Design and Comparative Evaluation of Vancomycin HCl-Loaded Rosin-Based In Situ Forming Gel and Microparticles
Abstract
:1. Introduction
2. Materials and Methods
2.1. Materials
2.2. Preparation of the Formulations
2.2.1. Preparation of In-Situ Forming Gel (ISG)
2.2.2. Preparation of In Situ Forming Microparticles (ISM)
2.3. Evaluation of the ISG and ISM Systems
2.3.1. Appearance and Phase Separation of ISM Emulsion
2.3.2. pH Measurement
2.3.3. Viscosity and Rheology Behavior
2.3.4. Injectability Test
2.3.5. Adhesion Properties
2.3.6. In-Vitro Gel and Microparticle Transformation
2.3.7. In-Vitro Drug Release
2.3.8. Topography
2.3.9. Antimicrobial Activities
2.4. Statistical Analysis
3. Results and Discussion
3.1. Appearance and Phase Separation
3.2. pH Measurement
3.3. Viscosity
3.4. Injectability Test
3.5. Adhesion Properties
3.6. In Vitro Transformation
3.7. Size of In Situ Forming Microparticles (ISM)
3.8. Drug Release
3.9. Surface Topography
3.10. Antimicrobial Activities
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 | Vancomycin HCl (V) | Rosin (R) | DMSO | Olive Oil | GMS |
---|---|---|---|---|---|
20RV | 1.0 | 20 | 79.0 | - | - |
30RV | 1.0 | 30 | 69.0 | - | - |
40RV | 1.0 | 40 | 59.0 | - | - |
50RV | 1.0 | 50 | 49.0 | - | - |
60RV | 1.0 | 60 | 39.0 | - | - |
20RV ISM | 0.5 | 10 | 39.5 | 42.5 | 7.5 |
30RV ISM | 0.5 | 15 | 34.5 | 42.5 | 7.5 |
40RV ISM | 0.5 | 20 | 29.5 | 42.5 | 7.5 |
50RV ISM | 0.5 | 25 | 24.5 | 42.5 | 7.5 |
60RV ISM | 0.5 | 30 | 19.5 | 42.5 | 7.5 |
V in DMSO | 1.0 | - | 99.0 | - | - |
Formula | pH | Viscosity (cPs) | Size (µm) | |
---|---|---|---|---|
Emulsion | Microparticle | |||
DMSO | 11.20 ± 0.17 | 3.53 ± 0.08 | - | - |
20RV | 5.89 ± 0.05 | 7.49 ± 0.60 | - | - |
30RV | 5.56 ± 0.06 | 16.57 ± 0.84 | - | - |
40RV | 5.17 ± 0.09 | 30.64 ± 1.02 | - | - |
50RV | 5.15 ± 0.08 | 59.98 ± 1.77 | - | - |
60RV | 5.02 ± 0.14 | 112.45 ± 0.98 | - | - |
40RV ISM | 6.48 ± 0.06 | 38.62 ± 1.33 | 98.48 ± 16.11 * | 78.63 ± 12.97 * |
50RV ISM | 6.46 ± 0.01 | 61.11 ± 1.67 | 125.55 ± 4.75 * | 93.81 ± 10.53 * |
60RV ISM | 5.93 ± 0.02 | 108.35 ± 2.45 | 137.80 ± 16.84 * | 118.32 ± 15.61 * |
Formula | Injectability Force (N) | Injectability AUC (N.s) | Adhesion Properties | |||
---|---|---|---|---|---|---|
Maximum Force (N) | Adhesion Force (N) | Remaining Force (N) | Elastic Properties | |||
20RV | 1.10 ± 0.01 | 20.59 ± 0.42 | 3.786 ± 0.172 | −0.026 ± 0.010 | 1.364 ± 0.244 | 0.36 |
30RV | 2.73 ± 0.12 | 37.89 ± 2.24 | 3.579 ± 1.170 | −0.002 ± 0.001 | 2.123 ± 0.773 | 0.59 |
40RV | 3.10 ± 0.04 | 56.19 ± 0.57 | 0.856 ± 0.065 * | −0.050 ± 0.001 * | 0.057 ± 0.026 | 0.07 |
50RV | 7.98 ± 0.17 | 140.48 ± 5.29 | 0.737 ± 0.084 * | −0.051 ± 0.001 * | 0.052 ± 0.003 | 0.07 |
60RV | - | - | 0.420 ± 0.043 * | −0.053 ± 0.002 * | 0.026 ± 0.005 | 0.06 |
40RV ISM | 5.36 ± 0.02 | 92.24 ± 2.58 | 1.227 ± 0.329 * | −3.4658 ± 0.517 * | 1.128 ± 0.350 | 0.91 |
50RV ISM | 8.31 ± 0.73 | 135.32 ± 3.75 | 0.133 ± 0.077 * | −2.010 ± 0.525 * | 0.003 ± 0.002 | 0.03 |
60RV ISM | 16.83 ± 1.14 | 272.89 ± 17.69 | 0.060 ± 0.016 * | −0.192 ± 0.019 * | 0.005 ± 0.001 | 0.08 |
Formula (% w/w) | Zero Order | First Order | Higuchi’s | POWER LAW | Release Mechanism | |||||
---|---|---|---|---|---|---|---|---|---|---|
cd | msc | cd | msc | cd | msc | cd | msc | N ± S.D. | ||
V in DMSO | 0.7061 | 0.9135 | 0.9850 | 3.9777 | 0.8905 | 1.9892 | 0.9089 | 2.0846 | 0.4035 ± 0.075 | Fickian |
20RV | 0.8602 | 1.7970 | 0.9899 | 4.4740 | 0.9437 | 2.7598 | 0.9495 | 2.8144 | 0.5763 ± 0.075 | Non-Fickian |
30RV | 0.8991 | 2.1226 | 0.9947 | 5.1257 | 0.9615 | 3.1398 | 0.9727 | 3.4319 | 0.5947 ± 0.075 | Non-Fickian |
40RV | 0.8960 | 2.0923 | 0.9816 | 3.8771 | 0.9615 | 3.1384 | 0.9714 | 3.3842 | 0.5894 ± 0.075 | Non-Fickian |
50RV | 0.8860 | 2.0004 | 0.9235 | 2.4528 | 0.9772 | 3.6630 | 0.9787 | 3.6774 | 0.5408 ± 0.075 | Non-Fickian |
60RV | 0.8710 | 1.8772 | 0.8678 | 1.9058 | 0.9749 | 3.5668 | 0.9742 | 3.4882 | 0.5231 ± 0.075 | Non-Fickian |
40RV ISM | 0.8083 | 1.4811 | 0.8660 | 1.8920 | 0.9572 | 3.0330 | 0.9556 | 2.9443 | 0.4762 ± 0.075 | Fickian |
50RV ISM | 0.7828 | 1.3560 | 0.7715 | 1.3585 | 0.9484 | 2.8475 | 0.9539 | 2.9061 | 0.4415 ± 0.075 | Fickian |
60RV ISM | 0.7383 | 1.1698 | 0.6725 | 0.9987 | 0.9245 | 2.4661 | 0.9413 | 2.6643 | 0.4131 ± 0.075 | Fickian |
Formula | Inhibition Zone (mm) | |||
---|---|---|---|---|
S. aureus | S. mutans | P. gingivalis | E. coli | |
NSS | - | - | - | - |
DMSO | 12.67 ± 0.58 | 11.00 ± 0.00 a | 13.67 ± 1.15 d | 12.00 ± 0.00 |
VD | 23.67 ± 0.58 | 22.67 ± 0.58 a,b,c | 23.00 ± 0.00 d,e,f | 13.67 ± 0.58 |
20RV | 23.33 ± 0.58 | 22.00 ± 0.00 b | 18.33 ± 0.58 e | 12.33 ± 0.58 |
30RV | 22.67 ± 1.15 | 18.67 ± 0.58 b | 18.00 ± 0.00 e | 11.33 ± 0.58 |
40RV | 14.67 ± 0.58 | 14.33 ± 0.58 b | 14.67 ± 0.58 e | - |
50RV | 11.67 ± 0.58 | 11.67 ± 0.58 b | 12.67 ± 0.58 e | - |
60RV | 11.00 ± 0.00 | 11.00 ± 0.00 b | 11.67 ± 0.58 e | - |
40RV ISM | 10.00 ± 0.00 | 15.00 ± 0.00 c | 13.67 ± 0.58 f | - |
50RV ISM | - | 13.67 ± 0.58 c | 12.00 ± 0.00 f | - |
60RV ISM | - | 12.67 ± 0.58 c | 11.67 ± 0.58 f | - |
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Chuenbarn, T.; Sirirak, J.; Tuntarawongsa, S.; Okonogi, S.; Phaechamud, T. Design and Comparative Evaluation of Vancomycin HCl-Loaded Rosin-Based In Situ Forming Gel and Microparticles. Gels 2022, 8, 231. https://doi.org/10.3390/gels8040231
Chuenbarn T, Sirirak J, Tuntarawongsa S, Okonogi S, Phaechamud T. Design and Comparative Evaluation of Vancomycin HCl-Loaded Rosin-Based In Situ Forming Gel and Microparticles. Gels. 2022; 8(4):231. https://doi.org/10.3390/gels8040231
Chicago/Turabian StyleChuenbarn, Tiraniti, Jitnapa Sirirak, Sarun Tuntarawongsa, Siriporn Okonogi, and Thawatchai Phaechamud. 2022. "Design and Comparative Evaluation of Vancomycin HCl-Loaded Rosin-Based In Situ Forming Gel and Microparticles" Gels 8, no. 4: 231. https://doi.org/10.3390/gels8040231