Amorphous Solid Dispersion of Hesperidin with Polymer Excipients for Enhanced Apparent Solubility as a More Effective Approach to the Treatment of Civilization Diseases
Abstract
:1. Introduction
2. Results
3. Discussion
4. Materials and Methods
4.1. The Active Substance and Materials
4.2. Preparation of Amorphous Hesperidin and Hesperidin-Carrier Amorphous Solid Dispersions
4.3. The Characterization of Hesperidin-Carrier Amorphous Solid Dispersions
4.3.1. X-ray Powder Diffraction (XRPD)
4.3.2. Thermogravimetric Analysis (TG)
4.3.3. Differential Scanning Calorimetry (DSC) and Gordon–Taylor equation
4.3.4. Fourier-Transform Infrared Spectroscopy (FTIR) and Density Functional Theory (DFT) Calculations
4.4. Solubility and Apparent Solubility Studies of Hesperidin and Its Amorphous Solid Dispersions with Carriers
4.4.1. HPLC Method
4.4.2. Media for Solubility and Apparent Solubility Studies
4.4.3. Procedure of Solubility Studies
4.4.4. Procedure of Apparent Solubility Studies
5. Conclusions
Supplementary Materials
Author Contributions
Funding
Institutional Review Board Statement
Informed Consent Statement
Data Availability Statement
Conflicts of Interest
References
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Mass (mg) | ΔCp (J·(g K)−1) | Tg, calc (°C) | Tg, exp (°C) | Deviation | |
---|---|---|---|---|---|
Hes | 10.24 | 0.431 | − | 107.10 ± 0.65 | − |
Sol | 9.45 | 0.247 | − | 79.20 ± 0.55 | − |
Hes:Sol 1:2 | 9.28 | 0.192 | 84.52 ± 0.58 | 88.70 ± 0.86 | + |
Hes:Sol 1:5 | 8.79 | 0.171 | 81.60 ± 0.56 | 81.30 ± 0.36 | * |
HPMC | 6.43 | 0.211 | − | 134.20 ± 0.93 | − |
Hes:HPMC 1:2 | 10.74 | 0.105 | 125.02 ± 0.33 | 114.30 ± 0.67 | − |
Hes:HPMC 1:5 | 10.23 | 0.239 | 129.59 ± 0.61 | 122.10 ± 0.76 | − |
Medium | System | Concentration [mg mL−1] | Improved Solubility [–Fold] |
---|---|---|---|
Water | Hesperidin | 0.009 ± 0.001 | – |
Hes:Sol 1:2 | 1.149 ± 0.011 | 128 | |
Hes:Sol 1:5 | 2.710 ± 0.004 | 301 | |
Hes:SA 1:2 | 1.059 ± 0.008 | 118 | |
Hes:SA 1:5 | 1.184 ± 0.003 | 132 | |
Hes:HPMC 1:2 | 0.088 ± 0.001 | 10 | |
Hes:HPMC 1:5 | 0.622 ± 0.002 | 69 | |
phosphate buffer (pH 6.8) | Hesperidin | 0.009 ± 0.002 | – |
Hes:Sol 1:2 | 0.869 ± 0.020 | 97 | |
Hes:Sol 1:5 | 2.616 ± 0.036 | 291 | |
Hes:SA 1:2 | 1.605 ± 0.014 | 178 | |
Hes:SA 1:5 | 1.726 ± 0.003 | 192 | |
Hes:HPMC 1:2 | 0.068 ± 0.001 | 8 | |
Hes:HPMC 1:5 | 0.711 ± 0.007 | 79 | |
HCl 0.1 N | Hesperidin | 0.008 ± 0.003 | – |
Hes:Sol 1:2 | 0.777 ± 0.009 | 97 | |
Hes:Sol 1:5 | 2.486 ± 0.033 | 311 | |
Hes:SA 1:2 | 0.055 ± 0.002 | 7 | |
Hes:SA 1:5 | 0.027 ± 0.002 | 4 | |
Hes:HPMC 1:2 | 0.064 ± 0.001 | 8 | |
Hes:HPMC 1:5 | 0.075 ± 0.001 | 9 |
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Rosiak, N.; Wdowiak, K.; Tykarska, E.; Cielecka-Piontek, J. Amorphous Solid Dispersion of Hesperidin with Polymer Excipients for Enhanced Apparent Solubility as a More Effective Approach to the Treatment of Civilization Diseases. Int. J. Mol. Sci. 2022, 23, 15198. https://doi.org/10.3390/ijms232315198
Rosiak N, Wdowiak K, Tykarska E, Cielecka-Piontek J. Amorphous Solid Dispersion of Hesperidin with Polymer Excipients for Enhanced Apparent Solubility as a More Effective Approach to the Treatment of Civilization Diseases. International Journal of Molecular Sciences. 2022; 23(23):15198. https://doi.org/10.3390/ijms232315198
Chicago/Turabian StyleRosiak, Natalia, Kamil Wdowiak, Ewa Tykarska, and Judyta Cielecka-Piontek. 2022. "Amorphous Solid Dispersion of Hesperidin with Polymer Excipients for Enhanced Apparent Solubility as a More Effective Approach to the Treatment of Civilization Diseases" International Journal of Molecular Sciences 23, no. 23: 15198. https://doi.org/10.3390/ijms232315198