assembly /
cationic nanoemulsion /
oral absorption
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Footnotes
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