布洛芬磁性固体脂质纳米粒的制备

背景：布洛芬因溶解度和溶血问题，目前仍无注射给药剂型上市。 目的：将自制的磁流体载入固体脂质纳米粒中，制备布洛芬磁性固体脂质纳米粒。 方法：以包封率为指标，用正交设计确定布洛芬固体脂质纳米粒的最优处方。以共沉淀法制备Fe3O4磁流体作为磁性材料，采用乳化分散-超声法，按照最优处方制备布洛芬磁性固体脂质纳米粒。观察其表面形态、粒径大小、分布和Zeta电位、饱和磁化强度、包封率及体外释放特征。 结果与结论：通过正交实验得最优处方为布洛芬0.05 g、F-68 0.2 g、吐温80 0.05 g、卵磷脂0.1 g、单硬脂酸甘油酯0.05 g、磁流体2.5 mL。用该工艺和处方制备的布洛芬磁性固体脂质纳米粒粒子呈均匀球形；平均粒径、zeta电位为(122±16) nm和(-13.3±6.94) mV；药物包封率和Fe3O4铁包封率分别为84.15%和83.19%；布洛芬在给定介质中36 h释放较完全，符合制剂学性质要求。

Preparation of magnetic solid lipid nanoparticles loaded with ibuprofen

BACKGROUND: There is no injected drug dosage form listing because of solubility and hemolysis problem of ibuprofen. OBJECTIVE: To put ferrofluid into magnetic solid lipid nanoparticles (MSLN) so as to prepare ibuprofen-MSLN. METHODS: The optimal formulation was obtained by orthogonal experiment design, based on the encapsulate efficiency (EE%). Fe3O4 magnetic fluid was perpared with co-precipitation method as magnetic materials. Ibuprofen-MSLN was finally acquired with the method of emulsification dispersion-ultrasound. The appearance, the size distribution, Zeta potential, saturation magnetization, EE% and in vitro release characteristics were observed. RESULTS AND CONCLUSION: The optimal formulation was ibuprofen 0.05 g, F-68 0.2 g, Tween 80 0.05 g, lecithin 0.1 g, glyceryl monostearate 0.05 g, ferrofluid 2.5 mL. The ibuprofen-MSLN was uniformly spherical; the average size and Zeta potential were (122±16) nm and (-13.3±6.94) mV, respectively; the EE% of ibuprofen and ferroso-ferric oxide were 84.15% and 83.19%, respectivley; the release of ibuprofen-MSLN was complete in the given media in 36 hours. Ibuprofen-MSLN prepeared by this condition and technology is consistent with the demand of nano-preparations.