Encapsulation in Polymeric Nanoparticles Enhances the Enzymatic Stability and the Permeability of the GLP-1 Analog, Liraglutide, Across a Culture Model of Intestinal Permeability
Abstract
:1. Introduction
2. Materials and Methods
2.1. Materials
2.2. Human Caco-2 Intestinal Epithelial Cell Line
2.3. Preparation of PLGA NPs
2.4. Preparation of Lira and PN159 Solutions
2.5. In Vitro Drug Release Study
2.6. Release Kinetics Studies
2.7. Enzymatic Degradation Study
2.8. Treatment of Caco-2 Cells
2.9. Cell Viability Measurement by Impedance
2.10. Permeability Study on the Caco-2 Model
2.11. Immunohistochemistry
2.12. Chromatographic Equipment and Conditions
2.13. Statistical Analysis
3. Results
3.1. In Vitro Release of Lira from PLGA NPs
3.2. Release Kinetics Studies
3.3. Enzymatic Degradation Study
3.4. Cell Viability Assay
3.5. Permeability Study on the Caco-2 Intestinal Barrier Model
3.6. Immunohistochemistry
4. Discussion
5. Conclusions
Author Contributions
Funding
Conflicts of Interest
References
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Formulation Parameters | |
---|---|
PLGA amount | 60 mg |
Lira amount | 5 mg |
2nd sonication time | 0.5 min |
PVA amount | 1.48% |
Lyoprotectant type | Mannitol |
Lyoprotectant amount | 5% |
W2/O ratio | 5 |
Kinetic Model | SGF | SIF | ||||
---|---|---|---|---|---|---|
N | k | R2 | n | k | R2 | |
Zero order | 7.9857 | 1.84 | 0.9991 | 0.9836 | 12.658 | 0.9925 |
First order | 0.038 | 2.01 | 0.998 | 0.0052 | 1.9418 | 0.9934 |
Higuchi | 17.049 | 10.262 | 0.9854 | 4.1563 | 8.3559 | 0.9983 |
Korsmeyer-Peppas | 1.3162 | 0.762 | 0.9993 | 0.2456 | 1.0696 | 0.9996 |
Liraglutide | Recovery (%) Mean ± SD |
---|---|
Liraglutide | 80.9 ± 1.6 |
Liraglutide in NPs | 75.3 ± 2.3 |
Liraglutide + PN159 | 81.3 ± 6.9 |
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Ismail, R.; Bocsik, A.; Katona, G.; Gróf, I.; Deli, M.A.; Csóka, I. Encapsulation in Polymeric Nanoparticles Enhances the Enzymatic Stability and the Permeability of the GLP-1 Analog, Liraglutide, Across a Culture Model of Intestinal Permeability. Pharmaceutics 2019, 11, 599. https://doi.org/10.3390/pharmaceutics11110599
Ismail R, Bocsik A, Katona G, Gróf I, Deli MA, Csóka I. Encapsulation in Polymeric Nanoparticles Enhances the Enzymatic Stability and the Permeability of the GLP-1 Analog, Liraglutide, Across a Culture Model of Intestinal Permeability. Pharmaceutics. 2019; 11(11):599. https://doi.org/10.3390/pharmaceutics11110599
Chicago/Turabian StyleIsmail, Ruba, Alexandra Bocsik, Gábor Katona, Ilona Gróf, Mária A. Deli, and Ildikó Csóka. 2019. "Encapsulation in Polymeric Nanoparticles Enhances the Enzymatic Stability and the Permeability of the GLP-1 Analog, Liraglutide, Across a Culture Model of Intestinal Permeability" Pharmaceutics 11, no. 11: 599. https://doi.org/10.3390/pharmaceutics11110599