Mitra R, Pezron I, Li Y, Mitra A K
Division of Pharmaceutical Sciences, School of Pharmacy, University of Missouri-Kansas City, 5100 Rockhill Road, Kansas City, MO 64110-2499, USA.
Int J Pharm. 2001 Apr 17;217(1-2):25-31. doi: 10.1016/s0378-5173(01)00588-9.
Pulmonary delivery appears to be the most promising non-parenteral route of insulin administration. In this work, we investigated the enhancement of insulin absorption in the presence of phospholipids and lung lavage fluid in vivo and in vitro. In-vitro experiments of insulin uptake by type II cells showed a significantly enhanced absorption in presence of lavage fluid, compared to various buffer preparations. The same trend was obtained with in-vivo studies of tracheal instillation of insulin. The incorporation of phospholipids as absorption enhancers in 1,2-dipalmitoyl phosphatidylcholine (DPPC) dispersion was compared to blank liposomes. A significantly higher blood glucose decrease was observed with a DPPC-insulin physical mixture compared to liposome, suggesting a possible effect of the phospholipid chain physical state on the insulin in-vivo absorption.
肺部给药似乎是最具前景的非肠道胰岛素给药途径。在本研究中，我们在体内和体外研究了磷脂和肺灌洗液存在下胰岛素吸收的增强情况。II型细胞摄取胰岛素的体外实验表明，与各种缓冲液制剂相比，在灌洗液存在下吸收显著增强。胰岛素气管内滴注的体内研究也得到了相同的趋势。将作为吸收促进剂的磷脂掺入1,2-二棕榈酰磷脂酰胆碱（DPPC）分散体中，并与空白脂质体进行比较。与脂质体相比，DPPC-胰岛素物理混合物观察到血糖显著降低，表明磷脂链物理状态对胰岛素体内吸收可能有影响。
