Xu Dongling, Xie Jiming, Feng Xiaolian, Zhang Xiaofang, Ren Zhenzhen, Zheng Yunquan, Yang Jianming
College of Chemistry, Fuzhou University 2 Xueyuan Road Fuzhou Fujian 350116 China
Fujian Key Laboratory of Medical Instrument and Pharmaceutical Technology, Fuzhou University 2 Xueyuan Road Fuzhou 350116 China
RSC Adv. 2020 Mar 11;10(17):10352-10360. doi: 10.1039/c9ra10390b. eCollection 2020 Mar 6.
Rubropunctatin is a naturally occurring constituent of polyketide compounds that has great potential in the development of cancer-assisted chemotherapy. However, it has certain shortcomings such as water insolubility and photo instability that limit its clinical application. In this study, we constructed a Rubropunctatin-loaded liposome (R-Liposome) anticancer drug carrier for the first time. The results indicate that R-Liposome is water soluble, has spherical morphology, great homogeneity and dispersibility with high encapsulation efficiency (EE%, 90 ± 3.5%) and loading rate (LR%, 5.60 ± 2.5%) values. Moreover, the carrier improves the photostability, storage and pH stabilities of Rubropunctatin. The R-Liposome also prolongs the release of Rubropunctatin, enhances the anticancer activity of Rubropunctatin and encourages the mechanism of Rubropunctatin to promote apoptosis. Therefore, liposomal nanoparticles have great potential as drug delivery vehicles of Rubropunctatin for cancer treatment.
玉红点菌素是聚酮化合物的一种天然成分,在癌症辅助化疗的发展中具有巨大潜力。然而,它存在一些缺点,如水不溶性和光不稳定,这限制了其临床应用。在本研究中,我们首次构建了负载玉红点菌素的脂质体(R-脂质体)抗癌药物载体。结果表明,R-脂质体具有水溶性,呈球形形态,具有良好的均一性和分散性,包封率(EE%,90±3.5%)和载药量(LR%,5.60±2.5%)较高。此外,该载体提高了玉红点菌素的光稳定性、储存稳定性和pH稳定性。R-脂质体还延长了玉红点菌素的释放,增强了玉红点菌素的抗癌活性,并促进了玉红点菌素促进细胞凋亡的机制。因此,脂质体纳米颗粒作为玉红点菌素的药物递送载体在癌症治疗中具有巨大潜力。