影响姜黄素口服吸收的因素及药物递送策略  

Overview of Factors Affecting Oral Absorption of Curcumin and Its Drug Delivery Strategies

作　　者：邢艾雅 高迪 陈跃杰 XING Aiya;GAO Di;CHEN Yuejie(College of Pharmacy,Minzu University of China,Beijing 100081,China)

机构地区：[1]中央民族大学药学院,北京100081

出　　处：《医药导报》2024年第5期762-768,共7页Herald of Medicine

基　　金：国家自然科学基金青年项目(82204321);中央民族大学青年教师科研能力提升计划(2022QNPY85)。

摘　　要：姜黄素是一类存在于姜黄根茎中的脂溶性多酚类化合物,具有抗氧化、抗炎、抗纤维化、抗肿瘤、抗菌、抗病毒等多种药理作用。由于姜黄素的水溶性低、化学稳定性差和首关效应强等因素导致口服吸收效果差,阻碍了其临床应用。增加姜黄素的口服生物利用度的策略包括加入代谢酶抑制剂或P-糖蛋白(P-gp)抑制剂,或者采用纳米药物递送系统。该文综述影响姜黄素口服吸收的关键因素及相关药物递送策略,建议对姜黄素纳米制剂的设计和工业化进行更深入研究;选择兼具P-gp和CYP酶抑制活性的药用辅料递送药物;对于药物浓度需求较高的治疗,靶向递送或皮肤局部给药使药物精确作用于病变部位可能更合理;基于药动学和药效学方面的协同作用进行药物联用。Curcumin is a lipophilic polyphenol compound in the rhizome of Curcuma longa.It possesses various pharmacological effects,including anti-oxidant,anti-inflammatory,anti-fibrosis,anti-tumor,anti-bacteria,anti-virus,and other activities.However,curcumin's poor solubility,instability,and extensive first pass effect result in poor oral absorption,which limits its applications in clinical therapy.Strategies to improve curcumin's bioavailability include adding metabolism or P-gp inhibitors or encapsulating curcumin in nano drug delivery systems.Based on the overview of various factors affecting oral absorption of curcumin,as well as the related drug delivery strategies for curcumin,some suggestions for further research in this field were presented below:as for the design and industrialization of curcumin nano-pharmaceutics,in-depth analysis still need to be carried out;select pharmaceutical excipients with P-gp and CYP enzymes inhibitory activities for drug delivery;for the medication with high concentration demand,targeted drug-delivery or dermal topical administration is more reasonable as drug could act directly on the lesion site;use drug combinations with synergistic therapeutic actions based on the synergism of pharmacokinetics and pharmacodyna-mics.

关 键 词：姜黄素 生物利用度 药物递送 纳米制剂 药物联用 

分 类 号：R282.71[医药卫生—中药学] R285[医药卫生—中医学]