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.