Journal
MOLECULES
Volume 16, Issue 9, Pages 7880-7892Publisher
MDPI AG
DOI: 10.3390/molecules16097880
Keywords
celastrol; liposomes; rat intestine perfusion model; ethanol-injection method
Funding
- Traditional Chinese Medicine for Public Interest Research from Ministry of Finance of China [200707008]
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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.
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