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

Formulation and Evaluation of Celastrol-Loaded Liposomes

1,†
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 and 1,*
Received: 21 July 2011; in revised form: 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 which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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MDPI and ACS Style

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.

AMA Style

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.

Chicago/Turabian Style

Song, Jie; Shi, Feng; Zhang, Zhenhai; Zhu, Fenxia; Xue, Jing; Tan, Xiaobin; Zhang, Luyong; Jia, Xiaobin. 2011. "Formulation and Evaluation of Celastrol-Loaded Liposomes." Molecules 16, no. 9: 7880-7892.



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