Agarwal Srishti, Mohamed M Sheikh, Raveendran Sreejith, Rochani Ankit K, Maekawa Toru, Kumar D Sakthi
Bio Nano Electronics Research Center, Graduate School of Interdisciplinary New Science, Toyo University Kawagoe Saitama 350-8585 Japan
School of Pharmacy and Biomolecular Sciences, University of Brighton Moulsecoomb Brighton BN2 4GJ UK.
RSC Adv. 2018 Sep 21;8(57):32621-32636. doi: 10.1039/c8ra06362a. eCollection 2018 Sep 18.
Morusin, a water-insoluble prenylated flavonoid is known for its numerous medicinal properties. It manifests its anticancer potential by suppression of genes involved in tumor progression. However, poor solubility of the drug results in low bioavailability and rapid degradation thus hindering its clinical utilization. In order to overcome this, we have synthesized a niosome system composed of non-ionic surfactant span 60 and cholesterol using a thin-layer evaporation technique to improve the aqueous-phase solubility of the drug. Highly cytocompatible niosomes of 479 nm average size with smooth and uniform spherical morphology were synthesized in a facile manner. Unlike free morusin, nanomorusin was found to be freely dispersible in aqueous media. Having an extremely high drug entrapment efficiency (97%), controlled and sustained release of morusin resulting in enhanced therapeutic efficacy was observed in cancer cell lines of 4 different lineages. The results demonstrate that the morusin-niosome system is a promising strategy for enhanced anti-cancer activity against multiple cancer types and could be an indispensable tool for future targeted chemotherapeutic strategies.
桑色素是一种水不溶性的异戊烯基黄酮，以其众多药用特性而闻名。它通过抑制参与肿瘤进展的基因来展现其抗癌潜力。然而，该药物的低溶解度导致其生物利用度低且降解迅速，从而阻碍了其临床应用。为了克服这一问题，我们采用薄膜蒸发技术合成了一种由非离子表面活性剂司盘60和胆固醇组成的脂质体系统，以提高药物在水相中的溶解度。以简便的方式合成了平均尺寸为479 nm、具有光滑均匀球形形态且细胞相容性高的脂质体。与游离桑色素不同，纳米桑色素在水性介质中可自由分散。脂质体对桑色素的包封率极高（97%），在4种不同谱系的癌细胞系中观察到桑色素的控释和缓释，从而提高了治疗效果。结果表明，桑色素-脂质体系统是增强对多种癌症类型抗癌活性的一种有前景的策略，并可能成为未来靶向化疗策略中不可或缺的工具。
