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

Formulation and Evaluation of Celastrol-Loaded Liposomes

1,†
,
2,†
,
1
,
1
,
1
,
1
,
3
 and
1,*
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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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.
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 (CC BY 3.0).
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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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