Folate-PEG-decorated docetaxel lipid nanoemulsion for improved antitumor activity

Abstract

Aim: To develop a folate-based docetaxel lipid nanoemulsion (FLNE) for tumor-targeted treatment.

Materials & methods: The docetaxel LNEs were prepared and characterized. In vitro cytotoxic and cell uptake studies were performed. The tissue distribution and targeting of drug were studied by fluorescence imaging and tumor regression in mice.

Results: The IC50 values of FLNE on cancer cells were significant. The cell uptake studies showed an increase in fluorescence with time. Imaging studies found that FLNE was superior in tumor targeting by 4.81- and 2.08-fold over controls. The tumor regression proved the superiority of FLNEs.

Conclusion: The folate strategy was superior over PEGylation, albumin and transferrin strategies. The study demonstrated great potential of FLNE as a prospective targeted delivery system.

Keywords: fluorescent LNE cell uptake; fluorescent tissue distribution; folate-containing emulsion; improved targeting; noninvasive imaging study; targeted docetaxel lipid emulsion.