非洛地平-硬脂酸固体脂质纳米粒的制备及其体外透皮吸收研究

Study on preparation and skin permeation of solid lipid nanoparticles containing felodipine

目的:以固体脂质纳米粒为载体,通过透皮给药达到提高非洛地平透皮吸收及缓释长效的目的。方法:采用溶剂挥发-超声法制备非洛地平固体脂质纳米粒水分散体,以大鼠皮肤为渗透屏障对非洛地平固体脂质纳米粒的经皮渗透进行研究。结果:非洛地平-硬脂酸固体脂质纳米粒为类球形实体粒子,平均粒径范围在50～150 nm,包封率大于85%,载药量大于7%,药物体外释放符合一级动力学过程,体外经皮渗透速率显著高于空白对照组。结论:非洛地平固体脂质纳米粒处方设计合理,制备工艺可靠,以纳米粒作为透皮给药载体具有广阔的发展前景。

Objective： To develop a new transdermal drug delivery system（ solid lipid nanoparticles） for felodipine to improve its effect. Methods： Solid lipid nanoparticles were prepared by solvent-dispersion technique and were treated further by sonication. The release rate and permeation rate of felodipine were studied through excised rat skin in vitro. Results ： Solid lipid nanoparticles containing felodipine were spherelike. The particle size was 50 - 150 nm;the drug entrapped efficiency was higher than 85% ;the drug loading was not less than 7%. The release of felodipine from solid lipid nanoparticles followed the first grade model kinetics and the permeation rate of felodipine was remarkably higher in vitro than placebo. Conclusion ： The formulation of solid lipid nanoparticles containing felodipine is reasonable. Solid lipid nanoparticles might he a suitable system for transdermal drug delivery.