Tomoda Keishiro, Ohkoshi Takumi, Nakajima Takehisa, Makino Kimiko
Faculty of Pharmaceutical Sciences, Tokyo University of Science, 2641 Yamazaki Noda, Chiba 278-8510, Japan.
Colloids Surf B Biointerfaces. 2008 Jun 15;64(1):70-6. doi: 10.1016/j.colsurfb.2008.01.016. Epub 2008 Jan 31.
Nanoparticles are expected to be applicable to inhalation as carrier but there exist disadvantages because of their size. Their deposition dose to the lung will be small. To overcome this problem and utilize nanoparticles for inhalation, we have prepared nanocomposite particles as drug carriers targeting lungs. The nanocomposite particles are prepared as drug-loaded nanoparticles-additive complex to reach deep in the lungs and to be decomposed into nanoparticles when they deposit into lung. In this study, we examined the effect of preparation condition--inlet temperature, size of primary nanoparticles and weight ratio of primary nanoparticles--on the property of nanocomposite particles. When the size of primary nanoparticles was 400 nm and inlet temperature was 90 degrees C, only the nanocomposite particles containing between 45 and 55% of primary nanoparticles could be decomposed into nanoparticles in water. On the other hand, when the inlet temperature was 80 degrees C, nanocomposite particles were decomposed into nanoparticles independent of the weight ratio of primary nanoparticles. Also, the aerodynamic diameter of the nanocomposite particles was between 1.5 and 2.5 microm, independent of the weight ratio of primary nanoparticles. When the size of primary nanoparticles was 200 nm and inlet temperature was 70 degrees C, nanocomposite particles were decomposed into nanoparticles independent of the weight ratio of primary nanoparticles. Also, the aerodynamic diameters of them were almost 2.0 microm independent of the weight ratio of primary nanoparticles. When the nanocomposite particles containing nanoparticles with the size of 200 nm are prepared at 80 degrees C, no decomposition into nanoparticles was observed in water. Fine particle values, FPF, of the nanocomposite particles were not affected by the weight ratio of primary nanoparticles when they were prepared at optimum inlet temperature.
纳米颗粒有望作为载体应用于吸入治疗，但由于其尺寸存在一些缺点。它们在肺部的沉积剂量会很小。为了克服这个问题并将纳米颗粒用于吸入治疗，我们制备了作为肺部靶向药物载体的纳米复合颗粒。纳米复合颗粒被制备成载药纳米颗粒 - 添加剂复合物，以便深入肺部，并在沉积到肺部时分解成纳米颗粒。在本研究中，我们研究了制备条件——入口温度、初级纳米颗粒的尺寸和初级纳米颗粒的重量比——对纳米复合颗粒性质的影响。当初级纳米颗粒的尺寸为400 nm且入口温度为90℃时，只有含有45%至55%初级纳米颗粒的纳米复合颗粒能在水中分解成纳米颗粒。另一方面，当入口温度为80℃时，纳米复合颗粒会分解成纳米颗粒，与初级纳米颗粒的重量比无关。此外，纳米复合颗粒的空气动力学直径在1.5至2.5微米之间，与初级纳米颗粒的重量比无关。当初级纳米颗粒的尺寸为200 nm且入口温度为70℃时，纳米复合颗粒会分解成纳米颗粒，与初级纳米颗粒的重量比无关。而且，它们的空气动力学直径几乎为2.0微米，与初级纳米颗粒的重量比无关。当在80℃制备含有尺寸为200 nm纳米颗粒的纳米复合颗粒时，在水中未观察到分解成纳米颗粒的现象。当纳米复合颗粒在最佳入口温度下制备时，其细颗粒值（FPF）不受初级纳米颗粒重量比的影响。
