苦参碱固体脂质纳米粒的制备

Preparation of Solid Lipid Nanoparticles Loading Matrine

目的:优选苦参碱固体脂质纳米粒的处方工艺并考察其外观性状、粒径分布。方法:采用超声分散法制备苦参碱固体脂质纳米粒,以苦参碱包封率为指标,通过正交试验考察苦参碱-硬脂酸质量比、硬脂酸-大豆卵磷脂质量比、泊洛沙姆质量浓度、油-水相体积比对处方工艺的影响。结果:优选的处方工艺为硬脂酸-大豆卵磷脂(1∶1),苦参碱-硬脂酸(1∶6),泊洛沙姆质量浓度12 g·L-1,油-水相体积比(1∶5)。制备的苦参碱固体脂质纳米粒为乳状溶液,呈乳白色,晃动后可能会产生白色絮状物,有光泽,平均包封率82.8%,平均载药量5.5%。该纳米粒呈不规则类球形或椭球形,分布较均匀,平均粒径155 nm。结论:优选的处方工艺稳定可靠,具有很大的应用前景。

Objective： To optimize formulation technology of matrine solid lipid nanoparticles and investigate its appearance and particle size distribution. Method： Matrine solid lipid nanoparticles were prepared ultrasonic dispersion method, with entrapment efficiency of matrine as index, orthogonal test was adopted to investigate effects of ratio of matrine-stearic acid, ratio of stearic acid-soybean lecithin, poloxamer concentration and oil-water phase ratio on formulation technology. Result： Optimum formulation technology was as following： matrine-stearic acid （ 1 ： 6）, stearic acid-soybean lecithin （ 1 ： 1 ）, poloxamer concentration 12 g ·L^-1, oil phase- water phase （1：5）. Prepared matrine solid lipid nanoparticles was emulsion solution with luster, showed ivory white, it may produce white flocculus after shaking, average encapsulation efficiency was 82.8% , average drug loading was 5.5%. These nanoparticles were irregular spherical or ellipsoidal with uniform distribution, average particle size was 155 nm. Conclusion： Optimzed formulation technology was feasible and stable with good application prospects.