Formulation and Evaluation of Celastrol-Loaded Liposomes
Abstract
:1. Introduction
2. Results and Discussion
2.1. Preparation and Characteristic of Liposomal Celastrol
Surfactants | Tween-80 | P188 | PEG400 | SD |
---|---|---|---|---|
EE% | 94.67 ± 3.58 | 92.36 ± 3.84 | 76.35 ± 2.03 | 81.23 ± 2.47 |
Injection velocity (mL/min) | 0.1 | 0.5 | 1.0 | 2.0 |
---|---|---|---|---|
EE% | 90.81 ± 2.80 | 94.67 ± 3.58 | 94.26 ± 3.78 | 91.31 ± 2.96 |
Average Size (nm) | 71.31 ± 0.43 | 63.62 ± 0.44 | 61.53 ± 0.46 | 97.41 ± 0.71 |
Batch | Celastrol | Cholesterol | Tween-80 | Aqueous Phase Volume | EE |
---|---|---|---|---|---|
Weight | Weight | Concentration | |||
(mg) | (mg) | (mg/mL) a | (mL) | (% w/w) b | |
1 | 10 | 40 | 0 | 20 | 79.42 ± 2.45 |
2 | 10 | 80 | 0.5 | 30 | 98.98 ± 2.16 |
3 | 10 | 120 | 1.0 | 40 | 89.77 ± 2.43 |
4 | 10 | 160 | 2.0 | 50 | 80.62 ± 2.37 |
5 | 20 | 40 | 0.5 | 40 | 88.54 ± 2.32 |
6 | 20 | 80 | 0 | 50 | 85.35 ± 2.52 |
7 | 20 | 120 | 2.0 | 20 | 79.89 ± 2.61 |
8 | 20 | 160 | 1.5 | 30 | 85.71 ± 2.59 |
9 | 30 | 40 | 1.5 | 50 | 85.38 ± 2.78 |
10 | 30 | 80 | 2.0 | 40 | 93.55 ± 2.59 |
11 | 30 | 120 | 0 | 30 | 84.18 ± 2.45 |
12 | 30 | 160 | 1.0 | 20 | 87.13 ± 2.53 |
13 | 40 | 40 | 2.0 | 20 | 75.60 ± 2.19 |
14 | 40 | 80 | 1.5 | 30 | 95.57 ± 2.24 |
15 | 40 | 120 | 1.0 | 50 | 89.25 ± 2.53 |
16 | 40 | 160 | 0 | 40 | 80.82 ± 2.62 |
2.2. Intestinal Absorption Activity Comparison
Concentration (μM) | k (×10−3 s−1) | |||
---|---|---|---|---|
pH 5.5 | pH 6.5 | pH 7.4 | pH 8.0 | |
4 | 2.11 | 1.71 | 1.54 | 1.39 |
8.3 | 2.57 | 2.49 | 2.38 | 2.03 |
20 | 3.31 | 2.17 | 1.97 | 1.56 |
2.3. Celastrol-Loaded Liposomes Inhibited Tumor Growth
3. Experimental
3.1. Chemicals
3.2. Animals
3.3. Liposome Preparation by Ethanol Injection Method
3.4. Morphological Study by Transmission Electron Microscopy
3.5. Particle Size and Zeta-Potential Analysis of Liposomes
3.6. Determination of Encapsulation Efficiency
3.7. Animal Surgery
3.8. Four Site Single-Pass Rat Intestinal Perfusion Experiment
3.9. UPLC Analysis of Intestinal Perfusate
3.10. Perfusate Preparations and Stability Test of Celastrol in the Perfusate
3.11. Data Analysis
3.12. Effect of Celastrol-Loaded Liposomes on Tumor Growth in C57BL/6 Mice
3.13. Statistical Analysis
4. Conclusions
Acknowledgments
- Sample Availability: Samples of the compound celastrol are available from the authors.
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Song, J.; Shi, F.; Zhang, Z.; Zhu, F.; Xue, J.; Tan, X.; Zhang, L.; Jia, X. Formulation and Evaluation of Celastrol-Loaded Liposomes. Molecules 2011, 16, 7880-7892. https://doi.org/10.3390/molecules16097880
Song J, Shi F, Zhang Z, Zhu F, Xue J, Tan X, Zhang L, Jia X. Formulation and Evaluation of Celastrol-Loaded Liposomes. Molecules. 2011; 16(9):7880-7892. https://doi.org/10.3390/molecules16097880
Chicago/Turabian StyleSong, Jie, Feng Shi, Zhenhai Zhang, Fenxia Zhu, Jing Xue, Xiaobin Tan, Luyong Zhang, and Xiaobin Jia. 2011. "Formulation and Evaluation of Celastrol-Loaded Liposomes" Molecules 16, no. 9: 7880-7892. https://doi.org/10.3390/molecules16097880