萘普生微乳经皮给药制剂的研究

Investigation of microemulsion system for transdermal drugdelivery of naproxen

目的:用聚山梨酯-80、肉豆蔻酸异丙酯(IPM)、水和2种助表面活性剂乙醇、丙二醇制备萘普生微乳,并对其进行体外经皮渗透性能考察。方法:用光散射粒度仪测定微乳的粒径,电子透射电镜观察微乳的形态。用药物渗透扩散仪测定萘普生微乳的透皮速率,高效液相色谱法测定萘普生含量。结果:所制萘普生微乳符合微乳的基本特性,且在贮存条件下稳定。萘普生微乳的透皮行为符合零级释放动力学规律;载药量增大,微乳的透皮能力加快。以乙醇为助表面活性剂时,微乳的稳态渗透速率均高于丙二醇。结论:微乳能克服口服给药所引起的毒副作用,有望成为萘普生的新型透皮给药制剂。

Objective：To prepare naproxen microemulsion using Tween-80, IPM, water and two kind cosurfactants alcohol,propylene glycol and investigate its in vitro transdermal delivery ability. Methods：The mean droplet sizes of naproxen microemulsion were measured via dynamic light scattering （DLS） on a Zeta sizer,their micro-structures were observed by transmission electron microscope （TEM）. Naproxen microemulsion diffusion studies were performed via excised rabbit skin using a drug diffusion apparatus. The contents of naproxen were measured by HPLC. Results：All the tested microemulsions accorded with the characterization of microemulsion,which were stable under stock condition. The permeation of naproxen microemulsion accorded with the Fick＇s first diffusion law. With the increase of the content of drug loaded in microemulsion,the permeability of microemulsion increased. The steady-state permeation rates of naproxen using alcohol as cosurfactant were higher than propylene glycol. Conclusion ：The results indicated that the system of naproxen microemulsion can solve the drawback caused by oral administration,which may be a promising vehicle for the transdermal delivery of naproxen.