Sodium colistimethate (SCM) and amikacin (AMK) are among the few antibiotics effective against resistant P. aeruginosa, K. pneumoniae and A. baumannii; however, their toxicity severely limits their use. Enclosing antibiotics into nanostructured lipid carriers (NLC) might decrease drug toxicity and improve antibiotic disposition. In this work, SCM or AMK was loaded into different NLC formulations, through high pressure homogenization, and their in vitro and in vivo effectiveness was analyzed. The encapsulation process did not reduce drug effectiveness since in vitro SCM-NLC and AMK-NLC drug activity was equal to that of the free drugs. As cryoprotectant, trehalose showed better properties than dextran. Instead, positive chitosan coating was discarded due to its limited cost-efficiency. Finally, the in vivo study in acute pneumonia model revealed that intraperitoneal administration was superior to the intramuscular route and confirmed that (−) SCM-NLC with trehalose, was the most suitable formulation against an extensively drug-resistant A. baumannii strain.

大黄素硫酸钠（SCM）和丁胺卡那霉素（AMK）是有效抵抗铜绿假单胞菌，肺炎克雷伯氏菌和鲍曼不动杆菌的少数抗生素。但是，它们的毒性严重限制了它们的使用。将抗生素封入纳米结构脂质载体（NLC）中可能会降低药物毒性并改善抗生素处置。在这项工作中，通过高压匀浆将SCM或AMK装入不同的NLC制剂中，并分析了它们的体外和体内有效性。自体外以来，封装过程并未降低药物效力SCM-NLC和AMK-NLC的药物活性与游离药物相同。海藻糖作为防冻剂比葡聚糖具有更好的性能。取而代之的是，由于其有限的成本效率，正的壳聚糖涂层被丢弃了。最后，在急性肺炎模型中的体内研究表明，腹膜内给药优于肌内途径，并证实（-）含海藻糖的SCM-NLC是对抗广泛耐药的鲍曼不动杆菌菌株的最合适制剂。