Eluxadoline Loaded Solid Lipid Nanoparticles for Improved Colon Targeting in Rat Model of Ulcerative Colitis
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...
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MDPI AG
2020-09-01
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| Series: | Pharmaceuticals |
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| Online Access: | https://www.mdpi.com/1424-8247/13/9/255 |
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| author | Md. Khalid Anwer Mohammed Muqtader Ahmed Mohammed F. Aldawsari Saad Alshahrani Farhat Fatima Mohd Nazam Ansari Najeeb Ur Rehman Ramadan I. Al-Shdefat |
| author_facet | Md. Khalid Anwer Mohammed Muqtader Ahmed Mohammed F. Aldawsari Saad Alshahrani Farhat Fatima Mohd Nazam Ansari Najeeb Ur Rehman Ramadan I. Al-Shdefat |
| author_sort | Md. Khalid Anwer |
| collection | DOAJ |
| description | 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. |
| first_indexed | 2024-03-10T16:12:14Z |
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| issn | 1424-8247 |
| language | English |
| last_indexed | 2024-03-10T16:12:14Z |
| publishDate | 2020-09-01 |
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| series | Pharmaceuticals |
| spelling | doaj.art-0b03e414241a4517aaa4eb6a485f75d22023-11-20T14:19:57ZengMDPI AGPharmaceuticals1424-82472020-09-0113925510.3390/ph13090255Eluxadoline Loaded Solid Lipid Nanoparticles for Improved Colon Targeting in Rat Model of Ulcerative ColitisMd. Khalid Anwer0Mohammed Muqtader Ahmed1Mohammed F. Aldawsari2Saad Alshahrani3Farhat Fatima4Mohd Nazam Ansari5Najeeb Ur Rehman6Ramadan I. Al-Shdefat7Department of Pharmaceutics, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Alkharj 11942, Saudi ArabiaDepartment of Pharmaceutics, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Alkharj 11942, Saudi ArabiaDepartment of Pharmaceutics, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Alkharj 11942, Saudi ArabiaDepartment of Pharmaceutics, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Alkharj 11942, Saudi ArabiaDepartment of Pharmaceutics, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Alkharj 11942, Saudi ArabiaDepartment of Pharmacology and Toxicology, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Alkharj 11942, Saudi ArabiaDepartment of Pharmacology and Toxicology, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Alkharj 11942, Saudi ArabiaDepartment of Pharmaceutical Sciences, Faculty of Pharmacy, Jadara University, Irbid 21110, JordanThe 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.https://www.mdpi.com/1424-8247/13/9/255eluxadolinelipidsolid lipid nanoparticlesin vitro releaseulcerative colitis |
| spellingShingle | Md. Khalid Anwer Mohammed Muqtader Ahmed Mohammed F. Aldawsari Saad Alshahrani Farhat Fatima Mohd Nazam Ansari Najeeb Ur Rehman Ramadan I. Al-Shdefat Eluxadoline Loaded Solid Lipid Nanoparticles for Improved Colon Targeting in Rat Model of Ulcerative Colitis Pharmaceuticals eluxadoline lipid solid lipid nanoparticles in vitro release ulcerative colitis |
| title | Eluxadoline Loaded Solid Lipid Nanoparticles for Improved Colon Targeting in Rat Model of Ulcerative Colitis |
| title_full | Eluxadoline Loaded Solid Lipid Nanoparticles for Improved Colon Targeting in Rat Model of Ulcerative Colitis |
| title_fullStr | Eluxadoline Loaded Solid Lipid Nanoparticles for Improved Colon Targeting in Rat Model of Ulcerative Colitis |
| title_full_unstemmed | Eluxadoline Loaded Solid Lipid Nanoparticles for Improved Colon Targeting in Rat Model of Ulcerative Colitis |
| title_short | Eluxadoline Loaded Solid Lipid Nanoparticles for Improved Colon Targeting in Rat Model of Ulcerative Colitis |
| title_sort | eluxadoline loaded solid lipid nanoparticles for improved colon targeting in rat model of ulcerative colitis |
| topic | eluxadoline lipid solid lipid nanoparticles in vitro release ulcerative colitis |
| url | https://www.mdpi.com/1424-8247/13/9/255 |
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