Increased Water-Solubility and Maintained Antioxidant Power of Resveratrol by Its Encapsulation in Vitamin E TPGS Micelles: A Potential Nutritional Supplement for Chronic Liver Disease
Abstract
:1. Introduction
2. Materials and Methods
2.1. Materials
2.2. Solubility Studies
2.3. Formulations Preparation
2.3.1. Solvent Diffusion Evaporation Method
2.3.2. Solution Casting Method
2.4. Determination of the Encapsulation Efficiency and Drug Loading Capacity
2.5. Determination of Micelle Size, Polydispersity Index (PDI), and Zeta (ƺ) Potential
Re-Dispersibility Study of Lyophilized RES-TPGS Micelles
2.6. Principal Component Analysis (PCA)-Assisted FTIR Spectroscopy
Chemometric Analysis: PCA
2.7. Differential Scanning Calorimetry (DSC)
2.8. Formulation Stability
2.9. In Vitro Release Studies
2.10. Determination of the Radical Scavenging Activity (RSA) of RES-TPGSs
2.11. Cytotoxicity Evaluations
2.11.1. Cell Culture
2.11.2. Viability Assay
2.12. Statistical Analyses
3. Results and Discussion
3.1. TPGS Suitability for RES Encapsulation
3.2. Preparation and Characterization of RES-TPGS Formulations
3.3. FTIR Analysis Assisted by PCA
3.3.1. FTIR Spectra
3.3.2. Principal Component Analysis (PCA)
3.4. Thermal Analysis Using Differential Scanning Calorimetry (DSC)
3.5. Stability of RES-TPGSs
3.6. In Vitro Drug Release Studies
3.7. Antioxidant Activity of RES
3.8. RES-TPGSs’ Effects on HaCaT Cells
4. Conclusions
Supplementary Materials
Author Contributions
Funding
Institutional Review Board Statement
Informed Consent Statement
Data Availability Statement
Acknowledgments
Conflicts of Interest
References
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RES:TPGS (w:w) Ratio in the Preparative Mixture | EE% | DL% |
---|---|---|
1:1 | 10 ± 1 * | 9 ± 1 |
1:2 | 20 ± 2 | 10 ± 2 |
1:3 | 31 ± 3 | 11 ± 1 |
1:4 | 44 ± 5 | 11 ± 2 |
1:5 | 56 ± 6 | 11 ± 3 |
1:6 | 76 ± 1 * | 13 ± 1 |
1:7 | 92 ± 6 * | 15 ± 2 * |
RES:TPGS (w:w) | Size (nm) Fresh Empty | PDI Fresh Empty | Size (nm) Fresh Loaded | PDI Fresh Loaded | ƺ (mV) Loaded | Size (nm) Lyophilized | PDI Lyophilized |
---|---|---|---|---|---|---|---|
1:1 | 14.1 ± 0.6 | 0.27 ± 0.05 | 12.5 ± 0.2 | 0.26 ± 0.04 * | −2.2 ± 3.6 | 12.2 ± 0.3 | 0.35 ± 0.06 * |
1:2 | 20.1 ± 0.7 * | 0.20 ± 0.02 | 12.7 ± 0.8 | 0.24 ± 0.01 | −3.6 ± 4.13 | 13.1 ± 0.6 | 0.27 ± 0.02 |
1:3 | 14.7 ± 0.1 | 0.31 ± 0.09 * | 12.0 ± 0.3 | 0.21 ± 0.07 | −3.1 ± 3.3 | 14.0 ± 0.7 | 0.32 ± 0.04 |
1:4 | 13.2 ± 0.3 | 0.26 ± 0.03 | 11.9 ± 0.8 | 0.19 ± 0.04 | −4.1 ± 2.4 | 15.0 ± 0.3 * | 0.212 ± 0.001 * |
1:5 | 12.3 ± 0.5 | 0.10 ± 0.02 * | 11.9 ± 0.2 | 0.24 ± 0.05 | −4.6 ± 7.7 * | 13.3 ± 0.4 | 0.298 ± 0.009 |
1:6 | 12.3 ± 0.2 | 0.126 ± 0.001 * | 9.13 ± 0.01 * | 0.13 ± 0.01 * | −4.8 ± 3.0 * | 9.7 ± 0.8 * | 0.28 ± 0.04 |
1:7 | 13.2 ± 0.4 | 0.21 ± 0.04 | 9.6 ± 0.3 * | 0.148 ± 0.001 * | −1.6 ± 3.9 * | 11.9 ± 0.1 | 0.245 ± 0.001 |
Sample | RSA% |
---|---|
RES pristine powder | 16.37 ± 0.28 |
Freeze-dried RES pristine powder | 15.71 ± 0.63 |
RES:TPGS 1:2 | 15.93 ± 0.02 |
RES:TPGS 1:6 | 17.96 ± 0.26 |
TPGS | 1.24 ± 0.33 |
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Zuccari, G.; Alfei, S.; Zorzoli, A.; Marimpietri, D.; Turrini, F.; Baldassari, S.; Marchitto, L.; Caviglioli, G. Increased Water-Solubility and Maintained Antioxidant Power of Resveratrol by Its Encapsulation in Vitamin E TPGS Micelles: A Potential Nutritional Supplement for Chronic Liver Disease. Pharmaceutics 2021, 13, 1128. https://doi.org/10.3390/pharmaceutics13081128
Zuccari G, Alfei S, Zorzoli A, Marimpietri D, Turrini F, Baldassari S, Marchitto L, Caviglioli G. Increased Water-Solubility and Maintained Antioxidant Power of Resveratrol by Its Encapsulation in Vitamin E TPGS Micelles: A Potential Nutritional Supplement for Chronic Liver Disease. Pharmaceutics. 2021; 13(8):1128. https://doi.org/10.3390/pharmaceutics13081128
Chicago/Turabian StyleZuccari, Guendalina, Silvana Alfei, Alessia Zorzoli, Danilo Marimpietri, Federica Turrini, Sara Baldassari, Leonardo Marchitto, and Gabriele Caviglioli. 2021. "Increased Water-Solubility and Maintained Antioxidant Power of Resveratrol by Its Encapsulation in Vitamin E TPGS Micelles: A Potential Nutritional Supplement for Chronic Liver Disease" Pharmaceutics 13, no. 8: 1128. https://doi.org/10.3390/pharmaceutics13081128