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Naringenin loaded multifunctional nanoparticles to enhance the chemotherapeutic efficacy in hepatic fibrosis.
Biomedical Microdevices ( IF 3.0 ) Pub Date : 2020-09-21 , DOI: 10.1007/s10544-020-00524-1
Fan Yang 1 , Shenghe Hu 2 , Xun Sheng 3 , Yu Liu 4
Affiliation  

Naringenin is highly potent dietary phenolic compound (Flavonoids) found as a major bioactive in citrus fruits. The low solubility of Naringenin, decreases its availability at the site of action by hindering solubility and transportation across the biological membrane. Naringenin loaded nanoparticles enhance the solubility and drug availability at site of action. Naringenin solid lipid nanoparticles were prepared by emulsification and homogenization method using GMO (glycerylmonooleate) and TPGS (Tocopheryl polyethylene glycol succinate) as co-stabilizer. Physico-chemical characterization confirmed the particles were of nanometer size, smooth and spherical morphology. The FTIR and DSC studies conforms that drug and polymers are compatible. The in-vitro study shows prolong and sustained release of Naringenin upto 90 Hrs. In-vivo studies conforms the prolonged and efficient treatment of Hepatic fibrosis. The liver enzymes and pro inflammatory cytokines in blood got significantly reversed with the rats exposed to Naringenin nanoparticle indicating reduced liver damage and fibrosis. Nanoformulation enhances the bioavailability of Naringenin and liver specific delivery of the same, which up-regulates MMP-2 hepatic proteins resulting in reduced liver fibrosis.



中文翻译:


柚皮素负载多功能纳米粒子可增强肝纤维化的化疗效果。



柚皮素是一种高效的膳食酚类化合物(类黄酮),被发现是柑橘类水果中的主要生物活性物质。柚皮素的低溶解度会阻碍溶解度和跨生物膜的运输,从而降低其在作用部位的可用性。负载柚皮素的纳米颗粒增强了作用部位的溶解度和药物利用度。以GMO(单油酸甘油酯)和TPGS(生育酚聚乙二醇琥珀酸酯)为助稳定剂,采用乳化均质法制备柚皮素固体脂质纳米粒。物理化学表征证实颗粒具有纳米尺寸、光滑的球形形态。 FTIR 和 DSC 研究证实药物和聚合物是相容的。体外研究表明柚皮素的持续释放时间长达 90 小时。体内研究证实了肝纤维化的长期有效治疗。暴露于柚皮素纳米颗粒的大鼠血液中的肝酶和促炎细胞因子显着逆转,表明肝损伤和纤维化减少。纳米制剂增强了柚皮素的生物利用度及其肝脏特异性递送,从而上调 MMP-2 肝蛋白,从而减少肝纤维化。

更新日期:2020-09-21
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