负载氢醌的甘油-丙二醇二元醇质体的制备及体外经皮渗透研究

Preparation and in vitro transdermal permeation study of hydroquinoneloaded glycerol-propylene glycol binary ethosomes

目的:制备包载氢醌(hydroquinone,HQ)的甘油-丙二醇二元醇质体(hydroquinone-loaded glycerol-propylene glycol binary ethosomes,HBEs)并考察其体外透皮性能。方法:采用注入法制备HBEs,马尔文粒度仪测量其粒径和zeta电位,反渗透法考察HBEs的包封率。透皮试验仪研究HBEs的体外透皮性能,模型拟合法评估HBEs的透皮行为。结果:HBEs的粒径为(87.09±0.28)nm,电位为(-23.43±0.31)mV,包封率为(77.14±1.32)%。HBEs的24 h累积经皮渗透量和透皮速率常数分别是游离HQ的1.85倍和1.76倍。模型拟合结果显示HBEs的经皮扩散模型符合Higuchi方程,游离HQ溶液符合一级方程。结论:新型甘油-丙二醇二元醇质体HBEs能显著促进HQ的经皮渗透。

Objective:To prepare hydroquinone-loaded glycerol-propylene glycol binary ethosomes(HBEs),and to evaluate their transdermal properties in vitro.Methods:The injection method was used to prepare HBEs,A Malvern particle size analyzer was used to measure their particle size and zeta potential,and the reverse osmosis method was used to evaluate the encapsulation efficiency of HBEs.A transdermal tester was used to evaluate the in vitro transdermal permeation of HBEs,and the model fitting method was used to evaluate transdermal behavior.Results:The particle size,zeta potential,and encapsulation efficiency of HBEs were(87.09±0.28)nm,(-23.43±0.31)mV,and(77.14±1.32)%,respectively.The cumulative transdermal permeation amount within 24 hours and transdermal rate constant of HBEs were 1.85 and 1.76 times those of free hydroquinone,respectively.The model fitting results showed that the transdermal permeation model of HBEs and free hydroquinone followed the Higuchi equation and first-order equation,respectively.Conclusion:HBEs,as a new glycerol-propylene glycol binary ethosome,could significantly promote the transdermal penetration of hydroquinone.