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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.



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





Author: Jie Song 1,†, Feng Shi 2,†, Zhenhai Zhang 1, Fenxia Zhu 1, Jing Xue 1, Xiaobin Tan 1, Luyong Zhang 3 and Xiaobin Jia 1,*

Source: http://mdpi.com/



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