In this study, 5-methylmellein (5-MM) loaded bovine serum albumin nanoparticles (BSA NPs) were developed using desolvation technique. The developed nanoparticles were characterized for their mean particle size, polydispersity, zeta potential, loading efficiency, X-ray diffractometry (XRD), differential scanning calorimetry (DSC) and release profile. The developed nanoparticles were spherical in shape under transmission electron microscopy (TEM) and atomic force microscopy (AFM). The developed 5-MM loaded BSA NPs demonstrated a mean particle size with a diameter of 154.95 ± 4.44 nm. The results from XRD and DSC studies demonstrated that the crystal state of the 5-MM was converted to an amorphous state in polymeric matrix. The encapsulation and loading efficiency was found to be 73.26 ± 4.48% and 7.09 ± 0.43%. The in vitro cytotoxicity in human prostate cancer cell line (PC-3), human colon cancer cells (HCT-116) and human breast adenocarcinoma cell line (MCF-7) cells demonstrated enhanced cytotoxicity of 5-MM BSA NPs as compared to native 5-MM after 72-h treatment. The enhancement in cytotoxicity of 5-MM BSA NPs was also supported by increase in cellular apoptosis, mitochondrial membrane potential loss and generation of high reactive oxygen species (ROS). In conclusion, these findings collectively indicated that BSA nanoparticles may serve as promising drug delivery system for improving the efficacy of 5-methylmellein.

在这项研究中，使用去溶剂化技术开发了加载有5-甲基水elle素（5-MM）的牛血清白蛋白纳米粒子（BSA NPs）。所开发的纳米颗粒的特征在于其平均粒径，多分散性，ζ电势，负载效率，X射线衍射法（XRD），差示扫描量热法（DSC）和释放曲线。在透射电子显微镜（TEM）和原子力显微镜（AFM）的作用下，已开发的纳米颗粒呈球形。已开发的5毫米负载BSA NP的平均粒径为154.95±4.44 nm。XRD和DSC研究的结果表明，在聚合物基质中5-MM的晶体状态已转换为非晶态。发现封装和装载效率为73.26±4.48％和7.09±0.43％。在体外在人前列腺癌细胞系（ PC-3），人结肠癌细胞（HCT-116）和人乳腺癌细胞系（MCF-7）中的细胞毒性显示，与天然5-MM相比，5-MM BSA NP的细胞毒性增强经过72小时的治疗。5-MM BSA NPs的细胞毒性增强还受到细胞凋亡，线粒体膜电位损失和高活性氧（ROS）生成增加的支持。总之，这些发现共同表明，BSA纳米颗粒可作为改善5-甲基水elle素功效的有前途的药物递送系统。