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
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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.
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.
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.