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Development and characterization of Brigatinib loaded solid lipid nanoparticles: In-vitro cytotoxicity against human carcinoma A549 lung cell lines
Chemistry and Physics of Lipids ( IF 3.4 ) Pub Date : 2020-10-20 , DOI: 10.1016/j.chemphyslip.2020.105003
Mohammed Muqtader Ahmed 1 , Farhat Fatima 1 , Md Khalid Anwer 1 , Mohammed F Aldawsari 1 , Yasser Saud M Alsaidan 1 , Suliman Abdulaziz Alfaiz 1 , Anzarul Haque 2 , Alanazi Az 3 , Khalid Alhazzani 3
Affiliation  

Brigatinib (BG) is a tyrosine kinase receptor inhibitor act as an antineoplastic agent by blocking the action of an abnormal protein that causes cancer cells to multiply. In the current study, nine formulae of BG loaded solid lipid nanoparticles (SLNs) were developed using 32 factorial design. SLNs were prepared by the solvent emulsification technique using stearic acid as lipid and soya- lecithin as a surfactant, both of these act as independent variables, whereas Particle size, polydispersity index (PDI), zeta potential, entrapment efficiency (EE) and drug loading (DL) were selected as responses. The particle size was found to be in the nano range (176−787 nm), fairly monodisperse (PDI indices 0.19−0.5), interparticle electrical stability was supported by zeta-potential (+1.78 mV to -15.4 mV), whereas EE and DL were in the range of (61.31–87.87 %) (3.35–31.01 %), respectively. Differential scanning calorimetry (DSC) thermograms indicated the amorphous state of BG in the SLN. Fourier transform infrared spectroscopy (FTIR) spectrums confirm non-interaction between drug and polymer while nuclear magnetic resonance (NMR) spectroscopy study revealed BG incorporation in the SLN. A scanning electron microscope (SEM) image exhibit a spherical shape of SLN. The in-vitro release profile demonstrates a sustained release pattern for the selected BS5 SLNs. MTT assay was performed on the optimized SLNs (BS5) and the results are indicative that BG loaded SLN (BS5) showed better cytotoxicity against A349 lung cell lines while compared to BG suspension and blank SLN. Thus, BG loaded SLNs can find Its better place in the non-small cell lung cancer treatment.



中文翻译:

载有 Brigatinib 的固体脂质纳米粒的开发和表征:对人癌 A549 肺细胞系的体外细胞毒性

Brigatinib (BG) 是一种酪氨酸激酶受体抑制剂,通过阻断导致癌细胞繁殖的异常蛋白质的作用,起到抗肿瘤剂的作用。在目前的研究中,使用 3 2因子设计。SLNs 是通过溶剂乳化技术制备的,使用硬脂酸作为脂质和大豆卵磷脂作为表面活性剂,这两者都作为自变量,而粒径、多分散指数 (PDI)、zeta 电位、包封率 (EE) 和载药量(DL) 被选为答复。发现粒径在纳米范围内(176-787 nm),相当单分散(PDI 指数 0.19-0.5),zeta 电位(+1.78 mV 至 -15.4 mV)支持颗粒间电稳定性,而 EE 和DL 分别在 (61.31–87.87 %) (3.35–31.01 %) 的范围内。差示扫描量热法 (DSC) 热谱图表明 SLN 中 BG 的无定形状态。傅里叶变换红外光谱 (FTIR) 光谱证实药物和聚合物之间不相互作用,而核磁共振 (NMR) 光谱研究显示 BG 掺入 SLN。扫描电子显微镜 (SEM) 图像显示 SLN 呈球形。体外释放曲线显示了所选 BS5 SLN 的持续释放模式。对优化的 SLN (BS5) 进行 MTT 测定,结果表明,与 BG 悬浮液和空白 SLN 相比,加载 BG 的 SLN (BS5) 对 A349 肺细胞系显示出更好的细胞毒性。因此,加载BG的前哨淋巴结可以在非小细胞肺癌治疗中找到更好的位置。体外释放曲线显示了所选 BS5 SLN 的持续释放模式。对优化的 SLN (BS5) 进行 MTT 测定,结果表明,与 BG 悬浮液和空白 SLN 相比,加载 BG 的 SLN (BS5) 对 A349 肺细胞系显示出更好的细胞毒性。因此,加载BG的前哨淋巴结可以在非小细胞肺癌治疗中找到更好的位置。体外释放曲线显示了所选 BS5 SLN 的持续释放模式。对优化的 SLN (BS5) 进行 MTT 测定,结果表明,与 BG 悬浮液和空白 SLN 相比,加载 BG 的 SLN (BS5) 对 A349 肺细胞系显示出更好的细胞毒性。因此,加载BG的前哨淋巴结可以在非小细胞肺癌治疗中找到更好的位置。

更新日期:2020-10-30
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