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.

中文翻译：

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用于缓释布加替尼治疗非小细胞肺癌的乙基纤维素纳米海绵的开发和表征

摘要 非小细胞肺癌 (NSCLC) 约占肺癌的 85%。到 2040 年，全球肺癌病例估计将增至 360 万。Brigatinib (BG) 作为酪氨酸激酶抑制剂，靶向上皮肺癌细胞的表皮生长因子受体。使用乙基纤维素 (EC) 和聚乙烯醇 (PVA) 作为稳定剂，通过乳液溶剂蒸发技术制备了负载 BG 的纳米海绵 (NSs)。通过改变药物 (BG)、EC 和 PVA 的浓度，然后通过颗粒表征进行优化，开发了八种配方；大小、多分散指数 (PDI)、zeta 电位 (ZP)、药物包封和装载效率。优化的配方 BGNS5 显示出粒径 (261.0 ± 3.5 nm)、PDI (0.301) 和 ZP(-19.83 ± 0.06 Mv) 以及截留效率 (85.69 ± 0)。04%) 和载药量 (17.69 ± 0.01%)。FTIR、DSC、XRD 和 SEM 显示药物-聚合物相容性、药物在 EC 核心中的包埋、NS 中 BG 的非结晶性，并证实了 NS 的球形多孔性质。BGNS5 以持续的方式反映药物释放，约 12 小时为 86.91 ± 2.12%。与纯药物 BG 和 EC 相比，BGNS5 显着降低 A549 人肺癌细胞系的细胞活力，溶血率较低。基于上述结果，BGNS5可用于NSCLC的有效治疗。与纯药物 BG 和 EC 相比，BGNS5 显着降低 A549 人肺癌细胞系的细胞活力，溶血率较低。基于上述结果，BGNS5可用于NSCLC的有效治疗。与纯药物 BG 和 EC 相比，BGNS5 显着降低 A549 人肺癌细胞系的细胞活力，溶血率较低。基于上述结果，BGNS5可用于NSCLC的有效治疗。