The Enhanced Inhibitory Effect of Different Antitumor Agents in Self-Microemulsifying Drug Delivery Systems on Human Cervical Cancer HeLa Cells
Abstract
:1. Introduction
2. Results
2.1. Formulation and Evaluation of Self-Micro-Emulsifying Drug Delivery Systems
Composition | API (mg) | Ratio of Surface Active Agents in SMEDDSs (Total Volume of Composition: 1 mL) | ||||||
---|---|---|---|---|---|---|---|---|
Kolliphor RH40 | Labrasol | Capryol 90 | Lauroglycol FCC | Transcutol HP | Isopropyl Myristate | |||
1 | 0.001–0.05 | Cisplatin | 2 | 2 | 1 | 0 | 2 | 1 |
0.1–5.00 | Ifosfamide | 2 | 2 | 1 | 0 | 2 | 1 | |
0.0005–0.05 | Bleomycin sulfate | 2 | 2 | 1 | 0 | 2 | 1 | |
2 | 0.001–0.05 | Cisplatin | 2 | 2 | 1 | 0 | 4 | 1 |
0.1–5.00 | Ifosfamide | 2 | 2 | 1 | 0 | 4 | 1 | |
0.0005–0.05 | Bleomycin sulfate | 2 | 2 | 1 | 0 | 4 | 1 | |
3 | 0.001–0.05 | Cisplatin | 2 | 2 | 1 | 0 | 6 | 1 |
0.1–5.00 | Ifosfamide | 2 | 2 | 1 | 0 | 6 | 1 | |
0.0005–0.05 | Bleomycin sulfate | 2 | 2 | 1 | 0 | 6 | 1 | |
4 | 0.001–0.05 | Cisplatin | 1 | 1 | 0 | 1 | 1 | 1 |
0.1–5.00 | Ifosfamide | 1 | 1 | 0 | 1 | 1 | 1 | |
0.0005–0.05 | Bleomycin sulfate | 1 | 1 | 0 | 1 | 1 | 1 | |
5 | 0.001–0.05 | Cisplatin | 1 | 1 | 0 | 1 | 2 | 1 |
0.1–5.00 | Ifosfamide | 1 | 1 | 0 | 1 | 2 | 1 | |
0.0005–0.05 | Bleomycin sulfate | 1 | 1 | 0 | 1 | 2 | 1 | |
6 | 0.001–0.05 | Cisplatin | 1 | 1 | 0 | 1 | 4 | 1 |
0.1–5.00 | Ifosfamide | 1 | 1 | 0 | 1 | 4 | 1 | |
0.0005–0.05 | Bleomycin sulfate | 1 | 1 | 0 | 1 | 4 | 1 |
2.2. Droplet Size and Zeta Potential Determination
2.3. Cell Viability Test of SMEDDS Ingredients
2.4. Evaluation of Inhibitory Effect of SMEDDS Containing Antitumor Agent
API(Bold/Compositions) | IC50 (μg/mL) | ±SD | IC50 (μg/mL) in Presence of TNF-α, IL-1-β | ±SD |
---|---|---|---|---|
Cisplatin | 16.68 | 0.10 | 25.96 | 0.56 |
Composition 1 | 9.63 | 0.11 | 27.88 | 0.21 |
Composition 2 | 4.81 | 0.21 | 8.69 | 1.00 |
Composition 3 | 2.82 | 0.15 | 5.84 | 0.45 |
Composition 4 | 11.03 | 0.96 | 9.00 | 0.01 |
Composition 5 | 4.26 | 0.85 | 32.70 | 0.21 |
Composition 6 | 5.35 | 0.32 | 14.29 | 041 |
Bleomycin sulfate | 4.21 | 0.11 | 5.69 | 0.11 |
Composition 1 | 3.84 | 0.15 | 4.37 | 0.19 |
Composition 2 | 3.99 | 0.50 | 6.70 | 0.32 |
Composition 3 | 0.61 | 0.012 | 0.82 | 0.01 |
Composition 4 | 4.71 | 0.12 | 6.81 | 0.01 |
Composition 5 | 5.12 | 0.33 | 7.56 | 0.02 |
Composition 6 | 4.93 | 0.22 | 6.33 | 0.01 |
Ifosfamide | 993.50 | 25.00 | 1936.02 | 5.40 |
Composition 1 | 521.70 | 20.40 | 641.10 | 4.21 |
Composition 2 | 247.30 | 35.60 | 479.00 | 4.52 |
Composition 3 | 148.50 | 1.00 | 191.10 | 3.66 |
Composition 4 | 607.30 | 10.90 | 823.20 | 0.99 |
Composition 5 | 802.41 | 30.55 | 873.14 | 0.99 |
Composition 6 | 1044.70 | 1.11 | 1098.70 | 1.90 |
BIP | 3.36 | 0.10 | 4.93 | 0.18 |
Composition 1 | 2.76 | 0.23 | 3.56 | 0.11 |
Composition 2 | 2.01 | 0.21 | 3.67 | 0.34 |
Composition 3 | 0.33 | 0.05 | 0.95 | 0.09 |
Composition 4 | 3.31 | 0.08 | 3.95 | 0.17 |
Composition 5 | 2.99 | 0.23 | 4.51 | 0.35 |
Composition 6 | 2.74 | 0.32 | 3.45 | 0.37 |
2.5. Evaluation of Inhibitory Effect of SMEDDS Containing Antitumor Agent in the Presence of Inflammatory Mediators
2.6. Discussion
3. Experimental Section
3.1. Materials
3.2. Methods
3.2.1. Formulation and Evaluation of Self-Micro-Emulsifying Drug Delivery Systems
3.2.2. Droplet Size and Zeta Potential Determination
3.2.3. Cell Culturing
3.2.4. In Vitro Cell Viability Assay
3.2.5. Inhibitory Effect of Different SMEDDS Containing Antitumor Agents
3.2.6. Inhibitory Effect of Different SMEDDS Containing Antitumor Agents in the Presence of Inflammatory Mediators
3.2.7. Statistical Analysis
4. Conclusions
Acknowledgements
Author Contributions
Conflicts of Interest
References
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Ujhelyi, Z.; Kalantari, A.; Vecsernyés, M.; Róka, E.; Fenyvesi, F.; Póka, R.; Kozma, B.; Bácskay, I. The Enhanced Inhibitory Effect of Different Antitumor Agents in Self-Microemulsifying Drug Delivery Systems on Human Cervical Cancer HeLa Cells. Molecules 2015, 20, 13226-13239. https://doi.org/10.3390/molecules200713226
Ujhelyi Z, Kalantari A, Vecsernyés M, Róka E, Fenyvesi F, Póka R, Kozma B, Bácskay I. The Enhanced Inhibitory Effect of Different Antitumor Agents in Self-Microemulsifying Drug Delivery Systems on Human Cervical Cancer HeLa Cells. Molecules. 2015; 20(7):13226-13239. https://doi.org/10.3390/molecules200713226
Chicago/Turabian StyleUjhelyi, Zoltán, Azin Kalantari, Miklós Vecsernyés, Eszter Róka, Ferenc Fenyvesi, Róbert Póka, Bence Kozma, and Ildikó Bácskay. 2015. "The Enhanced Inhibitory Effect of Different Antitumor Agents in Self-Microemulsifying Drug Delivery Systems on Human Cervical Cancer HeLa Cells" Molecules 20, no. 7: 13226-13239. https://doi.org/10.3390/molecules200713226