Abstract：
Emodin has been proven to have weight-reducing and lipid-lowering effects. In order to make emodin play a better anti-obesity role, we designed and developed an emodin loaded dissolving microneedle patch, in which emodin existed in the form of emodin-polyvinylpyrrolidone co-precipitate (Emodin-PVP). Meanwhile, polydopamine (PDA) was added to the microneedle patch (PDA-Emodin-PVP-MN) for photothermal-enhanced chemotherapy of obesity. The average weight of the patch was 0.1 ± 0.05 g and the drug loading was 0.37 ± 0.031 mg. After 5 min of NIR irradiation (808 nm, 0.6 W/cm2), the rat abdominal temperature could reach 48 ℃, and the cumulative release of emodin reached 96.25%. The diffusion coefficient of emodin in the in vitro agar diffusion experiment was 249.27 mm2 h-1. No obvious toxicity was observed in hemolysis test, CCK-8 assay and microscopic histopathological analysis. The patch significantly reduced the percent of body weight ( P < 0.01), lipid-body ratio ( P < 0.001), serum FFAs ( P < 0.01) and the cell volume of peritesticular adipose tissue in the high-fat diet induced obese rats, indicating the patch had good anti-obesity effect. The mechanism of action may be related to the up-regulation of HSL and LPL protein levels in rat peritesticular adipose tissue.
摘要：
大黄素已被证明具有减肥和降脂作用。为了使大黄素更好地发挥抗肥胖作用,我们设计并开发了一种载有大黄素的溶解微针贴片，其中大黄素以大黄素-聚乙烯吡咯烷酮共沉淀(大黄素-PVP)的形式存在。同时,在微针贴片(PDA-Emodin-PVP-MN)中加入聚多巴胺(PDA),用于肥胖的光热增强化疗.贴剂的平均重量为0.1±0.05g，载药量为0.37±0.031mg。NIR照射5分钟后（808nm，0.6W/cm2),大鼠腹部温度可达48℃,大黄素的累积释放量达到96.25%。大黄素在体外琼脂扩散实验中的扩散系数为249.27mm2h-1。溶血试验未见明显毒性,CCK-8测定和显微组织病理学分析。贴剂显著降低了体重百分比(P<0.01),脂体比（P<0.001），高脂饮食诱导的肥胖大鼠血清FFAs(P<0.01)和睾丸周围脂肪细胞体积,表明该贴剂具有良好的抗肥胖作用。其作用机制可能与大鼠睾丸周围脂肪组织中HSL和LPL蛋白水平的上调有关。
