伊曲康唑白蛋白纳米粒混悬液的制备与体外评价

Preparation and in vitro evaluation of itraconazole albumin nanoparticle suspensions

目的制备伊曲康唑白蛋白纳米粒混悬液,并优化其处方和制备工艺,同时对所优化的白蛋白纳米粒混悬液进行评价。方法采用单因素实验法筛选超高压微射流技术制备伊曲康唑白蛋白纳米粒混悬液的处方和制备工艺,考察了白蛋白纳米粒混悬液的外观形态、粒径分布等理化性质以及体外释药情况。结果制备的伊曲康唑白蛋白纳米粒混悬液呈圆整的球形或类球形分布,平均粒径为(108.1±32.8)nm,PdI为0.205,Zeta电位为(-47.6±1.7)mV;伊曲康唑白蛋白纳米粒在0.5%聚山梨酯-80磷酸盐缓冲液(pH7.4)中24h累积释放73.5%。结论采用超高压微射流技术制备伊曲康唑白蛋白纳米粒混悬液,工艺简便可行,重现性好,有望工业化生产。

Objective To prepare the itraconazole albumin nanoparticle suspensions, optimize the formulation and preparation process, and evaluate the physicochemical characteristics of albumin nanoparticle suspensions. Methods The single factor experimental method was used to study the formulation composition and preparation process of itraconazole albumin nanoparticle suspensions by the ultra-high pressure microfluidization technology. The physicochemical properties of itraconazole albumin nanoparticle suspensions were studied, including morphology and particle size distribution. In vitro release characteristics of itraconazole from albumin nanoparticle suspensions were investigated in pH7.4 phosphate buffered saline. Results Itraconazole albumin nanoparticle suspensions were homogeneous small spheres as seen in the transmission electron microscopy. The average particle diameter was （108.1±32.8）nm, the polydispersity index was 0.205, and the Zeta potential was （-47.6±1.7）mV. In 0.5% Polysorbate-80 phosphate buffered saline （pH7.4）, the in vitro cumulative release of itraconazole albumin nanoparticle suspensions reached up to 73.5% within 24h. Conclusion The preparation technology of itraconazole albumin nanopartiele suspensions by ultra-high pressure microfluidization technology is simple and feasible. This preparation technology can be used in industrial production.