Comparative Study of TPGS and Soluplus Polymeric Micelles Embedded in Poloxamer 407 In Situ Gels for Intranasal Administration
Abstract
:1. Introduction
2. Results and Discussion
2.1. Finding the Optimal Polymer Concentrations via Phase Solubility Study
2.2. Micelle Size, Micelle Size Distribution, and Zeta Potential Measurements
2.3. Determination of Encapsulation Efficiency and Thermodynamic Solubility
2.4. Finding the Optimal In Situ Gel-Forming Polymer Concentration via the Determination of Gelation Time and Temperature
2.5. Characterization of the In Situ Gel Formulations
2.6. In Vitro Mucoadhesion Study
2.7. In Vitro Drug Release Study
2.8. In Vitro Nasal Passive Diffusion Study
3. Conclusions
4. Materials and Methods
4.1. Materials
4.2. Quantitative Analysis of Dexamethasone via Liquid Chromatography
4.3. Quantitative Analysis of Tobramycin via Liquid Chromatography
4.4. Phase Solubility Study of Dexamethasone
4.5. Formulation of Dexamethasone-Loaded Polymeric Micelles
4.6. Characterization of Polymeric Micelles
4.6.1. Determination of Micelle Size, Size Distribution, and Zeta Potential
4.6.2. Determination of Encapsulation Efficiency
4.6.3. Determination of Thermodynamic Solubility
4.7. Incorporation of Polymeric Micelles and Tobramycin into In Situ Gelling Systems
4.8. Characterization of the In Situ Gelling Formulations
4.8.1. Determination of Gelling Time and Temperature of the In Situ Gelling Formulations
4.8.2. Determination of pH, Clarity, and Drug Content of the In Situ Gelling Formulations
4.9. In Vitro Nasal Applicability Investigations
4.9.1. In Vitro Mucoadhesion Study
4.9.2. In Vitro Drug Release Study
4.9.3. In Vitro Nasal Passive Diffusion Study
4.10. Statistical Analysis
Author Contributions
Funding
Institutional Review Board Statement
Informed Consent Statement
Data Availability Statement
Acknowledgments
Conflicts of Interest
References
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DT_SP | DT_TPGS | DT_SP/TPGS | |
---|---|---|---|
DH (nm) | 72.41 ± 6.32 | 21.43 ± 7.26 | 92.30 ± 3.4 |
PdI | 0.119 ± 0.004 | 0.169 ± 0.011 | 0.249 ± 0.027 |
ζ (mV) | −18.4 ± 4.1 | −13.4 ± 2.3 | −21.2 ± 2.8 |
DXM | DT_SP | DT_TPGS | DT_SP/TPGS | |
---|---|---|---|---|
EEDXM (%) | - | 89.13 ± 2.70 | 83.05 ± 3.3 | 93.77 ± 4.1 |
SDXM,25°C (µg/mL) | 124.13 ± 4.51 | 1432.21 ± 28.79 | 896.25 ± 32.88 | 1658.02 ± 22.49 |
DT_SP (G) (13%) | DT_TPGS (G) (14%) | DT_SP/TPGS (G) (13%) | |
---|---|---|---|
pHsol | 6.58 ± 0.23 | 6.67 ± 0.13 | 6.71 ± 0.15 |
pHgel | 6.83 ± 0.11 | 6.91 ± 0.20 | 7.02 ± 0.09 |
Clarity | Transparent | Transparent | Transparent |
Drug content (DXM) (%) | 92.13 ± 4.12 | 91.39 ± 3.55 | 97.35 ± 1.06 |
Drug content (TB) (%) | 94.24 ± 2.31 | 92.11 ± 0.87 | 95.45 ± 2.15 |
DT_SP (13%) | DT_TPGS (14%) | DT_SP/TPGS (13%) | ||
---|---|---|---|---|
DXM | ||||
J (µg/cm2 × h) | 24.5 ± 2.90 | 137.76 ± 17.72 | 171.3 ± 13.21 | 184.6 ± 25.09 |
Kp (cm/h) | 0.0245 | 0.1378 | 0.1713 | 0.1846 |
Papp (×10−4 cm/s) | 1.23 | 6.89 | 8.57 | 9.23 |
TB | ||||
J (µg/cm2 × h) | 141.4 ± 9.6 | 341.3 ± 29.9 | 381.9 ± 28.9 | 395.8 ± 21.9 |
Kp (cm/h) | 0.0236 | 0.0569 | 0.0634 | 0.0659 |
Papp (×10−4 cm/s) | 1.18 | 2.84 | 3.18 | 3.30 |
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Sipos, B.; Földes, F.; Budai-Szűcs, M.; Katona, G.; Csóka, I. Comparative Study of TPGS and Soluplus Polymeric Micelles Embedded in Poloxamer 407 In Situ Gels for Intranasal Administration. Gels 2024, 10, 521. https://doi.org/10.3390/gels10080521
Sipos B, Földes F, Budai-Szűcs M, Katona G, Csóka I. Comparative Study of TPGS and Soluplus Polymeric Micelles Embedded in Poloxamer 407 In Situ Gels for Intranasal Administration. Gels. 2024; 10(8):521. https://doi.org/10.3390/gels10080521
Chicago/Turabian StyleSipos, Bence, Frézia Földes, Mária Budai-Szűcs, Gábor Katona, and Ildikó Csóka. 2024. "Comparative Study of TPGS and Soluplus Polymeric Micelles Embedded in Poloxamer 407 In Situ Gels for Intranasal Administration" Gels 10, no. 8: 521. https://doi.org/10.3390/gels10080521