Hadinoto Kunn, Phanapavudhikul Ponpan, Kewu Zhu, Tan Reginald B H
A*STAR Institute of Chemical and Engineering Sciences, Singapore 627833, Singapore.
Int J Pharm. 2007 Mar 21;333(1-2):187-98. doi: 10.1016/j.ijpharm.2006.10.009. Epub 2006 Oct 10.
The present work details the effects of incorporating phospholipids, a major component of lung surfactants, in the formulation of large hollow nanoparticulate aggregates, which are specifically designed to serve as potential carrier particles in inhaled delivery of nanoparticulate drugs. The large hollow aerosol particles (d(g) approximately 10 microm), whose shells are composed of nanoparticulate aggregates, are manufactured via the spray drying of nanoparticulate suspensions under a predetermined operating condition. Polyacrylate and silica nanoparticles of various sizes (20-170 nm), without loaded drugs, are employed as the model nanoparticles. The effects of increasing the phospholipids concentration in the presence of the nanoparticles, and vice versa, on the degree of hollowness and morphology of the spray-dried particles are investigated. Varying the phospholipids concentration in the presence of a constant amount of nanoparticles is found to influence the degree of hollowness, without significantly affecting the particle size distribution and respirable fine particle fraction, of the aerosol particles. The effects of increasing the phospholipids concentration on the degree of hollowness of the spray-dried particles are found to depend on the size and chemical nature of the nanoparticles.
本研究详细阐述了将肺表面活性剂的主要成分磷脂掺入大型中空纳米颗粒聚集体制剂中的效果，这些聚集体是专门设计用作纳米颗粒药物吸入给药的潜在载体颗粒。大型中空气溶胶颗粒（d(g)约为10微米），其外壳由纳米颗粒聚集体组成，是在预定操作条件下通过纳米颗粒悬浮液的喷雾干燥制备的。使用各种尺寸（20 - 170纳米）且未负载药物的聚丙烯酸酯和二氧化硅纳米颗粒作为模型纳米颗粒。研究了在纳米颗粒存在下增加磷脂浓度以及反之在磷脂存在下增加纳米颗粒浓度对喷雾干燥颗粒的中空度和形态的影响。发现在恒定数量的纳米颗粒存在下改变磷脂浓度会影响气溶胶颗粒的中空度，而不会显著影响颗粒大小分布和可吸入细颗粒分数。还发现增加磷脂浓度对喷雾干燥颗粒中空度的影响取决于纳米颗粒的尺寸和化学性质。
