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Molecules 2011, 16(9), 7880-7892; doi:10.3390/molecules16097880

Formulation and Evaluation of Celastrol-Loaded Liposomes

1 Key Laboratory of Delivery Systems of Chinese Meteria Medica, Jiangsu Provincial Academy of Chinese Medicine, Nanjing 210028, Jiangsu, China 2 Department of Traditional Chinese Medicine, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China 3 National Center of Drug Screening, China Pharmaceutical University, Nanjing 210038, Jiangsu, China These two authors contributed equally to this work.
* Author to whom correspondence should be addressed.
Received: 21 July 2011 / Revised: 5 September 2011 / Accepted: 5 September 2011 / Published: 13 September 2011
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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.
Keywords: celastrol; liposomes; rat intestine perfusion model; ethanol-injection method celastrol; liposomes; rat intestine perfusion model; ethanol-injection method
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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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.

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