广藿香酮传递体体外透皮效能评价及传递体透皮机制研究

In vitro evaluation of transdermal penetration effectiveness of systemically applied pogostone transfersomes and its mechanism

目的评价广藿香酮传递体的体外透皮效能,并对传递体的透皮机制进行初步探究。方法采用薄膜分散法制备广藿香酮传递体,并对其进行物理表征;通过体外经皮渗透实验考察广藿香酮传递体的透皮效能,并基于透射电子显微法对传递体的透皮机制进行研究。结果广藿香酮传递体的透皮速率显著高于广藿香酮80%丙二醇溶液,传递体用于广藿香酮的经皮全身性给药,具有更大优势;传递体在角质层沿着亲水通道进行传递,且过程中可凭借形变与自我调节能力保持结构的完整性。结论传递体经皮给药系统的确能够改善广藿香酮的透皮吸收,本试验初步揭示了传递体透皮的形态学机制。

Objective To evaluate the transdermal penetration effectiveness of pogostone transfersomes and determine the penetration mechanism. Methods Pogostone transfersomes were prepared by film-ultrasonic dispersion method. Basic characterization parameters of transfersomes were checked for transfersomes. Invitro skin permeation studies were conducted. TEM was used to study the interaction between transfersomes and the skin. Results The drug flux rate across the skin of pogostone transfersomes was obviously higher than that of pogostone in 80% propylene glycol solution, which implied transfersomes had a greater advantage for transdermal systemic delivery of pogostone. Transfersomes were penetrated along the hydrophilic pathways in the stratum corneum, and their structure kept complete during the permeation process, owing to their self- regulation and deformation. Conclusion Skin penetration ofpogostone is enhanced by transfersome preparation. The morphological skin penetration mechanism of transfersomes is partly revealed by this experiment.