Enhanced anticancer activity in vitro and in vivo of luteolin incorporated into long-circulating micelles based on DSPE-PEG2000 and TPGS

Abstract

Objectives: This study aimed to evaluate enhanced anticancer activity in vitro and in vivo of luteolin-loaded long-circulating micelles (DTLLMs) formulated.

Methods: DTLLM was the luteolin formulation prepared with 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-methoxy-poly (ethylene glycol 2000) (DSPE-PEG2000 ) and d-α-tocopheryl polyethylene glycol succinate (TPGS) in this study. We performed a systematic comparative evaluation of the antiproliferative effect, cellular uptake, antitumour efficacy and in vivo tumour targeting of these micelles using non-small cell lung cancer (NSCLC) A549 cells.

Key findings: Results showed that the obtained micelles have a mean particle size of around 42.34 nm, and the size of micelles was narrowly distributed. With the improved cellular uptake, DTLLM displayed a more potent antiproliferative action on A549 cell lines than luteolin; half-maximal inhibitory concentration (IC50 ) was 7.29 vs 19.14 μg/ml, respectively. The antitumour efficacy test in nude mice showed that DTLLM exhibited significantly higher antitumour activity against NSCLC with lesser toxic effects on normal tissues. The imaging study for in vivo targeting demonstrated that the long-circulating micelles formulation achieved targeted drug delivery and make drug release slow to prolong the circulating time.

Conclusion: DTLLM might be a potential antitumour formulation.

Keywords: DSPE-PEG2000; TPGS; antitumour; long-circulating micelles; luteolin.