Lehmler Hans-Joachim
Research Scientist, University of Iowa, Department of Occupational and Environmental Health, Iowa City, IA 52242, USA.
Expert Opin Drug Deliv. 2007 May;4(3):247-62. doi: 10.1517/17425247.4.3.247.
Drug delivery to the diseased lung is hindered by the buildup of fluid and shunting of blood flow away from the site of injury. The use of perfluorocarbon compounds (PFCs) as drug delivery vehicles has been proposed to overcome these obstacles. This drug delivery approach is based on the unique properties of PFCs. For example, PFCs can homogeneously fill the lung and recruit airways by replacing edematous fluid. Analogously, drugs administered with a PFC vehicle are expected to be homogeneously distributed throughout the lung. At the same time, intrapulmonary administration of the drug will achieve higher drug concentrations in the lung than conventional approaches, while reducing systemic exposure. Unfortunately, PFCs are poor solvents for typical drug molecules. To overcome this obstacle, several approaches, such as dispersions, prodrugs, solubilizing agents and (micro)emulsions, are under investigation to develop homogeneous PFC-drug mixtures suitable for intrapulmonary administration.
液体的积聚和血流从损伤部位分流阻碍了药物向患病肺部的递送。有人提出使用全氟化碳化合物（PFCs）作为药物递送载体来克服这些障碍。这种药物递送方法基于PFCs的独特性质。例如，PFCs可以均匀地填充肺部并通过取代水肿液来恢复气道功能。类似地，预计与PFC载体一起给药的药物将均匀地分布在整个肺部。同时，药物的肺内给药将比传统方法在肺部实现更高的药物浓度，同时减少全身暴露。不幸的是，PFCs对于典型的药物分子来说是不良溶剂。为了克服这一障碍，正在研究几种方法，如分散体、前药、增溶剂和（微）乳液，以开发适合肺内给药的均匀PFC-药物混合物。
