Abstract：
Ulcerative colitis (UC) is an idiopathic disease characterized by colonic mucosal tissue destruction secondary to an excessive immune response. We synthesized pH-sensitive cross-linked chitosan/Eudragit® S100 nanoparticles (EU S100/CS NPs) as carriers for 5-aminosalicylic acid (5-ASA) and hesperidin (HSP), then conducted in-vitro and in-vivo studies and evaluated the therapeutic effects. In-vitro analysis revealed that the 5-ASA-loaded EU S100/CS NPs and the HSP-loaded EU S100/CS NPs had smooth and curved surfaces and ranged in size between 250 and 300 nm, with a zeta potential of 32 to 34 mV. FTIR analysis demonstrated that the drugs were loaded on the nanoparticles without significant alterations. The loading capacity and encapsulation efficiency of loading 5-ASA onto EU S100/CS NPs were 25.13 % and 60.81 %, respectively. Regarding HSP, these values were 38.34 % and 77.84 %, respectively. Drug release did not occur in simulated gastric fluid (SGF), while a slow-release pattern was recorded for both drugs in simulated intestinal fluid (SIF). In-vivo macroscopic and histopathological examinations revealed that both NPs containing drugs significantly relieved the symptoms of acetic acid (AA)-induced UC in Wistar rats. We conclude that the synthesized pH-sensitive 5-ASA/EU S100/CS NPs and HSP/EU S100/CS NPs offer promise in treating UC.
摘要：
溃疡性结肠炎（UC）是一种特发性疾病，其特征是继发于过度免疫反应的结肠粘膜组织破坏。我们合成了pH敏感的交联壳聚糖/Eudragit®S100纳米颗粒（EUS100/CSNP）作为5-氨基水杨酸（5-ASA）和橙皮苷（HSP）的载体，然后进行了体外和体内研究，并评估了治疗效果。体外分析显示，负载5-ASA的EUS100/CSNP和负载HSP的EUS100/CSNP具有光滑和弯曲的表面，尺寸在250和300nm之间。zeta电位为32至34mV。FTIR分析表明,药物负载在纳米颗粒上而没有显著改变。将5-ASA装载到EUS100/CSNP上的装载能力和包封效率分别为25.13%和60.81%,分别。关于HSP，这些值分别为38.34%和77.84%，分别。模拟胃液（SGF）中没有药物释放，而两种药物在模拟肠液（SIF）中的缓释模式均有记录。体内宏观和组织病理学检查显示，两种含NPs的药物均显着缓解了Wistar大鼠乙酸（AA）诱导的UC症状。我们得出的结论是，合成的对pH敏感的5-ASA/EUS100/CSNP和HSP/EUS100/CSNP在治疗UC方面具有希望。
