水溶性芦丁/羟丙基-β-环糊精包合物的制备及其抗氧化活性、稳定性研究

Preparation of Water-soluble Rutin/Hydroxypropyl-β-Cyclodextrin Inclusion Complex and Its Antioxidant Activity and Stability Studies

芦丁具有多种药理活性,为解决其水溶性差导致的应用缺陷。本文通过溶剂蒸发法制备了芦丁/羟丙基-β-环糊精(Hydroxypropyl-beta-cyclodextrin,HPCD)包合物,分析了包合物的结构、溶解性、抗氧化活性和稳定性。结果表明,HPCD能够有效包埋芦丁,包合物中二者摩尔比为1:1,其包封率和载药率分别为89.33%、26.67%,包合物在水中的溶解度是游离芦丁的51倍。芦丁被包合后,其晶体衍射峰完全消失,提高了最大失重速率温度(266℃到318℃),且固态包合物呈现出不规则的片状结构,表明HPCD成功包合了芦丁。包合物清除DPPH和ABTS^(+)自由基的IC_(50)显著低于芦丁(P<0.05),并且其铁离子还原能力是芦丁的1.2倍。稳定性实验表明,自然光处理6 d后游离芦丁和包合芦丁保留率分别为31.80%、66.70%,50℃热处理15 d后保留率分别为66.91%、87.38%。因此HPCD不仅提高了芦丁的水溶性,也提升了其抗氧化活性和稳定性,使芦丁可在不同环境中发挥其保健功能。

Rutin has a variety of pharmacological activities,in order to solve the application defects caused by its poor water solubility.In this paper,rutin/hydroxypropyl-β-cyclodextrin(HPCD)inclusion complexes were prepared by solvent evaporation method and analysed for structure,solubility,antioxidant activity and stability.The analysis of the inclusion complex showed that HPCD could effectively encapsulate rutin in a molar ratio of 1:1,and its encapsulation efficiency and drug loading rate were 89.33%and 26.67%,respectively.The solubility of the inclusion complex in water was 51 times higher than that of rutin.After complexation,the crystal diffraction peaks of rutin disappeared and the temperature of the maximum weight loss increased from 266℃to 318℃and solid inclusion complex forms showed an irregular sheet-like structures indicating a successful complexation of rutin by HPCD.The IC_(50) of the inclusion complex for scavenging DPPH radicals and ABTS cationic radicals was significantly lower than that of rutin(P<0.05),and its ferric ion reduction capacity was 1.2 times that of rutin.The stability study also showed a higher retention rate of rutin in the inclusion complex after exposure to natural light for 6 days(31.80%,66.70%)or heat treatment at 50℃for 15 days(66.91%,87.38%).The complexation of rutin by HPCD significantly improved its solubility,antioxidant activity and stability,which could be used in different environments to exert its health functions.