Key Laboratory of Delivery Systems of Chinese Meteria Medica, Jiangsu Provincial Academy of Chinese Medicine, Nanjing 210028, Jiangsu, China.
Molecules. 2011 Sep 13;16(9):7880-92. doi: 10.3390/molecules16097880.
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.
本研究的主要目的是评估脂作为口服药物递送系统时，雷公藤红素这种难溶于水的药物的肠道吸收和抗肿瘤效果。采用乙醇注入法制备脂质体。由磷脂、胆固醇和吐温-80 组成的优化脂质体配方可实现 98.06 ± 0.94%的有利包封效率。通过激光粒度分析仪测定均匀且稳定的粒径为 89.6 ± 7.3nm 和 zeta 电位为-(87.7 ± 5.8)mV。随后，四部位灌流大鼠肠模型显示，与游离药物相比，雷公藤红素脂质体在四个肠段均具有更高的有效渗透（p < 0.05）。此外，雷公藤红素脂质体还可以抑制 C57BL/6 小鼠的肿瘤生长。这些结果表明，脂质体可以成为雷公藤红素的一种有前途的经口载体。
