Nanostructured lipid carriers as novel carrier for parenteral delivery of docetaxel

The aim of this study was to design docetaxel-loaded nanostructured lipid carriers (DTX-NLC) to reduce toxicity and improve therapeutic efficacy. Docetaxel-loaded nanostructured lipid carriers (DTX-NLC) were prepared by the modified film ultrasonication–dispersion method. The DTX-NLC were characterized by particle size distribution, zeta potential and entrapment efficiency. In vitro cytotoxicity of DTX-NLC was evaluated by MTT assay against three human cancer cell lines and one murine malignant melanoma (B16). AnnexinV-FITC kit was used to measure the percentage of apoptosis induced by Duopafei® or DTX-NLC. In vivo anti-tumor efficacy was evaluated in Kunming mice bearing murine malignant melanoma (B16). Compared with Duopafei®, DTX-NLC revealed more cytotoxicity against A549 cells by inducing more apoptosis and more G2/M arrest. The inhibition rates of Duopafei®, DTX-NLC (10 mg/kg) and DTX-NLC (20 mg/kg) were 42.74%, 62.69% and 90.36%, respectively, indicating that DTX-NLC could more effectively inhibit tumor growth. The results of the body weight variations of mice also showed that compared with Duopafei®, DTX-NLC had lower toxicity during the therapeutic procedure. These results suggest that DTX-NLC may be a promising drug delivery system for cancer therapy. To our knowledge, this was the first report about DTX-NLC for murine malignant melanoma treatment.

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► DTX-NLC were designed to reduce toxicity and improve therapeutic efficacy.
► DTX-NLC revealed more cytotoxicity against tumor cells in vitro.
► DTX-NLC induced more apoptosis and more G2/M arrest in vitro.
► Compared with Duopafei®, DTX-NLC showed stronger antitumor effect and lower toxicity.