Assistant Professor, University of Macau, Institute of Chinese Medical Sciences, State Key Laboratory of Quality Research in Chinese Medicine , Av. Padre Tomas Pereira S.J, Taipa, Macau, 999078 , China
Expert Opin Drug Deliv. 2013 Oct;10(10):1411-28. doi: 10.1517/17425247.2013.807795. Epub 2013 Jul 18.
Long-term epidemiological studies have demonstrated that regular ingestion of flavonoids contained in dietary sources is associated with a reduced risk for many chronic diseases including cancer. However, although flavonoids are largely consumed in the diet and high concentrations may exist in the intestine after oral administration, the plasma/tissue concentrations of flavonoids are lower than their effective therapeutic doses due to poor bioavailability, resulting in the limited efficacy of flavonoids in various clinical studies. Therefore, the application of nanotechnology to deliver flavonoids to tumor sites has received considerable attention in recent years.
In this review, after a general review of the potential benefits of flavonoids in cancer therapy and several key factors affecting their bioavailability, the current efforts in improving the delivery efficacy of promising candidates that are particularly important in the human diet, namely quercetin, epigallocatechin-3-gallate (EGCG) and genistein were focused on. Finally, the challenges of developing flavonoid delivery systems that improve flavonoid bioavailability and their anticancer therapy potentials were summarized.
The design of suitable molecular carriers for flavonoids is an area of research that is in rapid progress. A large number of unheeded promising favonoids are suffering from poor in vivo parameters, their potential benefits deserves further research. Furthermore, more effort should be placed on developing active targeting systems, evaluating the efficacy and toxicity of novel flavonoid delivery systems through small and large scale clinical trials.
长期的流行病学研究表明,经常摄入饮食来源中的类黄酮与许多慢性疾病(包括癌症)的风险降低有关。然而,尽管类黄酮在饮食中大量摄入,并且口服后肠道内可能存在高浓度的类黄酮,但由于生物利用度差,类黄酮在血浆/组织中的浓度低于其有效治疗剂量,导致类黄酮在各种临床研究中的疗效有限。因此,近年来,将纳米技术应用于将类黄酮递送至肿瘤部位受到了相当多的关注。
在这篇综述中,在一般性地回顾了类黄酮在癌症治疗中的潜在益处以及影响其生物利用度的几个关键因素之后,重点关注了目前在提高几种有望成为人类饮食中特别重要的候选药物(即槲皮素、表没食子儿茶素-3-没食子酸酯(EGCG)和染料木黄酮)的递送效果方面的努力。最后,总结了开发能够提高类黄酮生物利用度和抗癌治疗潜力的类黄酮递送系统所面临的挑战。
类黄酮的合适分子载体的设计是一个研究进展迅速的领域。大量被忽视的有前途的黄酮类化合物由于体内参数不佳而受到影响,它们的潜在益处值得进一步研究。此外,应更多地致力于开发主动靶向系统,通过小型和大型临床试验评估新型类黄酮递送系统的疗效和毒性。