Hadinoto Kunn, Zhu Kewu, Tan Reginald B H
A STAR Institute of Chemical and Engineering Sciences, Singapore 627833, Singapore.
Int J Pharm. 2007 Aug 16;341(1-2):195-206. doi: 10.1016/j.ijpharm.2007.03.035. Epub 2007 Mar 30.
The aim of the present work is to examine the viability of using large hollow nanoparticulate aggregates as the therapeutic carrier particles in dry powder inhaler delivery of nanoparticulate drugs. The large hollow carrier particles are manufactured by spray drying of nanoparticulate suspensions of biocompatible acrylic polymer with loaded drugs. The size and concentration of the nanoparticles, as well as the phospholipids inclusion, have been known to influence the resulting morphology (i.e. size and degree of hollowness) of the spray-dried carrier particles. The effects of the resulting morphology of the carrier particles on the drug release rate are therefore investigated by varying the above three variables. The results of the drug release study are presented using aspirin and salbutamol sulfate as the model drugs with a varying degree of water solubility. The results indicate that the drug release rate is governed by the degree of hollowness of the carrier particles, and to a lesser extent by the nanoparticles size, as a result of the variation in the drug loading capacity of nanoparticles of different sizes.
本研究的目的是考察在纳米颗粒药物的干粉吸入器给药中,使用大型中空纳米颗粒聚集体作为治疗载体颗粒的可行性。大型中空载体颗粒是通过对负载药物的生物相容性丙烯酸聚合物纳米颗粒悬浮液进行喷雾干燥制备的。已知纳米颗粒的尺寸和浓度以及磷脂的加入会影响喷雾干燥载体颗粒的最终形态(即尺寸和中空程度)。因此,通过改变上述三个变量来研究载体颗粒最终形态对药物释放速率的影响。使用阿司匹林和硫酸沙丁胺醇作为具有不同水溶性程度的模型药物,呈现药物释放研究的结果。结果表明,由于不同尺寸纳米颗粒的载药量不同,药物释放速率受载体颗粒中空程度的控制,在较小程度上受纳米颗粒尺寸的影响。