Université Paris-Sud, Institut Galien Paris Sud, UMR CNRS 8612, Faculté de Pharmacie, 5, Rue J.B. Clément, 92296 Châtenay-Malabry cedex, France.
Int J Pharm. 2013 Oct 1;454(2):678-85. doi: 10.1016/j.ijpharm.2013.06.062. Epub 2013 Jul 5.
The scale-up of oil-containing polyamide nanocapsules produced by simultaneous interfacial polycondensation and solvent diffusion was successfully achieved. Up to 1,500 mL were produced by using a Y-shaped mixer device. The sizes of nanocapsules containing olive oil were modulated from 646 to 211 nm by changing process parameters without modification of the formulation composition. All the results of nanocapsule diameters (dsc) expressed as a function of the Reynolds number (Re) showed the existence of a typical power-law relationship. It was demonstrated that the high turbulences created upon nanocapsule formation are the most important parameter allowing to nanocapsule size to be controlled without modifying the formulation composition. Finally, the power-law relationship was used to predict the size of nanocapsules composed of polyamide or polyester and loaded with Parsol(®) MCX. The physico-chemical properties of both polyamide and polyester nanocapsules at the laboratory scale were compared to the ones obtained at the pilot scale. The encapsulation efficiency was higher than 98% in both types of nanocapsules at the laboratory and the pilot scales. The in vitro releases of Parsol(®) MCX from polyester nanocapsules were reproducible at both scales. This is the first time such a power-law was described for the preparation of nanocapsules by interfacial polycondensation and solvent diffusion.
通过界面缩聚和溶剂扩散同时进行,成功实现了含油聚酰胺纳米胶囊的放大生产。使用 Y 型混合器设备,可生产多达 1500 毫升的纳米胶囊。通过改变工艺参数,无需改变配方组成,就可以将含有橄榄油的纳米胶囊的尺寸从 646nm 调节到 211nm。所有纳米胶囊直径(dsc)的结果(表示为雷诺数(Re)的函数)都表明存在典型的幂律关系。结果表明,在纳米胶囊形成过程中产生的高湍流是最重要的参数,可在不改变配方组成的情况下控制纳米胶囊的尺寸。最后,使用幂律关系来预测由聚酰胺或聚酯组成并负载 Parsol(®)MCX 的纳米胶囊的尺寸。在实验室规模和中试规模上比较了聚酰胺和聚酯纳米胶囊的物理化学性质。在实验室和中试规模上,两种类型的纳米胶囊的包封效率均高于 98%。聚酯纳米胶囊中 Parsol(®)MCX 的体外释放在两个规模上均具有重现性。这是首次通过界面缩聚和溶剂扩散制备纳米胶囊时描述这种幂律关系。