Development of docetaxel liposome surface modified with CD133 aptamers for lung cancer targeting.

The aim of the present study was to prepare a novel CD133 aptamer modified DTX liposome system and investigate its characteristics in vitro and in vivo studies. In this study, the CD133-DTX LP was prepared by the thin-film hydration method and with the particle size of 100-120 nm. The TEM photomicrographs were smooth, sub-spherical in shape and aggregated to form small clusters. In vitro, a relatively slower DTX release profile was observed in CD133-DTX LP due to the presence of CD133 aptamers on the outer surface which might hinder the drug release. The drug release mechanism fit well with the Higuchi equation better. In cytotoxicity study, CD133 aptamers modified DTX LP significantly decreased cell proliferation and improved the therapeutic efficiency. In vivo imaging result indicated that CD133-DTX LP had very good tumour targeting ability. In vivo antitumour activity indicated that the CD133-DTX LP showed a significant antitumour activity in A549 tumour mice, with a very low systemic toxicity.