Shenyang Pharmaceutical University, Benxi, Liaoning 110016, PR China.
Shenyang Pharmaceutical University, Benxi, Liaoning 110016, PR China.
Colloids Surf B Biointerfaces. 2024 Apr;236:113809. doi: 10.1016/j.colsurfb.2024.113809. Epub 2024 Feb 23.
The aim of the study was to develop an oral targeting drug delivery system (OTDDS) of oxymatrine (OMT) to effectively treat ulcerative colitis (UC). The OTDDS of OMT (OMT/SA-NPs) was constructed with OMT, pectin, Ca, chitosan (CS) and sialic acid (SA). The obtained particles were characterized in terms of particle size, zeta potential, morphology, drug loading, encapsulation efficiency, drug release and stability. The average size of OMT/SA-NPs was 255.0 nm with a zeta potential of -12.4 mV. The loading content and encapsulation efficiency of OMT/SA-NPs were 14.65% and 84.83%, respectively. The particle size of OMT/SA-NPs changed slightly in the gastrointestinal tract. The nanoparticles can delivery most of the drug to the colon region. In vitro cell experiments showed that the SA-NPs had excellent biocompatibility and anti-inflammation, and the uptake of SA-NPs by RAW 264.7 cells was time and concentration-dependent. The conjugated SA can help the internalization of NPs into target cells. In vivo experiments showed that OMT/SA-NPs had a superior anti-inflammation effect and the effect of reducing UC, which was attributed to the delivery most of OMT to the colonic lumen, the specific targeting and retention in colitis site and the combined anti-inflammation of OMT and NPs.
本研究旨在开发氧化苦参碱（OMT）的口服靶向药物传递系统（OTDDS），以有效治疗溃疡性结肠炎（UC）。OMT 的 OTDDS（OMT/SA-NPs）由 OMT、果胶、Ca、壳聚糖（CS）和唾液酸（SA）构建而成。所获得的颗粒在粒径、Zeta 电位、形态、载药量、包封效率、药物释放和稳定性方面进行了表征。OMT/SA-NPs 的平均粒径为 255.0nm，Zeta 电位为-12.4mV。OMT/SA-NPs 的载药量和包封效率分别为 14.65%和 84.83%。OMT/SA-NPs 的粒径在胃肠道中变化不大。纳米粒可以将大部分药物递送到结肠区域。体外细胞实验表明，SA-NPs 具有良好的生物相容性和抗炎作用，SA-NPs 被 RAW 264.7 细胞摄取具有时间和浓度依赖性。结合的 SA 有助于 NPs 进入靶细胞的内化。体内实验表明，OMT/SA-NPs 具有优异的抗炎作用和减轻 UC 的作用，这归因于将大部分 OMT 递送到结肠腔中，在结肠炎部位的特异性靶向和保留以及 OMT 和 NPs 的联合抗炎作用。
