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- Title
Formulation and Evaluation of Celastrol-Loaded Liposomes.
- Authors
Jie Song; Feng Shi; Zhenhai Zhang; Fenxia Zhu; Jing Xue; Xiaobin Tan; Luyong Zhang; Xiaobin Jia
- Abstract
The main purpose of this study was to evaluate the intestinal absorption and the antineoplastic effect of the poorly water-soluble drug celastrol when liposomes were used as oral drug delivery system. Liposomes were prepared by the ethanol-injection method. An optimized liposome formulation composed of phospholipid, cholesterol and Tween-80 resulted in favorable encapsulation efficiency at 98.06 ± 0.94%. Homogeneous and stable particle size of 89.6 ± 7.3 nm and zeta potential of -(87.7 ± 5.8) mV were determined by laser particle size analyzer. Subsequently, the four-site perfusion rat intestinal model revealed that celastrol-loaded liposomes had improved effective permeability compared to the free drug in four intestinal segments (p < 0.05). Moreover, celastrol-loaded liposomes could also inhibit the tumor growth in C57BL/6 mice. These results suggest that liposomes could be a promising perioral carrier for celastrol.
- Subjects
LIPOSOMES; INTESTINAL absorption; ANTINEOPLASTIC agents; ORAL medicine; DRUG delivery systems
- Publication
Molecules, 2011, Vol 16, Issue 9, p7880
- ISSN
1420-3049
- Publication type
Article
- DOI
10.3390/molecules16097880