Eluxadoline Loaded Solid Lipid Nanoparticles for Improved Colon Targeting in Rat Model of Ulcerative Colitis

被引:21
作者
Anwer, Md. Khalid [1 ]
Ahmed, Mohammed Muqtader [1 ]
Aldawsari, Mohammed F. [1 ]
Alshahrani, Saad [1 ]
Fatima, Farhat [1 ]
Ansari, Mohd Nazam [2 ]
Rehman, Najeeb Ur [2 ]
Al-Shdefat, Ramadan I. [3 ]
机构
[1] Prince Sattam Bin Abdulaziz Univ, Dept Pharmaceut, Coll Pharm, Alkharj 11942, Saudi Arabia
[2] Prince Sattam Bin Abdulaziz Univ, Dept Pharmacol & Toxicol, Coll Pharm, Alkharj 11942, Saudi Arabia
[3] Jadara Univ, Dept Pharmaceut Sci, Fac Pharm, Irbid 21110, Jordan
关键词
eluxadoline; lipid; solid lipid nanoparticles; in vitro release; ulcerative colitis; MOUSE MODELS; CARRIERS; PHARMACOKINETICS; RELEASE;
D O I
10.3390/ph13090255
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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.
引用
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页码:1 / 16
页数:16
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