2. Academic Validation
  3. An Osimertinib-Perfluorocarbon Nanoemulsion with Excellent Targeted Therapeutic Efficacy in Non-small Cell Lung Cancer: Achieving Intratracheal and Intravenous Administration

An Osimertinib-Perfluorocarbon Nanoemulsion with Excellent Targeted Therapeutic Efficacy in Non-small Cell Lung Cancer: Achieving Intratracheal and Intravenous Administration

  • ACS Nano. 2022 Jul 21. doi: 10.1021/acsnano.2c04159.
Jie Yang 1 2,  Yingbo Li 1 2,  Jiemei Sun 1 2,  Hongyan Zou 1 2,  Yige Sun 1 2,  Jing Luo 1 2,  Qian Xie 1 2,  Rong A 1 2,  Hongbin Wang 1 2,  Xiaona Li 1 2,  Kai Wang 1 2,  Lili Yang 1 2,  Teng Ma 3,  Lina Wu 1 2,  Xilin Sun 1 2
Affiliations

Affiliations

  • 1 NHC and CAMS Key Laboratory of Molecular Probe and Targeted Theranostics, Molecular Imaging Research Center (MIRC), Harbin Medical University, 150028 Harbin, Heilongjiang, China.
  • 2 Department of Nuclear Medicine, the Fourth Hospital of Harbin Medical University, 150028 Harbin, Heilongjiang, China.
  • 3 Shenzhen Key Laboratory of Ultrasound Imaging and Therapy, Shenzhen Institutes of Advanced Technology, Chinese Academy of Sciences, 518055 Shenzhen, Guangdong, China.
PMID: 35863049 DOI: 10.1021/acsnano.2c04159
Abstract

Low accumulation of Anticancer drugs in tumors and serious systemic toxicity remain the main challenges to the clinical efficiency of pharmaceuticals. Pulmonary delivery of nanoscale-based drug delivery systems offered a strategy to increase antitumor activity with minimal adverse exposure. Herein, we report an osimertinib-loaded perfluoro-15-crown-5-ether (AZD9291-PFCE) nanoemulsion, through intratracheal and intravenous delivery, synergizes with 19F magnetic resonance imaging (19F MRI)-guided low-intensity focused ultrasound (LIFU) for lung Cancer therapy. Pulmonary delivery of AZD9291-PFCE nanoemulsion in orthotopic lung carcinoma models achieves quick distribution of the nanoemulsion in lung tissues and tumors without short-term and long-term toxic effects. Furthermore, LIFU can trigger drug release from the AZD9291-PFCE nanoemulsion and specifically increases tumor vascular and tumor tissue permeability. 19F MRI was applied to quantify nanoemulsion accumulation in tumors in real time after LIFU irradiation. We validate the treatment effect of AZD9291-PFCE nanoemulsion in resected human lung Cancer tissues, proving the translational potential to enhance clinical outcomes of lung Cancer therapy. Thus, this work presents a promising pulmonary nanoemulsion delivery system of osimertinib (AZD9291) for targeted therapy of lung Cancer without severe side effects.

Keywords

drug delivery system; low-intensity focused ultrasound; perfluorocarbon; pulmonary delivery; third-generation EGFR-TKI; tumor penetration.

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  • HY-15772
    99.96%, Mutant-Selective EGFR Inhibitor