Arora Divya, Kumar Amit, Gupta Prasoon, Chashoo Gousia, Jaglan Sundeep
Microbial Biotechnology Division, CSIR-Indian Institute of Integrative Medicine, Jammu 180001, India; Academy of Scientific and Innovative Research (AcSIR), Jammu Campus, Jammu 180001, India.
Instrumentation Division, CSIR-Indian Institute of Integrative Medicine, Jammu 180001, India.
Bioorg Med Chem Lett. 2017 Dec 1;27(23):5126-5130. doi: 10.1016/j.bmcl.2017.10.064.
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.
在本研究中,采用去溶剂化技术制备了负载5-甲基麦角硫因(5-MM)的牛血清白蛋白纳米粒(BSA NPs)。对所制备的纳米粒进行了平均粒径、多分散性、zeta电位、负载效率、X射线衍射(XRD)、差示扫描量热法(DSC)和释放曲线等表征。在透射电子显微镜(TEM)和原子力显微镜(AFM)下,所制备的纳米粒呈球形。所制备的负载5-MM的BSA NPs的平均粒径为154.95±4.44 nm。XRD和DSC研究结果表明,5-MM在聚合物基质中的晶态转变为非晶态。包封率和负载率分别为73.26±4.48%和7.09±0.43%。在人前列腺癌细胞系(PC-3)、人结肠癌细胞(HCT-116)和人乳腺腺癌细胞系(MCF-7)中的体外细胞毒性研究表明,与天然5-MM相比,5-MM BSA NPs在72小时处理后具有增强的细胞毒性。5-MM BSA NPs细胞毒性的增强还得到细胞凋亡增加、线粒体膜电位丧失和高活性氧(ROS)生成的支持。总之,这些发现共同表明,BSA纳米粒可能是一种有前景的药物递送系统,可提高5-甲基麦角硫因的疗效。