Solanki Raghu, Jangid Ashok Kumar, Jadav Mahima, Kulhari Hitesh, Patel Sunita
School of Life Sciences, Central University of Gujarat, Gandhinagar, 382030, India.
School of Nano Sciences, Central University of Gujarat, Gandhinagar, 382030, India.
Macromol Biosci. 2023 Sep;23(9):e2300077. doi: 10.1002/mabi.202300077. Epub 2023 May 18.
Evodiamine (Evo) is a natural, biologically active plant alkaloid with wide range of pharmacological activities. In the present study Evo-loaded folate-conjugated Pluronic F108 nano-micelles (ENM) is synthesized to enhance the therapeutic efficacy of Evo against cervical cancer. ENM are synthesized, physicochemically characterized and in vitro anticancer activity is performed. The study demonstrates that ENM have nanoscale size (50.33 ± 3.09 nm), monodispersity of 0.122 ± 0.072, with high drug encapsulation efficiency (71.30 ± 3.76%) and controlled drug release at the tumor microenvironment. ENM showed dose-dependent and time-dependent cytotoxicity against HeLa human cervical cancer cells. The results of in vitro anticancer studies demonstrated that ENM have significant anticancer effects and greatly induce apoptosis as compared to pure Evo. The cellular uptake study suggests that increased anticancer activity of ENM is due to the improved intracellular delivery of Evo through overexpressed folate receptors. Overall, the designed ENM can be a potential targeted delivery system for hydrophobic anticancer bioactive compound like Evo.
吴茱萸碱(Evo)是一种天然的、具有生物活性的植物生物碱,具有广泛的药理活性。在本研究中,合成了负载吴茱萸碱的叶酸共轭普朗尼克F108纳米胶束(ENM),以提高吴茱萸碱对宫颈癌的治疗效果。对ENM进行了合成、理化性质表征,并进行了体外抗癌活性研究。研究表明,ENM具有纳米级尺寸(50.33±3.09nm),单分散性为0.122±0.072,具有较高的药物包封率(71.30±3.76%),并在肿瘤微环境中实现药物控释。ENM对人宫颈癌HeLa细胞显示出剂量依赖性和时间依赖性细胞毒性。体外抗癌研究结果表明,与纯吴茱萸碱相比,ENM具有显著的抗癌作用,并能极大地诱导细胞凋亡。细胞摄取研究表明,ENM抗癌活性的提高是由于通过过表达的叶酸受体改善了吴茱萸碱的细胞内递送。总体而言,所设计的ENM可以成为像吴茱萸碱这样的疏水性抗癌生物活性化合物的潜在靶向递送系统。