可溶性 PDA-Emodin-PVP-MN 贴片的设计与开发及其对大鼠的抗肥胖作用

IF 5.7 3区 医学 Q1 MEDICINE, RESEARCH & EXPERIMENTAL Drug Delivery and Translational Research Pub Date : 2025-02-01 Epub Date: 2024-05-22 DOI:10.1007/s13346-024-01623-9
Haijiao Wang, Lifang Wang, Meng Wang, Jingjing Niu, Bowen Yang, Yinxiong Wang, Min An, Xiuxia Sun, Zhigang Yang, Xuefeng Li, Yanbin Shi
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引用次数: 0

摘要

大黄素已被证实具有减轻体重和降低血脂的作用。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大黄素负载型溶解微针贴片,其中大黄素以大黄素-聚乙烯吡咯烷酮共沉淀物(Emodin-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),用于肥胖症的光热增强化疗。贴片的平均重量为 0.1 ± 0.05 克,载药量为 0.37 ± 0.031 毫克。经过5分钟的近红外照射(808 nm,0.6 W/cm2),大鼠腹部温度达到48 ℃,大黄素的累积释放率达到96.25%。大黄素在体外琼脂扩散实验中的扩散系数为 249.27 mm2 h-1。溶血试验、CCK-8 检测和显微组织病理学分析均未发现明显毒性。大黄素贴片明显降低了大黄素对小鼠体重的影响(P
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Design and development of a soluble PDA-Emodin-PVP-MN patch and its anti-obesity effect in rats.

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.

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来源期刊
Drug Delivery and Translational Research
Drug Delivery and Translational Research MEDICINE, RESEARCH & EXPERIMENTALPHARMACOL-PHARMACOLOGY & PHARMACY
CiteScore
11.70
自引率
1.90%
发文量
160
期刊介绍: The journal provides a unique forum for scientific publication of high-quality research that is exclusively focused on translational aspects of drug delivery. Rationally developed, effective delivery systems can potentially affect clinical outcome in different disease conditions. Research focused on the following areas of translational drug delivery research will be considered for publication in the journal. Designing and developing novel drug delivery systems, with a focus on their application to disease conditions; Preclinical and clinical data related to drug delivery systems; Drug distribution, pharmacokinetics, clearance, with drug delivery systems as compared to traditional dosing to demonstrate beneficial outcomes Short-term and long-term biocompatibility of drug delivery systems, host response; Biomaterials with growth factors for stem-cell differentiation in regenerative medicine and tissue engineering; Image-guided drug therapy, Nanomedicine; Devices for drug delivery and drug/device combination products. In addition to original full-length papers, communications, and reviews, the journal includes editorials, reports of future meetings, research highlights, and announcements pertaining to the activities of the Controlled Release Society.
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