Development and characterization of ethyl cellulose nanosponges for sustained release of brigatinib for the treatment of non-small cell lung cancer

Abstract

Abstract Non-small cell lung cancer (NSCLC) contributes to about 85% of lung cancer. By 2040, lung cancer cases estimated to rise to 3.6 million globally. Brigatinib (BG) acts as tyrosine kinase inhibitors that target the epidermal growth factor receptor of the epithelial lung cancer cells. BG loaded nanosponges (NSs) were prepared by the emulsion solvent evaporation technique using ethylcellulose (EC) and polyvinyl alcohol (PVA) as a stabilizer. Eight formulations were developed by varying the concentration of the drug (BG), EC and PVA followed by optimization through particle characterization; size, polydispersity index (PDI), zeta potential (ZP), drug entrapment and loading efficiency. The optimized formulation BGNS5 showed particles size (261.0 ± 3.5 nm), PDI (0.301) and ZP(−19.83 ± 0.06 Mv) together with entrapment efficiency (85.69 ± 0.04%) and drug loading (17.69 ± 0.01%). FTIR, DSC, XRD, and SEM showed drug-polymer compatibility, entrapment of drug in EC core, non-crystallinity of BG in NS and confirm spherical porous nature of the NS. BGNS5 reflects drug release in a sustained manner, 86.91 ± 2.12% for about 12 h. BGNS5 significantly decreased the cell viability of A549 human lung cancer cell lines with less hemolytic ratio compared to pure drug BG and EC. Based on the aforementioned results BGNS5 could be used in the effective treatment of NSCLC.