Topical Delivery of Coenzyme Q10-Loaded Microemulsion for Skin Regeneration
Abstract
:1. Introduction
2. Materials and Methods
2.1. Materials
2.2. Selection of Oils, Surfactants, and Co-Surfactant Mixtures for Microemulsions
2.3. Quantitative Analysis of CoQ10
2.4. Construction of Pseudo-Ternary Phase Diagram
2.5. Preparation of CoQ10-Loaded o/w Microemulsion
2.6. Characterization of CoQ10-Loaded o/w Microemulsion
2.6.1. Stability Assessment
2.6.2. Entrapment Efficacy of CoQ10 in o/w Microemulsion
2.6.3. Measurement of Droplet Size and Zeta Potential Value
2.7. In Vitro Cell Experiment
2.7.1. Preparation of Cells
2.7.2. Cell Proliferation Assay
2.7.3. Wound Healing Scratch Assay
2.8. Permeation Experiment
2.8.1. In Vitro Membrane Permeation Experiment
2.8.2. In Vitro Skin Permeation Experiment
2.9. Statistics
3. Results
3.1. Screening of CoQ10 in Oils, Surfactants, and Co-Surfactants
3.2. Phase Behavior
3.3. Optimization of CoQ10-Loaded o/w Microemulsion
3.4. Physicochemical characterization of CoQ10-loaded o/w microemulsion
3.5. Permeation Experiments
3.6. Effect of CoQ10 on Skin Regeneration
4. Discussion
5. Conclusions
Supplementary Materials
Author Contributions
Funding
Conflicts of Interest
References
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Substance | Solubility (mg/mL) | Substance | Solubility (mg/mL) |
---|---|---|---|
Isopropyl myristate (IPM) | 209.88 ± 7.42 | Tween 80 | 21.88 ± 12.06 |
Oleic acid (OA) | 87.36 ± 34.59 | Cremophor EL® | 33.10 ± 11.71 |
IPM:OA (3:1) | 143.50 ± 18.97 | Labarasol | 26.53 ± 12.88 |
IPM:OA (2:1) | 137.53 ± 14.17 | PG | 2.13 ± 2.13 |
Labrafil M1944 | 86.80 ± 12.98 | Transcutol® HP | 9.35 ± 1.96 |
Cottonseed oil | 107.12 ± 23.16 | PEG-400 | 0.24 ± 0.21 |
Formulation | S/CoS ratio | Composition of ME w/w % * | Drug (%) | Dilution Test | Thermodynamic Stability Test | |||||
---|---|---|---|---|---|---|---|---|---|---|
Oil | S/CoS | Water | Centrifugation | Heating-Cooling | Freeze-Thaw | Decision | ||||
F1 | 2:1 | 5.06 | 35.44 | 59.5 | 0.5 | Clear | √ | √ | √ | Pass |
F2 | 5.06 | 35.44 | 59.5 | 1 | Clear | √ | √ | √ | Pass | |
F3 | 6.56 | 32.79 | 60.65 | 0.5 | Clear | √ | × | - | Failed | |
F4 | 6.56 | 32.79 | 60.65 | 1 | Clear | √ | × | - | Failed | |
F5 | 5.8 | 40.58 | 53.62 | 0.5 | Clear | √ | √ | △ | Failed | |
F6 | 5.8 | 40.58 | 53.62 | 1 | Clear | √ | √ | △ | Failed | |
F7 | 5 | 45 | 50 | 0.5 | Clear | √ | √ | × | Failed | |
F8 | 5 | 45 | 50 | 1 | Clear | √ | √ | × | Failed | |
F9 | 3:1 | 5.06 | 35.44 | 59.5 | 0.5 | Clear | √ | √ | √ | Pass |
F10 | 5.06 | 35.44 | 59.5 | 1 | Clear | √ | √ | √ | Pass | |
F11 | 6.56 | 32.79 | 60.65 | 0.5 | Clear | √ | △ | × | Failed | |
F12 | 6.56 | 32.79 | 60.65 | 1 | Clear | √ | △ | × | Failed | |
F13 | 5.8 | 40.58 | 53.62 | 0.5 | Clear | √ | △ | △ | Failed | |
F14 | 5.8 | 40.58 | 53.62 | 1 | Clear | √ | △ | △ | Failed | |
F15 | 5 | 45 | 50 | 0.5 | Clear | √ | × | - | Failed | |
F16 | 5 | 45 | 50 | 1 | Clear | √ | × | - | Failed | |
F17 | 4:1 | 5.06 | 35.44 | 59.5 | 0.5 | Clear | √ | √ | √ | Pass |
F18 | 5.06 | 35.44 | 59.5 | 1 | Clear | √ | √ | √ | Pass | |
F19 | 6.56 | 32.79 | 60.65 | 0.5 | Clear | √ | △ | × | Failed | |
F20 | 6.56 | 32.79 | 60.65 | 1 | Clear | √ | △ | × | Failed | |
F21 | 5.8 | 40.58 | 53.62 | 0.5 | Turbid | - | - | - | Failed | |
F22 | 5.8 | 40.58 | 53.62 | 1 | Turbid | - | - | - | Failed | |
F23 | 5 | 45 | 50 | 0.5 | Turbid | - | - | - | Failed | |
F24 | 5 | 45 | 50 | 1 | Turbid | - | - | - | Failed |
Formulation | S/CoS Ratio | Composition of ME w/w % * | Drug (%) | Physicochemical Properties | ||||||
---|---|---|---|---|---|---|---|---|---|---|
Oil | S/CoS | Water | Droplet Size (nm) | PDI | Zeta Potential (mV) | Drug Content(%) | pH | |||
F2 | 2:1 | 5.06 | 35.44 | 59.5 | 1 | 16.89 ± 0.050 | 0.040 ± 0.012 | −13.1 ± 1.32 | 102.01 ± 0.128 | 7.12 ± 0.064 |
F10 | 3:1 | 5.06 | 35.44 | 59.5 | 1 | 16.72 ± 0.055 | 0.058 ± 0.007 | −14.7 ± 1.23 | 101.7 ± 0.41 | 7.01 ± 0.021 |
F18 | 4:1 | 5.06 | 35.44 | 59.5 | 1 | 16.65 ± 0.172 | 0.080 ± 0.006 | −11.8 ± 1.01 | 101.62 ± 0.4 | 7.00 ± 0.042 |
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Ryu, K.-A.; Park, P.J.; Kim, S.-B.; Bin, B.-H.; Jang, D.-J.; Kim, S.T. Topical Delivery of Coenzyme Q10-Loaded Microemulsion for Skin Regeneration. Pharmaceutics 2020, 12, 332. https://doi.org/10.3390/pharmaceutics12040332
Ryu K-A, Park PJ, Kim S-B, Bin B-H, Jang D-J, Kim ST. Topical Delivery of Coenzyme Q10-Loaded Microemulsion for Skin Regeneration. Pharmaceutics. 2020; 12(4):332. https://doi.org/10.3390/pharmaceutics12040332
Chicago/Turabian StyleRyu, Kyeong-A, Phil June Park, Seong-Bo Kim, Bum-Ho Bin, Dong-Jin Jang, and Sung Tae Kim. 2020. "Topical Delivery of Coenzyme Q10-Loaded Microemulsion for Skin Regeneration" Pharmaceutics 12, no. 4: 332. https://doi.org/10.3390/pharmaceutics12040332