载叶黄素白蛋白纳米粒口腔速溶膜的制备及评价

Preparation and evaluation of oral fast dissolving films containing lutein nanoparticles incorporated with bovine serum albumin

联合应用白蛋白纳米粒和口腔速溶膜技术,以期改善叶黄素的生物利用度并提高患者顺应性。采用反溶剂沉淀法制得叶黄素白蛋白纳米粒、溶剂浇铸法将其载入口腔速溶膜,并对所得速溶膜进行体内外评价。所得膜剂中粒子分散均匀,厚度36μm,耐折度为87次,30 s内迅速崩解。药物以无定形状态存在或高度分散在膜中。与口服溶液相比,SD大鼠舌上给予膜剂后的C_(max)提高了7.02倍,AUC_(0 h^24 h)增大了2.91倍。结果表明,载叶黄素白蛋白纳米粒口腔速溶膜综合了白蛋白纳米粒和口腔速溶膜的双重优点,吸收速度和程度显著提高,应用前景良好。

To improve the bioavailability of lutein and compliance of patients using albumin nanoparticles and oral fast dissolving films. Lutein-BSA nanoparticles were firstly prepared by anti-solvent precipitation method and then encapsulated into films by solvent casting method. The films were characterized on their physicochemical properties, in vitro release and in vivo pharmacokinetics. The films exhibited uniform thickness of 36 μm and folding endurance of 87 times, and disintegrated rapidly in 30 s. The drug in films showed faster release rate in vitro than raw lutein. Thermograms and diffractograms indicated lutein were highly dispersed in films. After administrated to SD rats, the C_（max） and AUC_（0 h^24 h） of films by tongue administration were 7.02 fold and 2.91 fold higher than that of raw lutein by oral administration, respectively. Oral fast dissolving films containing lutein-loaded BSA nanoparticles can be promising for enhanced bioavailability of lutein.