柚皮素β-环糊精包合物的制备及对模型大鼠脉络膜新生血管形成的抑制作用

目的:制备柚皮素β-环糊精(β-CD)包合物,研究其对模型大鼠脉络膜新生血管(CNV)形成的抑制作用。方法:采用饱和溶液法制备柚皮素β-CD包合物;利用红外光谱、X射线衍射法对包合物进行表征分析,测定柚皮素的含量与水溶解度;通过氪激光复制大鼠CNV模型,15只BN大鼠随机均分为溶媒对照(等容溶媒)组、柚皮素(20 mg/kg)组与柚皮素β-CD包合物(97.4 mg/kg)组,腹腔注射给药,每天1次,连续4周。以脉络膜铺片法测量大鼠CNV面积。结果:柚皮素和β-CD形成了稳定的包合物,柚皮素β-CD包合物中柚皮素质量分数为20.53%,柚皮素在水中的溶解度为单体的11.8倍。与溶媒对照组比较,柚皮素组、柚皮素β-CD包合物组大鼠CNV面积减小,差异有统计学意义(P<0.01或P<0.05);与柚皮素组比较,柚皮素β-CD包合物组大鼠CNV面积减小,差异有统计学意义(P<0.05)。结论:柚皮素和β-CD包合后,水溶性增加;柚皮素β-CD包合物抑制模型大鼠CNV形成的作用优于柚皮素。

Preparation of Inclusion Complex of Naringenin andβ-cyclodextrin and Inhibitory Effects of It on Choroidal Neovascularization in Model Rats

OBJECTIVE： To prepare inclusion complex of naringenin and β-cyclodextrin （β-CD）, and to study the inhibitory effects of it on choroidal neovascularization （CNV） in model rats. METHODS： The inclusion complex of naringenin with β-CD was prepared by saturated solution method. The inclusion characterization of naringenin with β-CD was determined by x-ray diffrac- tometry （XRD） and FTIR, the contentand the solubility of naringenin in water was calculated based on standard curve. Rats were anesthetized to receive krypton laser to induce CNV. 15 BN rats were randomly divided into solvent control group （constant volume of solvent）, naringenin group （20 mg/kg） and naringenin β-CDinclusion group（97.4 mg/kg）, and then given relevant medicines in- traperitoneally once a day for consecutive 4 weeks. The area of CNV lesions were measured in choroidal flatmounts by the tech- nique of chorioid sheeting. RESULTS： It had been found that β-CD had strong inclusion capacity with naringenin; the solubility of naringenin in water was 11.8-fold of naringenin monomer. Compared with solvent control group, the area of CNV in naringenin group and β-CD inclusion group were decreased; there was statistical significance （P〈0.01 or P〈0.05）. Compared naringenin group, the area of CNV in naringenin fl-CD inclusion group was decreased; there was statistical significance（P〈0.05）.CONCLU- SIONS： β-cyclodextrin increases the solubility of naringenin in water; naringenin/fl-CD inclusion has stronger inhibition on CNV in model rats than that of naringenin.