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

Mohd Nazam Ansari,Ramadan I Al-Shdefat,Mohammed Muqtader Ahmed,Mohammed F Aldawsari,Saad Alshahrani,Najeeb Ur Rehman,Farhat Fatima,Md Khalid Anwer

doi:10.3390/ph13090255

Mohd Nazam Ansari, Ramadan I Al-Shdefat + Show 6 more

Open Access

https://doi.org/10.3390/ph13090255

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Abstract

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.

Highlights

Irritable Bowel Syndrome (IBS) is a widespread and chronic disorder that affects the colon’s motility and ability to work properly [1]
The particle sizes for all solid lipid nanoparticles (SLNs) were found to be in the range of 266.0 ± 6.4 to 1570.5 ± 14.2 nm
The measurement of zeta potential is another particle characterization parameter which is directly correlated with the stability of colloidal particles

Summary

Introduction

Irritable Bowel Syndrome (IBS) is a widespread and chronic disorder that affects the colon’s motility and ability to work properly [1]. Cramps, gas, bloating, diarrhea, and/or constipation are common signs and symptoms of IBS. The exact cause of illness is unknown, so the goal of treatment is to improve the symptoms of the IBS [2,3]. Eluxadoline (ELX) is the choice of drug for IBS but it can be useful for the amelioration of pain and gastrointestinal disorders such as ulcerative colitis and Crohn’s disease [4]. Ulcerative colitis (UC) is a critical disease condition of ulcer and inflammation of the inner lining of the colon that causes rectal bleeding, diarrhea, abdominal pain, nausea, vomiting, anorexia, and fever [5]. UC can occur in people between 15 to 30 years of age and in both sexes

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