Abstract
INTRODUCTION: This study aims to develop a novel co-delivery gefitinib and quercetin system loaded with PLGA-PEG nanoparticles and evaluate their antitumor activity in vitro and in vivo. METHODS: Gef/Qur NPs were prepared and characterized. The release of drugs, stability, cellular uptake and cytotoxicity were evaluated in vitro. The antitumor effects and systemic toxicity of different formulations were also investigated. RESULTS: Gef/Qur NPs displayed a smaller particle size and a PDI and zeta potential of 0.11 and -23.5 mV, respectively. The hydrophobic Gef and Qur content in NPs reached up to 65.2% and 56.4%, respectively, and their high entrapment efficiencies recorded 83.7% and 82.3%, respectively. The in vitro release of Gef/Qur from the NPs was sustained for 12 h. Compared with control groups, Gef/Qur NPs showed higher cellular uptake and cell inhibition rates. In vivo studies identified the lungs as the target tissue and the region of maximum drug release. Through pharmacodynamics analysis, we found that two drugs (Gef and Qur) were incorporated into one nanoparticle carrier, which played a good role in generating synergistic effect. DISCUSSION: It is concluded that PLGA-PEG is an ideal drug carrier for the co-delivery of Gef/Qur to treat lung cancer.