目的 考察天麻苷元的透皮特性与皮肤刺激性,为其经皮给药制剂的开发提供依据。方法 选取离体大鼠皮肤,采用改良Franz扩散池法对天麻苷元的透皮性能进行评价,并进一步考察常用溶剂、促透剂以及透皮微粒载体对其透皮性的影响。此外,选择家兔为动物模型,评价天麻苷元溶液剂与凝胶剂的皮肤刺激性。结果 天麻苷元较易透皮,经大鼠腹部皮肤的渗透速率常数(Js)可达134.1μg/(cm2.h),24 h透过量约为3 mg/cm2。30%乙醇对天麻苷元兼具增溶与促透作用,是较理想的溶剂。常用促透剂氮酮、松节油、冰片以及透皮微粒载体微乳与醇质体对天麻苷元透皮性能的改善作用并不显著。家兔皮肤刺激性试验结果表明天麻苷元溶液剂与凝胶剂均无明显的皮肤刺激性。结论 天麻苷元具有良好的透皮性能,且无皮肤刺激性,适合开发成经皮给药制剂,应用于中枢神经系统疾病的治疗。

Objective To investigate percutaneous permeability and skin irritation of gastrodigenin so as to provide the basis on the development of transdermal drug delivery formulations. Methods The modified Franz diffusion cell method and the excised rat skin were used to evaluate the percutaneous permeability of gastrodigenin. The effects of various common-used solvents, transdermal enhancers, and particle carriers on the permeability of gastrodigenin were studied. The rabbit skin irritation test was used to evaluate the safety of gastrodigenin solutions and their gels. Results Gastrodigenin was easy to permeate rat abdominal skin. The penetration rate constant (Js) was 134.1 μg/(cm2·h), and transit dose accumulated in 24 h was 3 mg/cm2. The solubility and permeability of gastrodigenin could be enhanced by 30% EtOH, so it was an ideal solvent for gastrodigenin. Improvement effects of the transdermal enhancers (Azone, turpentine, and borneol) and the transdermal particle carriers (microemulsion and ethosomes) were not significant. The skin irritation test results indicated that neither gastrodigenin soultions nor their gels exerted irritative effects to the rabbit skin. Conclusion Gastrodigenin has good percutaneous permeability without skin irritation, so it is suitable for the transdermal drug delivery in the treatment of central nervous system diseases.

国家自然科学基金资助项目(30902009)