Hot-Melt Extrusion as an Effective Technique for Obtaining an Amorphous System of Curcumin and Piperine with Improved Properties Essential for Their Better Biological Activities
Abstract
:1. Introduction
2. Results and Discussion
3. Materials and Methods
3.1. Materials
3.2. Preparation of the Systems
3.3. Solid-State IDENTIFICATION
3.3.1. X-ray Powder Diffraction (XRPD)
3.3.2. Differential Scanning Calorimetry (DSC)
3.3.3. Fourier Transform Infrared Spectroscopy with Attenuated Total Reflectance (FTIR-ATR)
3.3.4. Physical Stability
3.4. Physicochemical Characterization
3.4.1. HPLC Conditions
3.4.2. Media for Dissolution and Solubility Studies
3.4.3. Dissolution Studies
3.4.4. Apparent Solubility Studies
3.4.5. Permeability Studies
3.5. Biological Activities Studies
3.5.1. Antioxidant Activity Assay
3.5.2. Determination of Butyrylcholinesterase (BuChE) Inhibition
3.6. Statistical Analysis
4. Conclusions
Supplementary Materials
Author Contributions
Funding
Institutional Review Board Statement
Informed Consent Statement
Data Availability Statement
Conflicts of Interest
Sample Availability
References
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System (Cur:Pip:VA 64) | Compound | |||
---|---|---|---|---|
CUR | PIP | |||
Conc. (mg/mL) | Improv. (-fold) | Conc. (mg/mL) | Improv. (-fold) | |
Raw | 0.0001 ± 0.0000 e | - | 0.006 ± 0.0001 e | - |
1:1:4 | 0.689 ± 0.002 d | 5514 | 0.153 ± 0.001 d | 23 |
1:1:8 | 0.910 ± 0.003 c | 7283 | 0.669 ± 0.028 c | 103 |
1:1:12 | 1.049 ± 0.009 b | 8396 | 0.826 ± 0.010 b | 138 |
1:1:16 | 1.187 ± 0.010 a | 9496 | 1.050 ± 0.016 a | 161 |
System (Cur:Pip:VA 64) | Compound | |||||
---|---|---|---|---|---|---|
CUR | PIP | |||||
Conc. (mg/mL) | Improv. (-fold) | Conc. (mg/mL) | Improv. (-fold) | |||
Model | GIT | Raw | 3.34 × 10−6 ± 1.94 × 10−6, e | - | 5.86 × 10−4 ± 1.35 × 10−4, e | - |
1:1:4 | 1.09 × 10−3 ± 4.09 × 10−4, d | 326 | 5.33 × 10−3 ± 1.76 × 10−3, d | 9 | ||
1:1:8 | 2.60 × 10−2 ± 4.57 × 10−3, c | 7776 | 1.21 × 10−1 ± 8.88 × 10−3, c | 207 | ||
1:1:12 | 3.33 × 10−2 ± 2.87 × 10−3, b | 9976 | 1.66 × 10−1 ± 1.09 × 10−2, b | 284 | ||
1:1:16 | 4.20 × 10−2 ± 2.21 × 10−3, a | 12,578 | 2.01 × 10−1 ± 7.77 × 10−3, a | 343 | ||
BBB | Raw | 1.86 × 10−5 ± 2.48 × 10−6, e | - | 2.10 × 10−3 ± 8.86 × 10−5, d | - | |
1:1:4 | 1.51 × 10−2 ± 1.86 × 10−3, d | 815 | 2.06 × 10−2 ± 3.73 × 10−3, c | 10 | ||
1:1:8 | 4.12 × 10−2 ± 1.40 × 10−3, c | 2218 | 2.99 × 10−1 ± 6.85 × 10−3, b | 142 | ||
1:1:12 | 4.45 × 10−2 ± 2.47 × 10−3, b | 2436 | 3.25 × 10−1 ± 2.97 × 10−2, a, b | 155 | ||
1:1:16 | 5.70 × 10−2 ± 1.40 × 10−3, a | 3069 | 3.45 × 10−1 ± 2.07 × 10−2, a | 164 |
System (Cur:Pip:VA 64) | Assay | |
---|---|---|
DPPH | BChE | |
% of Inhibition | % of Inhibition | |
Raw | 10.69 ± 0.92 d | 1.24 ± 0.27 e |
1:1:4 | 48.16 ± 2.56 c | 42.87 ± 2.27 d |
1:1:8 | 87.87 ± 1.12 b | 77.46 ± 2.48 c |
1:1:12 | 96.85 ± 1.35 a | 92.35 ± 3.55 b |
1:1:16 | 96.97 ± 1.32 a | 98.52 ± 0.87 a |
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Wdowiak, K.; Pietrzak, R.; Tykarska, E.; Cielecka-Piontek, J. Hot-Melt Extrusion as an Effective Technique for Obtaining an Amorphous System of Curcumin and Piperine with Improved Properties Essential for Their Better Biological Activities. Molecules 2023, 28, 3848. https://doi.org/10.3390/molecules28093848
Wdowiak K, Pietrzak R, Tykarska E, Cielecka-Piontek J. Hot-Melt Extrusion as an Effective Technique for Obtaining an Amorphous System of Curcumin and Piperine with Improved Properties Essential for Their Better Biological Activities. Molecules. 2023; 28(9):3848. https://doi.org/10.3390/molecules28093848
Chicago/Turabian StyleWdowiak, Kamil, Robert Pietrzak, Ewa Tykarska, and Judyta Cielecka-Piontek. 2023. "Hot-Melt Extrusion as an Effective Technique for Obtaining an Amorphous System of Curcumin and Piperine with Improved Properties Essential for Their Better Biological Activities" Molecules 28, no. 9: 3848. https://doi.org/10.3390/molecules28093848