摘要
传统的肿瘤治疗方法依然存在肿瘤组织可及性差和药物不良反应普遍的问题。黄酮类化合物已被证实对多种类型肿瘤有效,但其安全性和作用部位特异性尚未被评估。然而,膳食黄酮类化合物因溶解度小、代谢快、口服吸收差等特点限制了其在体内抗肿瘤活性的发挥。此外,黄酮类化合物在某些情况下还能通过生物转化等作用与药物相互作用而影响生物利用度。纳米载体因可改变药物的药动学和药效学特征而被设计用于靶向药物传递,提高难溶性药物的生物利用度,将大分子传递到细胞内的作用位点,同时还能减少药物不良反应。体内、外研究均表明,纳米类黄酮制剂,特别是槲皮素、柚皮素、芹菜素、儿茶素和非瑟酮等在多种肿瘤的预防和治疗方面具有潜在作用,但其临床应用价值仍有待阐明。本文就纳米类黄酮制剂在提高生物利用度、肿瘤治疗效果和安全性方面的作用展开综述,为肿瘤治疗药物的开发利用提供新思路。
The poor accessibility to tumor tissues and a range of adverse drug reactions are still great concerns for cancer therapies.Flavonoids are documented great potential in combating various types of cancer,while their safety profile and tumor site-specific action have not been evaluated thoroughly.Low solubility,rapid metabolism and poor absorption of dietary flavonoids limit their antitumor activity in vivo.Moreover,flavonoids may interact with other therapeutic agents resulting their bioavailability reduction,especially through biotransformation.Nanocarriers can alter pharmacokinetics and pharmacodynamic profile of incorporating drug.Moreover,nanocarriers are designed for targeted drug delivery,improving the bioavailability of poorly water-soluble drugs,delivery of macromolecules to site of action,and reducing ADRs.It has been shown the potential of flavonoids nano-formulations,especially quercetin,naringenin,apigenin,catechins and fisetin in the prevention and treatment of several types of cancer,both in vitro and in vivo studies.However,few clinical trials have yet to be performed.This review focuses on the impact of flavonoids nano-formulations on the improvement of their bioavailability,therapeutic and safety profile and will open new insights in the field of drug discovery for cancer therapeutics.
作者
高慧
付强
孙洁
左学志
姚颖
Gao Hui;Fu Qiang;Sun Jie;Zuo Xuezhi;Yao Ying(Department of Clinical Nutrition,Tongji Hospital,Tongji Medical College,Huazhong University of Science and Technology,Wuhan 430030,Hubei,China;Department of Oncology,Tongji Hospital,Tongji Medical College,Huazhong University of Science and Technology,Wuhan 430030,Hubei,China)
出处
《肿瘤代谢与营养电子杂志》
2020年第3期362-365,共4页
Electronic Journal of Metabolism and Nutrition of Cancer
基金
国家自然科学基金项目(81703215,81974381)。
关键词
肿瘤
纳米新技术
纳米类黄酮制剂
一级预防
Cancer
Nanometer new technology
Flavonoids nanoparticles
Primary prevention