Nanomodified strategies to overcome EGFR-tyrosine kinase inhibitors resistance in non-small cell lung cancer

• Published in: Journal of controlled release Vol. 324; pp. 482 - 492
• Main Authors: Liao, Zi-Xian, Huang, Kuo-Yen, Kempson, Ivan M., Li, Hsin-Jung, Tseng, S.-Ja, Yang, Pan-Chyr
• Format: Journal Article
• Language: English
• Published: Netherlands Elsevier B.V 10.08.2020
• Subjects: EGFR-TKIs resistance; Epidermal growth factor receptor; Nanotechnology; Non-small cell lung cancer; Tyrosine kinase inhibitor; EGFR-TKIs resistance; Tyrosine kinase inhibitor; Epidermal growth factor receptor; Nanotechnology; Non-small cell lung cancer
• ISSN: 0168-3659; 1873-4995
• DOI: 10.1016/j.jconrel.2020.05.043

Lung cancer is the primary cause of cancer-related death worldwide. 85%–90% of cases are non-small cell lung cancer (NSCLC) which characteristically exhibits altered epidermal growth factor receptor (EGFR) signaling is a major driver pathway. Unfortunately, therapeutic outcomes in treating NSCLC are compromised by the emergence of drug resistance in response to EGFR-tyrosine kinase inhibitor (TKI) targeted therapy due to the acquired resistance mutation EGFR T790M or activation of alternative pathways. There is current need for a new generation of TKIs to be developed to treat EGFR-TKI-resistant NSCLC. To overcome the above problems and improve clinical efficacy, nanotechnology with targeting abilities and sustained release has been proposed for EGFR-TKI-resistant NSCLC treatment and has already achieved success in in vitro or in vivo models. In this review, we summarize and illustrate representative nano-formulations targeting EGFR-TKI-resistant NSCLC. The described advances may pave the way to better understanding and design of nanocarriers and multifunctional nanosystems for efficient treatment for drug resistant NSCLC. [Display omitted] •NSCLC patients with EGFR mutation inevitably develop acquired TKIs resistance within one year of treatment.•Advances in nano science have led to development of targeting delivery systems in tumor microenvironment.•These nano-modified therapies show improved in vivo penetration and retention of therapeutic drugs.•A decrease in the side-effect and off targeting through systemic circulation has confirmed.•These nano-modified therapies can provide synergistic anticancer effects and overcome drug resistance in NSCLC.