葡萄糖酸亚铁固体脂质纳米粒的制备工艺研究

Study on Preparation Technique of Ferrous Gluconate-Loaded Solid Lipid Nanoparticles

[目的]探索葡萄糖酸亚铁固体脂质纳米粒的制备方法。[方法]采用两步W/O/W乳化方式制备葡萄糖酸亚铁固体脂质纳米粒(SLN)。以包埋率为指标,研究内外相、油水相体积比,卵磷脂浓度对SLN包埋率的影响。[结果]试验确定当内相中水相与油相的体积比为0.2,外水相与内相乳状液的体积比为5∶1,卵磷脂浓度为5%时,SLN的包埋率取得最大值,为52.48%。在内水相引入海藻酸钠(1∶2,W/W)的结果表明,SLN的包埋率增大,为59.03%,粒径、Zeta电位和多分散系数发生变化。体外释放试验表明,SLN能起到保护葡萄糖酸亚铁经受胃酸环境的作用,并在模拟肠液中表现为突释的释放效果。[结论]固体脂质纳米粒对葡萄糖酸亚铁有较好的保护及释放效果,可为无机铁补充剂的生产提供新的技术手段。

[Objective] The aim was to explore preparation method of ferrous gluconate-loaded solid lipid nanoparticles. [ Method] The fer-rous gluconate solid lipid nanoparticles （ SLN） was prepared by W/O/W double emulsion techniques. The influences of volume ratio of outer/inner phase, aqueous/oil phase of internal phase and concentration of lecithin applied as the surfactant on the entrapment efficiency of SLN were investigated. [Result] The maximal entrapment efficiency, 52. 48%, was obtained under the circumstances of 0. 2 as the aqueous/oil phase of internal phase, 5∶1 as the volume ratio of outer/ inner phase, and 5% as concentration of lecithin. The addition of sodium alginate with weight ratio of 1∶2 to ferrous gluconate posed a positively impact on the entrapment efficiency, which was 59. 03% and affected the size, Zeta potential and polydispersion index as well. The in vitro release profile showed that SLN could keep integrity in simulated gastric fluid and went through a burst release in simulated intestinal fluid. [ Conclusion] SLN could protect the drug from disintegration and release in the active site and be a new method to produce inorganic iron salts supplementation.