The Impact of Hypromellose on Pharmaceutical Properties of Alginate Microparticles as Novel Drug Carriers for Posaconazole
Abstract
:1. Introduction
2. Results and Discussion
2.1. Microparticle Characterization
2.2. Swelling and Mucoadhesion
2.3. In Vitro POS Release
2.4. DSC Analysis
2.5. Antifungal Activity
3. Materials and Methods
3.1. Materials
3.2. ALG and ALG/HPMC Solutions Preparation
3.3. Viscosity Measurements
3.4. Microparticle Preparation
3.5. Moisture Presence
3.6. Assessment of Microparticles Morphology
3.7. Estimation of POS Loading, Encapsulation Efficacy, and Production Yield
3.8. POS Spectrophotometry Analysis
3.9. Swelling Capacity
3.10. Mucoadhesive Properties
3.11. In Vitro POS Release
3.12. Mathematical Modeling of POS Release Profile
3.13. Thermal Analysis
3.14. Antifungal Activity
3.15. Statistics
4. Conclusions
Author Contributions
Funding
Institutional Review Board Statement
Informed Consent Statement
Data Availability Statement
Acknowledgments
Conflicts of Interest
References
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Formulation | Particle Size (µm) | Percent Loading (%) | Encapsulation Efficiency (%) | Production Yield (%) | Moisture Content (%) |
---|---|---|---|---|---|
A1 | 10.03 ± 3.84 | - | - | 63.99 ± 2.93 | 10.59 ± 1.09 * |
A2 | 10.69 ± 3.49 | - | - | 63.49 ± 2.77 | 13.28 ± 0.92 |
A3 | 13.42 ± 5.50 | - | - | 64.47 ± 6.51 | 14.23 ± 1.53 |
F1 | 12.66 ± 4.80 | 36.21 ± 2.95 | 118.73 ± 5.44 | 53.38 ± 4.14 | 13.12 ± 1.97 |
F2 | 13.73 ± 4.63 | 59.68 ± 2.72 * | 108.64 ± 8.84 * | 53.23 ± 2.65 | 8.97 ± 0.49 * |
F3 | 12.81 ± 5.86 | 37.46 ± 1.41 | 112.38 ± 4.22 | 57.72 ± 4.33 | 11.24 ± 2.22 |
F4 | 15.27 ± 5.76 | 54.30 ± 2.59 * | 108.59 ± 5.18 * | 56.55 ± 4.11 | 9.10 ± 1.48 * |
F5 | 11.70 ± 4.81 | 39.89 ± 1.14 | 119.67 ± 3.41 | 53.35 ± 2.95 | 8.93 ± 1.16 * |
F6 | 13.19 ± 4.01 | 58.39 ± 2.24 * | 116.78 ± 4.48 | 46.62 ± 3.84 * | 10.20 ± 0.81 |
H1 | 10.53 ± 3.22 | - | - | 54.06 ± 5.77 | 7.54 ± 0.32 * |
H2 | 14.00 ± 4.27 | - | - | 51.61 ± 4.69 | 11.87 ± 0.70 |
H3 | 15.25 ± 5.12 | - | - | 52.03 ± 4.58 | 10.54 ± 2.28 |
H4 | 12.23 ± 4.13 | 37.89 ± 2.39 | 113.77 ± 7.18 | 62.46 ± 4.56 | 9.89 ± 2.18 |
H5 | 14.08 ± 3.96 | 37.41 ± 3.09 | 112.34 ± 9.28 | 59.43 ± 1.90 | 7.60 ± 2.79 |
H6 | 15.64 ± 4.48 | 27.60 ± 2.84 * | 138.00 ± 14.21 * | 60.05 ± 1.18 | 13.44 ± 0.35 * |
Formulation | Zero-Order Kinetics | First-Order Kinetics | Higuchi Model | Hixson–Crowell Model | Korsmeyer–Peppas Model | ||||||
---|---|---|---|---|---|---|---|---|---|---|---|
R2 | K | R2 | K | R2 | K | R2 | K | R2 | K | n | |
0.1 M HCl (pH 1.2) | |||||||||||
F1 | 0.91 | 2.25 | 0.98 | 0.04 | 0.99 | 15.42 | 0.98 | 113.48 | 0.99 | 0.54 | 0.47 |
F2 | 0.88 | 2.22 | 0.97 | 0.04 | 0.99 | 17.43 | 0.98 | 115.33 | 0.99 | 0.55 | 0.49 |
F3 | 0.88 | 2.15 | 0.96 | 0.04 | 0.99 | 16.68 | 0.98 | 118.49 | 0.99 | 0.55 | 0.48 |
F4 | 0.88 | 2.37 | 0.98 | 0.05 | 0.99 | 18.31 | 0.98 | 107.89 | 0.99 | 0.56 | 0.49 |
F5 | 0.90 | 1.93 | 0.96 | 0.03 | 0.99 | 13.99 | 0.99 | 130.85 | 0.99 | 0.54 | 0.50 |
F6 | 0.91 | 2.72 | 0.99 | 0.07 | 0.99 | 19.23 | 0.97 | 91.96 | 0.99 | 0.59 | 0.53 |
H4 | 0.35 | 1.52 | 0.47 | 0.04 | 0.55 | 11.32 | 0.98 | 104.69 | 0.75 | 0.51 | 0.34 |
H5 | 0.24 | 1.73 | 0.37 | 0.03 | 0.43 | 13.77 | 0.95 | 44.00 | 0.66 | 0.54 | 0.36 |
H6 | 0.89 | 24.06 | 0.99 | 1.32 | 0.93 | 61.39 | 0.97 | 4.66 | 0.93 | 0.73 | 0.57 |
SVF (pH 4.2) | |||||||||||
F1 | 0.55 | 1.63 | 0.88 | 0.10 | 0.69 | 16.58 | 0.76 | 10.84 | 0.60 | 0.20 | 0.14 |
F2 | 0.56 | 1.52 | 0.99 | 0.18 | 0.70 | 15.51 | 0.77 | 8.92 | 0.58 | 0.20 | 0.12 |
F3 | 0.62 | 1.85 | 0.99 | 0.15 | 0.76 | 18.59 | 0.89 | 29.87 | 0.61 | 0.18 | 0.17 |
F4 | 0.45 | 1.42 | 0.98 | 0.27 | 0.60 | 14.84 | 0.87 | 17.76 | 0.51 | 0.21 | 0.12 |
F5 | 0.64 | 1.75 | 0.86 | 0.07 | 0.76 | 17.60 | 0.96 | 60.44 | 0.64 | 0.18 | 0.17 |
F6 | 0.88 | 4.92 | 0.85 | 0.43 | 0.94 | 34.02 | 0.86 | 25.76 | 0.86 | 0.22 | 0.27 |
H4 | 0.95 | 3.37 | 0.94 | 0.26 | 0.99 | 22.90 | 0.73 | 7.06 | 0.99 | 0.61 | 0.51 |
H5 | 0.99 | 5.01 | 0.89 | 0.21 | 0.99 | 33.64 | 0.93 | 49.65 | 0.99 | 1.10 | 1.06 |
H6 | 0.92 | 2.14 | 0.93 | 0.11 | 0.97 | 20.01 | 0.97 | 2.45 | 0.95 | 0.82 | 0.88 |
Formulation | ALG Concentration (w/v%) | HPMC Concentration (w/v%) | ALG:POS Ratio |
---|---|---|---|
A1 | 0.5 | - | - |
A2 | 1 | - | - |
A3 | 1.5 | - | - |
F1 | 0.5 | - | 1:0.5 |
F2 | 0.5 | - | 1:1 |
F3 | 1 | - | 1:0.5 |
F4 | 1 | - | 1:1 |
F5 | 1.5 | - | 1:0.5 |
F6 | 1.5 | - | 1:1 |
H1 | 1 | 1 | - |
H2 | 1 | 3 | - |
H3 | 1 | 5 | - |
H4 | 1 | 1 | 1:1 |
H5 | 1 | 3 | 1:1 |
H6 | 1 | 5 | 1:1 |
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Kruk, K.; Szekalska, M.; Basa, A.; Winnicka, K. The Impact of Hypromellose on Pharmaceutical Properties of Alginate Microparticles as Novel Drug Carriers for Posaconazole. Int. J. Mol. Sci. 2023, 24, 10793. https://doi.org/10.3390/ijms241310793
Kruk K, Szekalska M, Basa A, Winnicka K. The Impact of Hypromellose on Pharmaceutical Properties of Alginate Microparticles as Novel Drug Carriers for Posaconazole. International Journal of Molecular Sciences. 2023; 24(13):10793. https://doi.org/10.3390/ijms241310793
Chicago/Turabian StyleKruk, Katarzyna, Marta Szekalska, Anna Basa, and Katarzyna Winnicka. 2023. "The Impact of Hypromellose on Pharmaceutical Properties of Alginate Microparticles as Novel Drug Carriers for Posaconazole" International Journal of Molecular Sciences 24, no. 13: 10793. https://doi.org/10.3390/ijms241310793