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姜黄素包被酪蛋白纳米粒:提高生物利用度和抗癌疗效。

Curcumin Encapsulated Casein Nanoparticles: Enhanced Bioavailability and Anticancer Efficacy.

机构信息

Chemistry Division, Bhabha Atomic Research Centre, Trombay, Mumbai, 400 085; Homi Bhabha National Institute, Anushaktinagar, Mumbai, 400 094.

Chemistry Division, Bhabha Atomic Research Centre, Trombay, Mumbai, 400 085; Department of Pharmacy, Banasthali Vidyapith, Rajasthan, 304 022.

出版信息

J Pharm Sci. 2021 May;110(5):2114-2120. doi: 10.1016/j.xphs.2020.12.011. Epub 2020 Dec 15.

Abstract

The poor water solubility and bioactivity of drugs can be potentially improved by using suitable nanocarriers. Herein, an economically viable methodology is developed for encapsulation of hydrophobic anticancer agent, curcumin in casein nanoparticles (CasNPs). The successful encapsulation of curcumin was evident from the structural, thermal and spectroscopic analysis of curcumin encapsulated CasNPs (Cur-CasNPs). The CasNPs and Cur-CasNPs samples were lyophilized for their long-term stability and lyophilized powders are found to be stable for more than 6 months at 4-8 °C. From DLS studies, it has been observed that the variation in average size of drug formulations before and after reconstitution were less than 5%. Further, it shows good water-dispersibility, enhanced bioavailability and pH dependent charge conversal feature. Cur-CasNPs showed pH dependent release characteristics with higher at mild acidic environment and enhanced toxicity towards cancer cells (MCF-7) as compared to normal cells (CHO). Moreover, the CasNPs are non-toxic in nature and the developed nanoformulation of drug exhibits substantial cellular internalization and enhanced toxicity towards MCF-7 cells over pure drug, indicating their potential applications.

摘要

通过使用合适的纳米载体,可以有效提高药物的水溶性和生物活性。在此,我们开发了一种经济可行的方法,用于将疏水性抗癌药物姜黄素封装在酪蛋白纳米粒(CasNPs)中。从姜黄素包封的 CasNPs(Cur-CasNPs)的结构、热和光谱分析中可以明显看出姜黄素的成功包封。CasNPs 和 Cur-CasNPs 样品被冻干以实现其长期稳定性,冻干粉末在 4-8°C 下可稳定保存超过 6 个月。从 DLS 研究中可以观察到,药物制剂在重构前后平均粒径的变化小于 5%。此外,它还表现出良好的水分散性、增强的生物利用度和 pH 值依赖性电荷转换特性。Cur-CasNPs 表现出 pH 值依赖性释放特性,在温和的酸性环境下更高,并表现出比正常细胞(CHO)更强的抗癌细胞(MCF-7)毒性。此外,CasNPs 具有非毒性,开发的药物纳米制剂对 MCF-7 细胞的细胞内化和毒性增强作用明显优于纯药物,表明其具有潜在的应用前景。

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