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目的以pH敏感聚乙二醇单甲醚-聚乳酸-聚组氨酸(poly(ethylene glycol)-poly(D,L-lactide)-poly(L-histidine),m PEG-PLA-PHis)两亲性嵌段共聚物为载体制备白藜芦醇载药胶束,并进行大鼠体内药动学研究。方法采用薄膜分散法制备白藜芦醇载药胶束,分别采用动态光散射法、透射电子显微镜法和差示扫描量热法对载药胶束进行表征,以白藜芦醇溶液为对照,测定p H敏感载药胶束在大鼠体内药动学。结果白藜芦醇p H敏感胶束的载药量为10.25%,包封率为90.69%,平均粒径为54.1 nm,zeta电位为-12.7 m V。透射电子显微镜照片显示载药胶束呈类球形,分布均匀。白藜芦醇在胶束内核以分子或无定型形式存在。大鼠药动学结果显示,与白藜芦醇溶液相比,白藜芦醇载药胶束组的血药质量浓度-时间曲线下面积显著提高(P<0.05),清除率显著下降(P<0.05),平均滞留时间显著增加(P<0.05)。结论白藜芦醇胶束具有较小的粒径且分布较窄,包封率较高,具有较好的长循环效果。
OBJECTIVE To study the effects of pH-sensitive poly (ethylene glycol) -poly (D, L- latidde) -poly (L-histidine), m PEG-PLA-PHis The amphiphilic block copolymer was used as a carrier to prepare resveratrol drug-loaded micelles, and pharmacokinetic studies in rats were performed. Methods The resveratrol-loaded micelles were prepared by thin-film dispersion method. The drug-loaded micelles were characterized by dynamic light scattering, transmission electron microscopy and differential scanning calorimetry, resveratrol solution was used as control, Determination of p H-sensitive drug-loaded micelles in rats pharmacokinetics. Results Resveratrol p H-sensitive micelles had a drug loading of 10.25%, encapsulation efficiency of 90.69%, average particle diameter of 54.1 nm and zeta potential of -12.7 mV. Transmission electron microscopy photographs showed that the drug-loaded micelles were spherical and evenly distributed. Resveratrol exists in molecular or amorphous form in the micellar core. Pharmacokinetic results of rats showed that compared with resveratrol solution, the area under the plasma concentration-time curve of resveratrol-loaded micelles group was significantly increased (P <0.05), and the clearance rate was significantly decreased (P <0.05), mean residence time increased significantly (P <0.05). Conclusion Resveratrol micelles have smaller particle size, narrower distribution, higher entrapment efficiency and better long-term circulation.