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载抗癌药物纳米粒子协同治疗肺癌细胞。

Co-Delivery Anticancer Drug Nanoparticles for Synergistic Therapy Against Lung Cancer Cells.

机构信息

Department of Thoracic Surgery, Shanghai Chest Hospital, Shanghai Jiao Tong University, Shanghai 200030, People's Republic of China.

出版信息

Drug Des Devel Ther. 2020 Oct 23;14:4503-4510. doi: 10.2147/DDDT.S275123. eCollection 2020.

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.

摘要

简介

本研究旨在开发一种新型共递送吉非替尼和槲皮素系统,该系统负载于 PLGA-PEG 纳米粒中,并评估其在体外和体内的抗肿瘤活性。

方法

制备并表征了 Gef/Qur NPs。评估了药物的释放、稳定性、细胞摄取和细胞毒性。还研究了不同制剂的抗肿瘤作用和全身毒性。

结果

Gef/Qur NPs 显示出较小的粒径和 PDI 以及 -23.5 mV 的 ζ 电位,分别为 0.11 和 -23.5 mV。NPs 中吉非替尼和槲皮素的疏水性含量分别高达 65.2%和 56.4%,包封率分别高达 83.7%和 82.3%。Gef/Qur 从 NPs 中的体外释放持续了 12 小时。与对照组相比,Gef/Qur NPs 表现出更高的细胞摄取率和细胞抑制率。体内研究确定了肺部是靶组织和药物释放的最大区域。通过药效学分析,我们发现两种药物(吉非替尼和槲皮素)被整合到一个纳米载体中,这对产生协同作用起到了很好的作用。

讨论

PLGA-PEG 是共递送吉非替尼和槲皮素治疗肺癌的理想药物载体。

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