In vitro and in vivo antitumor properties of 7-epidocetaxel, a major impurity of docetaxel
Purpose: To investigate the antitumor properties and toxicity of 7-epi docetaxel (7-epi DTX) as an active pharmaceutical ingredient, and in formulations.
Methods: Docetaxel-loaded albumin nanoparticles (DTX NPs) were prepared by freeze-drying, while 7- epi DTX was detected and isolated by high performance liquid chromatography (HPLC). Their antitumor properties were evaluated in vitro in CT26 cells and in vivo in BALB/c sk-ov-3 xenograft nude mice model. The tissues were histological examined.
Results: The in vivo antitumor effects of DTX NPs at different doses of 7-epi DTX were similar. Moreover, the in vitro anti-cancer effect of 7-epi DTX was comparable to that of DTX. However, the in vivo antitumor effectiveness of 7-epi DTX was inferior to that of DTX. In toxicity studies, 7-epi DTX did not elicit any acute toxic effects both as active pharmaceutical ingredients, and as a component of formulations.
Conclusion: The results indicate that 7-epi DTX does not elicit acute toxic effects both as an active pharmaceutical ingredient and in bulk formulations. The antitumor property of 7-epi DTX is less than that of DTX.
Keywords: 7-Epidocetaxel, Impurity, Antitumor properties, Toxicity