Enhancement of Anti-Inflammatory Activity of Optimized Niosomal Colchicine Loaded into Jojoba Oil-Based Emulgel Using Response Surface Methodology
Abstract
:1. Introduction
2. Results and Discussion
2.1. Entrapment Efficiency
2.2. Vesicular Size and Size Distribution (PDI)
2.3. Stability Study
2.4. Experimental Design
2.4.1. Fitting the Model
2.4.2. Statistical Analysis of the Design
2.5. Effect of Independent Variables on Viscosity (R1)
2.6. Effect of Independent Variables on In Vitro Release Study (R2)
2.7. Optimizing the Investigated Variables
2.8. Characterization of Optimized Topical Formulations
2.9. Assessment of In Vitro Drug Release Studies
2.10. Release Kinetic Mechanism
2.11. Anti-Inflammatory Testing; Carrageenan-Induced Rat Paw Edema Test
3. Conclusions
4. Materials and Methods
4.1. Materials
4.2. Preparation of Colchicine Loaded Noisome
4.3. Entrapment Efficiency
4.4. Vesicular Size and Size Distribution
4.5. Stability Study
4.6. Preparation of Colchicine Niosomal Emulgel
4.7. Experimental Design Using BBD
4.8. Characterization
4.8.1. Physical Inspection
4.8.2. Measurement of pH
4.8.3. Viscosity
4.8.4. Spreadability
4.9. Assessment of In Vitro Drug Release Studies
4.10. Release Kinetic Mechanism
4.11. Animal
4.12. Anti-Inflammatory Testing
Carrageenan-Induced Rat Paw Edema Test
- Group I: control group that did not receive any treatment.
- Group II: treated orally with colchicine solution (1 mg/kg).
- Group III: treated with niosomal gel with no drug (placebo I).
- Group IV: treated with niosomal emulgel with no drug (placebo II).
- Group V: treated with colchicine niosomal gel.
- Group VI: treated with colchicine niosomal emulgel (1 mg/kg) [53].
4.13. Statistical Analysis
Author Contributions
Funding
Institutional Review Board Statement
Informed Consent Statement
Data Availability Statement
Acknowledgments
Conflicts of Interest
References
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Formula | Independent Variables | Dependent Response | |||
---|---|---|---|---|---|
X1 (g) | X2 (g) | X3 (g) | R1 (cP) | R2 (%) | |
F1 | 1 | 1 | 1 | 4772 ± 123 | 49.5 ± 4.0 |
F2 | 1.5 | 1 | 0.8 | 5302 ± 188 | 42.8 ± 2.6 |
F3 | 1.5 | 0.5 | 0.8 | 5645 ± 167 | 39.2 ± 3.9 |
F4 | 1 | 0.5 | 1 | 4553 ± 219 | 50.8 ± 3.1 |
F5 | 1.5 | 1 | 1.2 | 6952 ± 169 | 28.2 ± 1.2 |
F6 | 1.5 | 0.75 | 1 | 6428 ± 179 | 29.4 ± 2.7 |
F7 | 1.5 | 0.5 | 1.2 | 6655 ± 171 | 29.5 ± 3.5 |
F8 | 1 | 0.75 | 0.8 | 4265 ± 184 | 55.1 ± 3.6 |
F9 | 2 | 1 | 1 | 9592 ± 202 | 22.3 ± 2.5 |
F10 | 1.5 | 0.75 | 1 | 5909 ± 246 | 33.6 ± 3.1 |
F11 | 1.5 | 0.75 | 1 | 6125 ± 177 | 34.2 ± 3.8 |
F12 | 2 | 0.75 | 1.2 | 9834 ± 210 | 21.5 ± 2.7 |
F13 | 1.5 | 0.75 | 1 | 6396 ± 268 | 31.9 ± 2.9 |
F14 | 2 | 0.5 | 1 | 8316 ± 176 | 25.2 ± 2.1 |
F15 | 1 | 0.75 | 1.2 | 4991 ± 184 | 47.2 ± 3.4 |
F16 | 2 | 0.75 | 0.8 | 7832 ± 219 | 26.1 ± 2.3 |
F17 | 1.5 | 0.75 | 1 | 6290 ± 237 | 32.7 ± 3.4 |
Source | R1 | R2 | ||
---|---|---|---|---|
F-Value | p-Value | F-Value | p-Value | |
Model | 67.64 | <0.0001 * | 35.53 | <0.0001 * |
X1 | 520.34 | <0.0001 * | 272.19 | <0.0001 * |
X2 | 3.78 | 0.0928 | 0.0850 | 0.7790 |
X3 | 52.31 | 0.0002 * | 31.90 | 0.0008 * |
X1X2 | 4.03 | 0.0848 | 0.1206 | 0.7386 |
X2X3 | 5.87 | 0.0459 * | 0.5130 | 0.4970 |
X3X1 | 1.48 | 0.2638 | 1.13 | 0.3229 |
X12 | 20.80 | 0.0026 * | 10.11 | 0.0155 * |
X22 | 0.0027 | 0.9600 | 0.8254 | 0.3938 |
X32 | 0.4326 | 0.5317 | 1.89 | 0.2112 |
Lack of Fit | 2.18 | 0.2333 | 2.20 | 0.2304 |
R2 analysis | ||||
R² | 0.9886 | 0.9786 | ||
Adjusted R² | 0.9740 | 0.9510 | ||
Predicted R2 | 0.8805 | 0.7739 | ||
Adequate Precision | 27.6989 | 20.4175 | ||
Model | ||||
Remark | Quadratic | Quadratic |
Response | Predicted Values | Experimental Values |
---|---|---|
R1 (cP) | 4187.4 ± 263.4 | 4598 ± 229.1 |
R2 (%) | 55.53 ± 2.34 | 52.4 ± 3.0 |
Properties | Colchicine Niosomal Gel | Colchicine Niosomal Emulgel |
---|---|---|
Visual inspection | Smooth and homogenous | Smooth and homogenous |
pH | 6.58 ± 0.28 | 6.73 ± 0.25 |
Viscosity (cP) | 2578.3 ± 214.2 | 4598 ± 229.1 * |
Spreadability (mm) | 44.0 ± 1.6 | 38.3 ± 1.7 * |
Formulation | Zero Order Kinetic (r2) | First Order Kinetic (r2) | Higuchi Kinetic (r2) | Korsmeyer-Peppas Kinetic (r2) |
---|---|---|---|---|
Colchicine solution | 0.9370 | 0.8110 | 0.9744 | 0.9341 |
Colchicine niosome | 0.8954 | 0.6800 | 0.9724 | 0.9276 |
Colchicine niosomal gel | 0.9394 | 0.8119 | 0.9867 | 0.9837 |
Colchicine niosomal emulgel | 0.9814 | 0.9051 | 0.9856 | 0.9780 |
Independent Variable | Symbol | Level of Variation | ||
---|---|---|---|---|
Lowest (−1) | Central (0) | Highest (1) | ||
Oil concentration (g) | X1 | 1.0 | 1.5 | 2.0 |
Surfactant concentration (g) | X2 | 0.5 | 0.75 | 1.0 |
Gelling agent concentration (g) | X3 | 0.8 | 1.0 | 1.2 |
Dependent Variable | Symbol | Constraints | ||
Viscosity (cP) | R1 | Minimize | ||
In vitro release (%) | R2 | Maximize |
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Elsewedy, H.S.; Younis, N.S.; Shehata, T.M.; Mohamed, M.E.; Soliman, W.E. Enhancement of Anti-Inflammatory Activity of Optimized Niosomal Colchicine Loaded into Jojoba Oil-Based Emulgel Using Response Surface Methodology. Gels 2022, 8, 16. https://doi.org/10.3390/gels8010016
Elsewedy HS, Younis NS, Shehata TM, Mohamed ME, Soliman WE. Enhancement of Anti-Inflammatory Activity of Optimized Niosomal Colchicine Loaded into Jojoba Oil-Based Emulgel Using Response Surface Methodology. Gels. 2022; 8(1):16. https://doi.org/10.3390/gels8010016
Chicago/Turabian StyleElsewedy, Heba S., Nancy S. Younis, Tamer M. Shehata, Maged E. Mohamed, and Wafaa E. Soliman. 2022. "Enhancement of Anti-Inflammatory Activity of Optimized Niosomal Colchicine Loaded into Jojoba Oil-Based Emulgel Using Response Surface Methodology" Gels 8, no. 1: 16. https://doi.org/10.3390/gels8010016