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Design and development of a soluble PDA-Emodin-PVP-MN patch and its anti-obesity effect in rats

  • Haijiao Wang,
  • Lifang Wang,
  • Meng Wang,
  • Jingjing Niu,
  • Bowen Yang,
  • Yinxiong Wang,
  • Min An,
  • Xiuxia Sun,
  • Zhigang Yang,
  • Xuefeng Li,
  • Yanbin Shi

摘要

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.

Graphical Abstract

Schematic illustration of preparation, synergistic anti-obesity effect, safety and mechanism of action of PDA-Emodin-PVP-MN patches