A novel ligand-modified nanocomposite microparticles improved efficiency of quercetin and paclitaxel delivery in the non-small cell lung cancer

Drug Deliv. 2022 Dec;29(1):3123-3133. doi: 10.1080/10717544.2022.2120567.

Abstract

Chemotherapy is the first choice for the treatment of cancer but it is still limited by insufficient kill efficiency and drug resistance. These problems urgently need to be overcome in a way that minimizes damage to the body. In this study, we designed the nanocomposite microparticles (NMPs) modified by cetuximab (Cet) and loaded anti-tumor agents- quercetin (QUE) and paclitaxel (PTX)- for eliciting specific drugs homing and enhancing the killing efficiency of chemotherapy drugs (P/Q@CNMPs). Physicochemical characteristics results presented that P/Q@CNMPs have a suitable aerodynamic diameter and uniform morphology that could meet the requirements of particles deposition in the lung. And it also had the characteristics of sustained-release and pH-responsive which could release the agents in the right place and has a continuous effect. In vitro and in vivo analysis results presented that P/Q@CNMPs have the accuracy targeting ability and killing effect on non-small cell lung cancer (NSCLC) which express positive epidermal growth factor receptor (EGFR) on the membrane. Furthermore, this system also has low toxicity and good biocompatibility. These results demonstrated that P/Q@CNMPs could be a potential intelligent targeting strategy used for chemo-resistant NSCLC therapies.

Keywords: NSCLC; active targeting; anti-tumor; nanocomposite microspheres; orthotopic.

MeSH terms

  • Antineoplastic Agents* / pharmacology
  • Antineoplastic Agents* / therapeutic use
  • Carcinoma, Non-Small-Cell Lung* / drug therapy
  • Carcinoma, Non-Small-Cell Lung* / metabolism
  • Cell Line, Tumor
  • Cetuximab / pharmacology
  • Delayed-Action Preparations / therapeutic use
  • ErbB Receptors / metabolism
  • Humans
  • Ligands
  • Lung Neoplasms* / drug therapy
  • Lung Neoplasms* / metabolism
  • Nanocomposites*
  • Paclitaxel
  • Quercetin / pharmacology
  • Quercetin / therapeutic use

Substances

  • Antineoplastic Agents
  • Delayed-Action Preparations
  • Ligands
  • Quercetin
  • ErbB Receptors
  • Paclitaxel
  • Cetuximab

Grants and funding

This work was supported by a grant from the National Natural Science Foundation of China (81973671); The demonstration guide special project of benefitting people by science and technology in Qingdao (20-3-4-52-inch); The science and technology development project in medical and health of Shandong Province (202013020643); The technology project of the West Coast New Area of Qingdao in 2020 (2020-45).