Anwer Md Khalid, Ahmed Mohammed Muqtader, Aldawsari Mohammed F, Alshahrani Saad, Fatima Farhat, Ansari Mohd Nazam, Rehman Najeeb Ur, Al-Shdefat Ramadan I
Department of Pharmaceutics, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Alkharj 11942, Saudi Arabia.
Department of Pharmacology and Toxicology, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Alkharj 11942, Saudi Arabia.
Pharmaceuticals (Basel). 2020 Sep 19;13(9):255. doi: 10.3390/ph13090255.
The aim of the current study was to evaluate the therapeutics potential of eluxadoline (ELX) loaded solid lipid nanoparticles (SLNs) in ulcerative colitis. ELX loaded SLNs were prepared using three different lipids according to the solvent emulsification technique. The optimization of prepared SLNs (F1-F3) were carried out based on size, PDI, zeta potential, percent drug entrapment (%EE), and loading (%DL). The lipid (stearic acid) based SLNs (F2) was optimized with particle size (266.0 ± 6.4 nm), PDI (0.217 ± 0.04), zeta potential (31.2 ± 5.19 mV), EE (65.0 ± 4.8%), and DL (4.60 ± 0.8%). The optimized SLNs (F2) was further evaluated by DSC, FTIR, SEM, in vitro release, and stability studies, which confirmed the successful encapsulation of ELX in SLNs. The efficacy of optimized SLNs (F2) in comparison to the pure ELX drug was assessed in acetic acid induced colitis rat models. It was observed that the delivery of ELX by SLNs alleviated the induced acetic acid colitis significantly. Thus, ELX loaded SLNs delivery to the colon has a significant potential to be developed for the treatment of ulcerative colitis.
本研究的目的是评估载有埃卢多啉（ELX）的固体脂质纳米粒（SLNs）在溃疡性结肠炎中的治疗潜力。根据溶剂乳化技术，使用三种不同的脂质制备了载有ELX的SLNs。基于粒径、多分散指数（PDI）、zeta电位、药物包封率（%EE）和载药量（%DL）对制备的SLNs（F1-F3）进行优化。基于硬脂酸的SLNs（F2）的粒径为（266.0±6.4nm），PDI为（0.217±0.04），zeta电位为（31.2±5.19mV），EE为（65.0±4.8%），DL为（4.60±0.8%），得到优化。通过差示扫描量热法（DSC）、傅里叶变换红外光谱法（FTIR）、扫描电子显微镜（SEM）、体外释放和稳定性研究对优化后的SLNs（F2）进行进一步评估，证实ELX成功包封在SLNs中。在乙酸诱导的结肠炎大鼠模型中评估了优化后的SLNs（F2）与纯ELX药物相比的疗效。观察到SLNs递送ELX可显著减轻诱导的乙酸结肠炎。因此，载有ELX的SLNs递送至结肠具有开发用于治疗溃疡性结肠炎的巨大潜力。
