| It is well known that resveratrol is a kind of phytoalexin which has the properties of antioxidant and the function of lowering the prevanlence of coronary heart disease. In the present researches, it is reported that resveratrol is a new promosing anticancer drug with the cancer chemopreventive activity that represent in three major stages of carcinogenesis such as anti-initiation, anti-promotion and anti-progression activities. The application of resveratrol is limited and bioavailability of resveratrol is lower due to its poor solubility and unstability under intensive UV light. So it is important to enhance the resveratrol of solubility in water and stability to wide its applitication.Cyclodextrins (CDs) are a kind of larger-ring compounds shaped like truncated cone. Their unique structure of interior hydrophobic cavity can include guestes that local in its special cavity or between its self-aggregation. They have exterior hydrophilic surface and thus water solubility of the poorly soluble guests by inclused can be promoted.α-cyclode- xtrin (α-CD) andβ-cyclodextrin (β-CD) are wide used for enhancing the solubility. Beca- use of low solubility,β-CD is often improved by introducing modified groups into edges to extend its application. One of its derivatives often used as solubility increaser is hydroxyl- propyl-β-cyclodextrin (HP-β-CD), which has features of low toxicity and good water sol- ubility.In this paper, the complexation of poorly water-soluble resveratrol with HP-β- CD were investigated.(1) The inclusion complexes were prepared by freeze-drying method. The optimum preparation condition was studied by orthogonal test with encapsulation rate as the index of evaluation: the ratio of Resveratro to HP-β-CD 1 : 2, inclusion temperature 30℃, inclu- sion time 60 minutes. It had been preliminarily proved that the inclusion complexes of Resveratrol-hydroxypropyl-β-cyclodextrin were formed.The rate of inclusion satisfied us.(2) The inclusion complexes of Resveratrol-hydroxypropyl-β-cyclodextrin were character- rized by differential scanning calorimetry, IR and UV absorption spectrum. It was confir- med that the inclusion complexes of Resveratrol- hydroxypropyl -β- cyclode- xtrin were formed.(3) The hydroxypropyl-β-cyclodextrin is very stable in the alkalinity medium, but can be decomposed by the strong acid, therefore used the hydrochloric acid to damage on inclusion complexes from a pilot conducted, so that resveratrol released from the inclusion complexes; Resveratrol content was determined by high performance liquid chromato- graphy ,the result indicated that, the inclusion complex carried on with 0.1 mol/L hydr- ochloric acid escapes a package of effect to be good.(4) Used the solubility law to study the hydroxypropyl-β-cyclodextrin on the inclusion of resveratrol and to increase dissolves the function. The results indicated: When does not contain t cyclodextrin, the solubility of resveratrol is 0.0169 mg/mL. Along with cyclode- xtrin increased, the solubility increased gradually.When the hydroxypropyl-β-cyclodextrin concentration is 15.83 mg/mL, the solubility of resveratrol is 467.46 times to the original freedom. On the one hand the solubility of resveratrol increased can be further verified with hydrox- ypropyl-β-cyclodextrin inclusion complex formation, on the other hand illu- strated the hydroxypropyl-β-cyclodextrin has solubilization to resveratrol.(5) By comparing the inclusion compound resveratrol and resveratrol in the UV irrad- iation changes in the trend can be seen, hydroxypropyl-β-cyclodextrin of resveratrol can not only improve the water-soluble, but also increase its purple outside the stability. |
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