Eluxadoline Loaded Solid Lipid Nanoparticles for Improved Colon Targeting in Rat Model of Ulcerative Colitis
Abstract
:1. Introduction
2. Results and Discussion
2.1. Particles Characterization
2.2. Percent Drug Entrapment and Loading
2.3. Thermal Analysis
2.4. FTIR Spectra Analysis
2.5. In-Vitro Drug Release Profile
2.6. Morphology
2.7. Stability Studies
2.8. In Vivo Studies: Assessment of Ulcerative Colitis
2.8.1. Effect of ELX and F2 on Disease Activity Index (DAI)
2.8.2. Effect of ELX and F2 on Macroscopic Damage
2.8.3. Effect of ELX and F2 on Lipid Peroxidation Activity
2.8.4. Effect of ELX and F2 on Antioxidant Activity
2.8.5. Effect of ELX and F2 on Microscopic Damage
3. Materials and Method
3.1. Materials
3.2. Preparation of ELX Loaded Solid Lipid Nanoparticle (SLNs)
3.3. Particles Characterization
3.4. Percent Drug Entrapment (%EE) and Loading (%DL)
3.5. Thermal Analysis
3.6. FTIR Spectra Analysis
3.7. Morphology
3.8. In-Vitro Release Studies
3.9. Stability Studies
3.10. In Vivo Studies: Assessment of Ulcerative Colitis
3.10.1. Experimental Animals
3.10.2. Study Design
3.10.3. Induction of Acetic Acid Colitis
3.10.4. Assessment of Disease Activity Index (DAI)
3.10.5. Assessment of Macroscopic Damage
3.10.6. Assessment of Lipid Peroxidation Activity
3.10.7. Assessment of Antioxidant Activity
3.10.8. Microscopic Assessment of UC
3.11. Statistical Analysis
4. Conclusions
Author Contributions
Funding
Acknowledgments
Conflicts of Interest
References
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SLNs | SIZE ± SD (nm) | PDI | ZP ± SD (mV) | %EE ± SD | %DL ± SD |
---|---|---|---|---|---|
F1 | 394.3 ± 8.4 | 0.226 ± 0.03 | 26.8 ± 5.41 | 73.0 ± 3.2 | 5.13 ± 1.2 |
F2 | 266.0 ± 6.4 | 0.217 ± 0.04 | 31.2 ± 5.19 | 65.0 ± 4.8 | 4.60 ± 0.8 |
F3 | 1570.5 ± 14.2 | 0.882 ± 0.06 | 25.7 ± 6.11 | 54.1 ± 2.6 | 3.82 ± 0.7 |
Months | Conditions | Particle Size (nm ± SD) | PDI (± SD) | ZP (mV) (mV ± SD) | Entrapment Efficiency (% ± SD) | Release (% ± SD) |
---|---|---|---|---|---|---|
0 | - | 266 ± 6.4 | 0.217 ± 0.04 | 31.2 ± 5.1 | 65.0 ± 4.8 | 95.7 ± 4.7 |
1 | 30 ± 2 °C/65 ± 5% RH | 268 ± 4.5 | 0.243 ± 0.02 | 30.3 ± 6.3 | 67.2 ± 2.7 | 96.5 ± 3.1 |
2 | 272 ± 7.4 | 0.249 ± 0.06 | 27.2 ± 5.8 | 63.6 ± 3.9 | 94.6 ± 4.4 | |
3 | 276 ± 8.5 | 0.212 ± 0.04 | 30.5 ± 4.2 | 62.4 ± 8.3 | 91.4 ± 7.3 | |
1 | 40 ± 2 °C/75 ± 5% RH | 267 ± 2.5 | 0.223 ± 0.07 | 33.6 ± 9.4 | 65.2 ± 4.8 | 93.6 ± 6.4 |
2 | 273 ± 6.8 | 0.279 ± 0.09 | 29.2 ± 6.3 | 63.6 ± 2.6 | 93.2 ± 7.3 | |
3 | 276 ± 7.5 | 0.272 ± 0.08 | 25.7 ± 6.7 | 61.5 ± 5.9 | 90.8 ± 6.2 |
SLNs | ELX (mg) | Lipids (400 mg) | Soyalecithin (%w/v) |
---|---|---|---|
F1 | 40 | Glyceryl monostearate | 0.5 |
F2 | 40 | Stearic acid | 0.5 |
F3 | 40 | Glyceryl trioctanoate | 0.5 |
Weight Loss (%) | Stool Consistency | Occult/Gross Bleeding | Score |
---|---|---|---|
Normal | Normal | Normal | 0 |
1–5 | Soft but still formed | - | 1 |
5–10 | Loose stools | Hemo-occult positive | 2 |
10–20 | Diarrhea | - | 3 |
>20 | - | Gross bleeding | 4 |
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Anwer, M.K.; Ahmed, M.M.; Aldawsari, M.F.; Alshahrani, S.; Fatima, F.; Ansari, M.N.; Rehman, N.U.; Al-Shdefat, R.I. Eluxadoline Loaded Solid Lipid Nanoparticles for Improved Colon Targeting in Rat Model of Ulcerative Colitis. Pharmaceuticals 2020, 13, 255. https://doi.org/10.3390/ph13090255
Anwer MK, Ahmed MM, Aldawsari MF, Alshahrani S, Fatima F, Ansari MN, Rehman NU, Al-Shdefat RI. Eluxadoline Loaded Solid Lipid Nanoparticles for Improved Colon Targeting in Rat Model of Ulcerative Colitis. Pharmaceuticals. 2020; 13(9):255. https://doi.org/10.3390/ph13090255
Chicago/Turabian StyleAnwer, Md. Khalid, Mohammed Muqtader Ahmed, Mohammed F. Aldawsari, Saad Alshahrani, Farhat Fatima, Mohd Nazam Ansari, Najeeb Ur Rehman, and Ramadan I. Al-Shdefat. 2020. "Eluxadoline Loaded Solid Lipid Nanoparticles for Improved Colon Targeting in Rat Model of Ulcerative Colitis" Pharmaceuticals 13, no. 9: 255. https://doi.org/10.3390/ph13090255