■氯化Nitidine(NC)是一种植物性药物,以其有效的抗炎作用而闻名,抗疟药,和肝细胞癌抑制特性;然而,其有限的溶解性对其开发和应用提出了挑战。为了解决这个问题,我们设计了一种结肠靶向递送系统(NC-CS/PT-NP),旨在通过增强NC和肠道微生物群之间的相互作用来调节肠道微生物群的生态失调,从而发挥对抗非酒精性脂肪性肝病的作用。
■使用离子凝胶法合成NC-CS/PT-NP。随后,粒度分布,形态学,药物装载效率,表征了NC-CS/PT-NP的释放行为。此外,通过血清生化分析研究NC-CS/PT-NP对高脂饮食(HFD)诱导的小鼠非酒精性脂肪性肝病(NAFLD)的影响,ELISA,和组织化学染色。此外,使用16SrDNA基因测序分析NC-CS/PT-NP对肠道菌群的影响。
■本研究中制备的纳米颗粒的平均粒径为(255.9±5.10)nm,包封率为(72.83±2.13)%,载药量为(4.65±0.44)%。体外释放实验表明,在胃和小肠中的累积释放率低于22.0%,而在结肠中达到66.75%。对HFD诱导的NAFLD小鼠进行的体内实验表明,用NC-CS/PT-NP治疗可抑制体重增加,血清天冬氨酸转氨酶(AST)降低,丙氨酸氨基转移酶(ALT)和脂质水平,改善肝脏和肠道炎症,并改变了小鼠肠道微生物群的多样性。
■这项研究为使用中药活性成分通过调节肠道微生物群治疗NAFLD提供了新的证据。
UNASSIGNED: Nitidine chloride (NC) is a botanical drug renowned for its potent anti-inflammatory, antimalarial, and hepatocellular carcinoma-inhibiting properties; however, its limited solubility poses challenges to its development and application. To address this issue, we have devised a colon-targeted delivery system (NC-CS/PT-NPs) aimed at modulating the dysbiosis of the gut microbiota by augmenting the interaction between NC and the intestinal microbiota, thereby exerting an effect against nonalcoholic fatty liver disease.
UNASSIGNED: The NC-CS/PT-NPs were synthesized using the ion gel method. Subsequently, the particle size distribution, morphology, drug loading efficiency, and release behavior of the NC-CS/PT-NPs were characterized. Furthermore, the impact of NC-CS/PT-NPs on non-alcoholic fatty liver disease (NAFLD) induced by a high-fat diet (HFD) in mice was investigated through serum biochemical analysis, ELISA, and histochemical staining. Additionally, the influence of NC-CS/PT-NPs on intestinal microbiota was analyzed using 16S rDNA gene sequencing.
UNASSIGNED: The nanoparticles prepared in this study have an average particle size of (255.9±5.10) nm, with an encapsulation rate of (72.83±2.13) % and a drug loading of (4.65±0.44) %. In vitro release experiments demonstrated that the cumulative release rate in the stomach and small intestine was lower than 22.0%, while it reached 66.75% in the colon. In vivo experiments conducted on HFD-induced NAFLD mice showed that treatment with NC-CS/PT-NPs inhibited weight gain, decreased serum aspartate aminotransferase (AST), Alanine aminotransferase (ALT) and lipid levels, improved liver and intestinal inflammation, and altered the diversity of gut microbiota in mice.
UNASSIGNED: This study provides new evidence for the treatment of NAFLD through the regulation of gut microbiota using active ingredients from traditional Chinese medicine.