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A novel Ph-sensitive liposome to trigger delivery of afatinib to cancer cells: Impact on lung cancer therapy

Almurshedi, AS, Radwan, M, Omar, S, Alaiya, AA, Badran, MM, Elsaghire, H, Saleem, IY and Hutcheon, GA (2018) A novel Ph-sensitive liposome to trigger delivery of afatinib to cancer cells: Impact on lung cancer therapy. Journal of Molecular Liquids, 259. pp. 154-166. ISSN 0167-7322

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A novel drug delivery system based on cationic (CL) and pH-sensitive liposomes (PSL) for tyrosine kinase inhibitor afatinib (AFT) were developed to enhance tumor-targetability against NSCLC cells and therapeutic effect. Optimal lipid to drug ratio was selected to prepare AFT-loaded PSL and CL with desirable physiochemical properties based on particle size, drug encapsulation efficiency (EE%), stability and release profiles. Moreover, antitumor activity was performed in vitro on human lung cancer cells (H-1975) using a WST-1 assay and Annexin-V apoptosis assay. The mean particle size of the liposomes was less than 100 nm, and EE% was more than 50% with lipid to drug ratio of 1:0.5. Stability data showed that PSL and CL were physically stable for 1 months at 4 and 25oC. In vitro drug release study demonstrated the sustained release of AFT at pH 7.5; while PSL exhibited fast drug release in pH 5.5. This effect revealed that PSL showed pH-sensitive release behaviors. In addition, the in vitro cytotoxicity study was employed for AFT-loaded PSL due to optimal characterizations. Thus, in vitro anticancer activity revealed that AFT loaded-PSL triggered apoptosis in H-1975 cells. In addition, the inhibitory effect towards H-1975 and HCC-827 was observed, indicating, which indicated high antitumor activity of AFT-loaded PSL. Then, PSL might potentially create practical clinical strategies for better targetability and delivery of AFT for treatment of lung cancer.

Item Type: Article
Subjects: Q Science > QD Chemistry
R Medicine > RC Internal medicine > RC0254 Neoplasms. Tumors. Oncology (including Cancer)
Divisions: Pharmacy & Biomolecular Sciences
Publisher: Elsevier
Date Deposited: 19 Mar 2018 12:16
Last Modified: 04 Sep 2021 10:37
DOI or ID number: 10.1016/j.molliq.2018.03.024
URI: https://researchonline.ljmu.ac.uk/id/eprint/8334
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