Abstract
PURPOSE: The aim of this study was to prepare RGD-modified nanoliposomes containing quercetin (QCT) distearoyl-L-a-phosphatidylethanolamine-polyethylene glycol 2000-RGD-liposomes ([DSPE]-PEG2000-RGD-LPs/QCT) for lung cancer targeting treatment. METHODS: The physicochemical parameters of (DSPE)-PEG2000-RGD-LPs/QCT were characterized in terms of the particle size, zeta potential, morphology, entrapment efficiency, drug loading, and in vitro release behavior. In vivo, pharmacokinetics and antitumor studies of prepared formulations were also evaluated. RESULTS: In this study, QCT was found to be easily dispersed in lipid solution and entrapped by the thin-film hydration method. The encapsulation ratio and drug loading of prepared LPs were 89.2%±7.4% and 9.2%±1.3% and the mean diameter was 93.4±7.2 nm from 3 batches. The results of in vitro experiments showed that the particle size of liposomes was suitable for the fenestrated vasculatures of cancer tissues via the enhanced permeability retention effect. In vitro, a relatively slow QCT release profile was observed in (DSPE)-PEG2000-RGD-LPs, and the release mechanism fit with the Higuchi equation better. In vivo imaging results indicated that RGD-modified LPs had very good tumor targeting ability. (DSPE)-PEG2000-RGD-LPs/QCT showed a significant antitumor activity in mice with A549 tumors. CONCLUSION: Through this study, it was found that the RGD-modified LPs loaded with QCT could potentially be a very promising lung-targeted preparation.