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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150~300nm,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。
OBJECTIVE: To prepare fluorescent labeled lipid nanoparticles for determination of their physico-chemical properties, to investigate the absorption of lipid nanocarriers through the small intestine and the factors affecting their absorption. Methods Fluorescent labeled lipid nanoparticles were prepared by aqueous solvent diffusion method. Particle size and surface potential were measured by particle size and surface potentiometry. Encapsulation efficiency was measured by fluorescence spectrophotometry. Effects of Prescriptions of Nanoparticles on Intestinal Absorption. Results The size of fluorescent labeled lipid nanoparticles prepared was about 150-300 nm with negative charges. The entrapment efficiency of ODA-FITC was higher than 95%. The absorption of solid lipid nanoparticles in different parts of the small intestine was different , The largest absorption of the duodenum segment, followed by the jejunum, ileum at least. Oleic acid and lecithin can improve intestinal absorption of lipid nanoparticles. CONCLUSION: Lipid nanoparticles with high ODA-FITC entrapment efficiency can be easily prepared by aqueous solvent diffusion method. Liposomal nanocarriers absorbed by small intestine can be obtained by adjusting the formulation of lipid nanoparticles.