Abstract
Elastic vesicles of glycyrrhetic acid (GA) with lysine in the aqueous phase were prepared by the film-high pressure homogenization method. The influence of lysine on the formation of GA elastic vesicles was evaluated in this work. The lysine salt of GA was synthesized and entrapped in elastic vesicles as a control formulation. The particle size, zeta-potential, entrapment efficiency, phase transformation temperature, deformability of the elastic vesicles, and the permeation of GA through rat skin were investigated. By the incorporation of lysine into elastic vesicles the particle size decreased slightly and the phase transformation temperature decreased while the entrapment efficiency and deformability of the elastic vesicles increased obviously. The drug loading reached 1.5 mg·mL - 1 , which was 30 times higher than that of GA elastic vesicles without lysine. The drug loading and deformability of the elastic vesicles was remarkably higher than that obtained using the lysine salt. In addition, the cumulative amount of GA permeation through rat skin within 8 h and the residual amount in the skin were found to be 4.3 times and 9.2 times higher than that of the vesicles without lysine, which was higher than that of the elastic vesicles with the lysine salt of GA. These results indicate that lysine forms an ion associate with GA, which takes part in the formation of vesicle membranes and subsequently increases the membraneʹs fluidity. Such a high drug loading capability is a result of the synergistic effect between lysine and the elastic vesicles. (Article)
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