伊曲康唑柔性脂质体的制备及体外性能研究

Preparationand Transdermal Study in Vitro of Itraconazole Elastic Liposomes

目的:制备伊曲康唑柔性脂质体,并考察其体外透皮性能。方法:以大豆卵磷脂为成膜材料和聚山梨酯80为边缘活化剂,薄膜分散法制备伊曲康唑柔性脂质体,考察粒径、Zeta电位、包封率、载药量及稳定性。采用Franz扩散池,以大鼠皮肤为透皮屏障,考察伊曲康唑柔性脂质体及其溶液的体外透皮性能差异。结果:伊曲康唑柔性脂质体平均粒径为(222.5±15.34)nm,多分散系数(PDI)为(0.226±0.09),Zeta电位为(-5.09±1.52)mV,平均包封率为(83.80±2.18)%。体外透皮实验表明,伊曲康唑脂质体中伊曲康唑12 h的累积渗透量(Q12)是伊曲康唑溶液的2.21倍;渗透速率(Jss)是伊曲康唑溶液的2.20倍;皮肤滞留量(Qs)是伊曲康唑溶液的6.2倍。结论:伊曲康唑柔性脂质体可显著提高伊曲康唑的体外累积透皮量和皮肤滞留量,有望成为新型局部给药制剂。

Objective:To study the preparation and transdermal absorption in vitro of itraconazole elastic liposomes.Methods:Lipid and Span 80 were used as film-forming materials.Itraconazole elastic liposomes were commonly prepared by a thin-film dispersion method using a rotary evaporation technique.The particle size,Zeta potential,encapsulation efficiency,drug loading and stability of itraconazole elastic liposomes were determined.The skin penetration test was performed by the Franz diffusion cell method to evaluate the transdermal effecacy.Results:The average particle size,polydispersity index(PDI),Zeta potential and encapsulation efficiency were(222.5±15.34)nm,(0.226±0.09),(-5.09±1.52)mV and(83.80±2.18)%,respectively.The cumulative transdermal amount in 12 h(Q12)of itraconazole elastic liposomes was 2.21-fold higher than that of the drug solution.Comparative permeation flux(Jss)studies revealed an enhanced permeation,which was 2.20-fold higher than that of the drug solution.The skin retention(Qs)was 6.2-fold higher than that of the drug solution.Conclusion:Itraconazole elastic liposomes can remarkably improve the cumulative transdermal amount and the skin retention,which provides reference for the new dosage form for the topical use of itraconazole.