Department of Pharmacy, China Pharmaceutical University, Nanjing, PR China.
Drug Dev Ind Pharm. 2009 Sep;35(9):1059-65. doi: 10.1080/03639040902769628.
To study the preparation and application of pulmonary surfactant (PS) nanoparticles as absorption enhancers in insulin dry powder delivery. PS is a complex mixture of mainly phospholipids and proteins. The composition leads to a unique spreading effect of the surfactants as well as spontaneous nanoparticles formation, which may be favorable characteristics of pulmonary drug delivery systems.
In this article, insulin has been a model drug, as an important drug in lowering blood glucose and as a classic protein drug. PS was extracted from pig lungs and was observed as nanoparticles morphology in water by transmission electron microscopy after preparation. Inhalation dry powders were formulated by PS nanoparticles, insulin, and other excipients. In addition, blood glucose level of rats was determined when the insulin dry powder of PS group and control group was delivered by inhalation route.
Compared with control group, scanning electron microscopy showed that the dry powders of PS group possess similar particle size and smoother surface. The spray-dried powders re-suspended possessed similar nanoparticle appearance compared with the original PS suspension. Animal studies showed that blood glucose level was effectively reduced when the insulin dry powder of PS group was delivered by inhalation route. Compared with subcutaneous injection group (4 U/kg), the relative pharmacological bioavailability of the insulin dry powders of control group (14 U/kg) and PS group (14 U/kg) was 19.97% and 32.57%, respectively.
PS nanoparticles, as absorption enhancers used in dry powder inhalation, could evidently enhance the effect of insulin in lowering blood glucose.
研究肺表面活性剂（PS）纳米颗粒作为胰岛素干粉递药吸收促进剂的制备和应用。PS 是一种主要由磷脂和蛋白质组成的复杂混合物。这种组成导致了表面活性剂独特的铺展效果和自发形成纳米颗粒，这可能是肺部药物传递系统的有利特征。
本文以胰岛素为模型药物，作为降低血糖的重要药物和经典蛋白药物。PS 从猪肺中提取，经制备后在水中用透射电子显微镜观察到纳米颗粒形态。通过 PS 纳米颗粒、胰岛素和其他赋形剂来配制吸入干粉。此外，当 PS 组和对照组的胰岛素干粉通过吸入途径给药时，测定大鼠的血糖水平。
与对照组相比，扫描电子显微镜显示 PS 组的干粉具有相似的粒径和更光滑的表面。喷雾干燥粉末再混悬后与原始 PS 悬浮液具有相似的纳米颗粒外观。动物研究表明，当 PS 组的胰岛素干粉通过吸入途径给药时，血糖水平得到有效降低。与皮下注射组（4U/kg）相比，对照组（14U/kg）和 PS 组（14U/kg）的胰岛素干粉的相对药理生物利用度分别为 19.97%和 32.57%。
作为干粉吸入用吸收促进剂的 PS 纳米颗粒，可显著增强胰岛素降低血糖的效果。
