Faculty of Pharmacy, Jouf University, Saudi Arabia-Lecturer of Clinical Pharmacology, Faculty of Medicine, Beni-Suef University, Beni-Suef, Egypt.
Pre-Treatment and Finishing of Cellulosic Fabric Department, Textile Research Division, National Research Center, 33 El- Behooth St, Dokki, Giza, 12311, Egypt.
Invest New Drugs. 2020 Oct;38(5):1303-1315. doi: 10.1007/s10637-020-00905-6. Epub 2020 Feb 11.
Diabetes with poor glycemic control is accompanying with an increased risk of disease namely atherosclerotic cardiovascular. Diosmin (DSN), which is obtained from citrus fruit used to assist the treatment of hemorrhoids or chronic venous atherosclerosis diseases, has an antioxidant, anti-hyperglycemic and anti-inflammatory effect. DSN is characterized by poor water solubility which limits its absorption by the gastrointestinal tract. To overcome this limitation, this study was designed to increase DSN bioavailability and solubility, through its loading on polymeric matrix; hydroxypropyl starch (HPS) and Poly lactide-glycolide-chitin (PLGA/chitin) to prepare Diosmin nanoparticles (DSN-NPs). Two methods were used to prepare DSN- NPs; Emulsion-solvent evaporation and Acid-base neutralization followed by further assessment on diabetes induced atherosclerosis The study was conducted on 50 animals assigned into 5 groups with 10 animals in each group: Group I: Normal rats received only normal saline, Group II: Diabetic rats, Group III: diabetic rats received oral DSN, Group IV: diabetic rats received DSN loaded HPS, Group V: diabetic rats received DSN loaded PLGA/chitin. Levels of total cholesterol, triglycerides, HDL-cholesterol, insulin, MDA and NO. plasminogen activator inhibitor-1 PAI-1), Paraoxonase-1(PON1), transforming growth factor-β1 (TGF-β1), NF-ҡB and Ang II were estimated. Our study revealed that, there was statistically significant difference between DSN treated group compared with DSN loaded HPS treated group and DSN loaded PLGA/chitin. Furthermore, the results obtained clearly disclosed no statistically significant difference between DSN loaded PLGA/chitin and control group exhibited DSN loaded PLGA/chitin has the higher ability to counteract the atherosclerosis factors induced by diabetes in all rats.
糖尿病伴血糖控制不佳会增加疾病风险,即动脉粥样硬化性心血管疾病。地奥司明(DSN)从柑橘类水果中提取,用于辅助治疗痔疮或慢性静脉动脉粥样硬化疾病,具有抗氧化、降血糖和抗炎作用。DSN 的特点是水溶性差,限制了其在胃肠道的吸收。为了克服这一限制,本研究旨在通过将 DSN 负载到聚合物基质上来提高 DSN 的生物利用度和溶解度;羟丙基淀粉(HPS)和聚乳酸-乙醇酸-壳聚糖(PLGA/壳聚糖)制备地奥司明纳米粒(DSN-NPs)。采用两种方法制备 DSN-NPs;乳化-溶剂蒸发法和酸碱中和法,进一步评估糖尿病诱导的动脉粥样硬化。该研究在 50 只动物中进行,分为 5 组,每组 10 只:第 I 组:正常大鼠仅接受生理盐水,第 II 组:糖尿病大鼠,第 III 组:糖尿病大鼠口服 DSN,第 IV 组:糖尿病大鼠接受 HPS 负载的 DSN,第 V 组:糖尿病大鼠接受 PLGA/壳聚糖负载的 DSN。测定总胆固醇、甘油三酯、高密度脂蛋白胆固醇、胰岛素、丙二醛和一氧化氮(NO)、纤溶酶原激活物抑制剂-1(PAI-1)、对氧磷酶-1(PON1)、转化生长因子-β1(TGF-β1)、核因子-ҡB 和血管紧张素 II 的水平。我们的研究表明,与 HPS 负载的 DSN 治疗组和 PLGA/壳聚糖负载的 DSN 治疗组相比,DSN 治疗组有统计学显著差异。此外,研究结果清楚地表明,PLGA/壳聚糖负载的 DSN 组与对照组之间无统计学显著差异,表明 PLGA/壳聚糖负载的 DSN 具有更高的能力来对抗所有大鼠糖尿病诱导的动脉粥样硬化因素。