模拟高密度脂蛋白脂核的洛伐他汀纳米结构脂质载体的制备

The Preparation of Lovastatin Structure Lipid Carrier of Simulating High Density Liporotein Core

目的:选择洛伐他汀作为模型药物,以高密度脂蛋白的脂核成分作为纳米结构脂质载体的脂质材料,制备了洛伐他汀纳米结构脂质载体。方法:文章建立了洛伐他汀含量测定的高效液相色谱法;并且建立了LT-NLC包封率的测定方法-微柱离心法;采用溶剂扩散法制备载有洛伐他汀的纳米结构脂质载体。通过固定其它因素改变某一因素的单因素实验设计,在此基础上确定了最优处方和工艺。洛伐他汀纳米结构脂质载体的物理化学性质通过粒径、Zeta电位、形态、包封率来表征。结果:制得的洛伐他汀纳米结构脂质载体透射电镜下观察形态为固体球形或类球体,平均粒径为(13.8±2.2)nm,Zeta电位为(-29.3±0.2)m V,包封率EE%为(96.3±0.7)%。结论:溶剂挥发法制备的洛伐他汀纳米结构脂质载体粒径较小且分布均匀,包封率良好,稳定性可靠。纳米脂质载体提高了洛伐他汀的水溶性,拓展了其应用范围。

Objective： To prepare lovastatin nanostructured lipid carriers by chosing Lovastatin as model drug and utilizing High density lipoprotein lipid core components as the lipid material material of Nanostructured lopid carriers. Method： The article established a High performance liquid chromatography（HPLC） method for determination of the content of lovastatin and the technique of Micro column centrifugation to mensurate the Encapsulation efficiency（EE） of LT-NLC. Preparing the Nanostructured lipid carrier containing lovastatin by Solvent diffusion method. Deciding the optimal formulation and technology based on the single factor experimental design of fixing all factors except one factor. Showing the physicochemical properties of Lovastatin nanostructured lipid carriers by the data of particle size, zeta potential, shape and encapsulation efficiency. Result： The form of the prepared Lovastatin nanostructured lipid carriers, observed under the Transmission electron microscope, is spherical or quasi spherical solid. Average particle size were13.8±2.2 nm; Zeta potential were-29.3±0.2 m V; Encapsulation efficiency were 96.3±0.7 %. Conclusion： The lovastatin nanostructured lipid carrier prepared by Solvent evaporatin method has the advantages of smaller particle size, well distribution, good encapsulation efficiency, reliable stability, improved water-solubility of lovastatin and wider application range