脂质纳米粒通过离体大鼠小肠吸收的研究

Research of Isolated Intestina Parva Absorption of Lipid Nanoparticles in Rats

关键词:  荧光素嫁接物  脂质纳米粒  包封率  外翻肠吸收实验

Key words:  ODA-FITC  lipid nanoparticles  drug encapsulation efficiency  drug absorption in intestina parva.

摘要:

目的 制备荧光标记的脂质纳米粒，测定其理化性质，探讨脂质纳米载体通过小肠吸收的情况及影响吸收的因素。方法 采用水性溶剂扩散法制备荧光标记脂质纳米粒，以微粒粒度及表面电位仪测定粒径和表面电位，荧光分光光度法测定包封率，以大鼠外翻肠模型考察不同肠段及脂质纳米粒处方因素对小肠吸收的影响。结果 制备得到的荧光标记脂质纳米粒粒径约为150~300 nm，带负电，荧光素嫁接物(ODA-FITC)包封率均高于95%，固体脂质纳米粒小肠不同部位吸收不一，十二指肠段吸收量最大，空肠次之，回肠最少。油酸和卵磷脂能够改善脂质纳米粒的小肠吸收。结论 用水性溶剂扩散法易于制备高ODA-FITC包封率的脂质纳米粒，通过调整脂质纳米粒处方，可以得到理想的小肠吸收的脂质纳米载体。

Abstract:

OBJECTIVE To prepare fluorescein-labeled lipid nanoparticles, determine the physical and chemical properties of the nanoparticles and investigate the effect factors of the absorption in intestina parva. METHODS The solid lipid　nanoparticles(SLN) and nanostructured lipid carriers(NLC) were prepared by aquosity solvent diffusion method, the sizes and zeta potentials of the nanoparticles were measured by light scattering and electrophoretic mobility, the drug encapsulation efficiencies were determined by SPF. The absorption of SLN and NLC in intestina parva was investigated with different lipid concentration and different prescription. RESULTS The diameters of FITC-labeled lipid nanoparticles prepared was about 150-300 nm, with negatively charged. The encapsulation efficiencies of ODA-FITC were higher than 95%. The absorption studies showed that the largest absorption amount of SLN was obtained in duodenal segment, followed by jejunum, and ileum at least. The absorption studies of lipid nanoparticles with different formulation showed that oleinic acid and lecithin help the absorption. CONCLUSION The nano-sized SLN and NLC loading ODA-FITC with relative higher drug encapsulation efficiency could be prepared by using aquosity solvent diffusion method, and higher drug absorption efficiency could be achieved by improving the preparation formula.