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Modulated release of ciprofloxacin in the lung

机译：调节肺中环丙沙星的释放

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Purpose: Previous studies [1] have shown that the best protection against respiratory infections is by delivering anti-infectives and antibiotics directly to the lungs. In this work; a new class of pulmonary delivery particles is described. These particles consist of multi-micron sized chemically linked agglomerates of core nanoparticles. The links between the nanoparticles can be either permanent (e.g. Carbonyl); or cleavable (e.g. disulfide or ester). The release rate of drug from the assembly can be modulated by controlling the extent of cleavage of the links. Data on the release of ciprofloxacin from these agglomerates in vitro is presented. Methods: Ciprofloxacin was remotely loaded [2] into liposomes bearing PEG-NH2 functional groups. These loaded liposomes were then agglomerated using a thiolytically cleavable linker – DTBP (dimethyl 3;3’-dithiobispropionimidate?2HCl) [3]. Size characterization using light scattering as also aerosol characterization and encapsulation studies upon nebulization (using Parijet LC nebulizer) of ciprofloxacin-loaded carriers was performed. Additionally; the in vitro release profiles of ciprofloxacin from the agglomerates in simulated lung media at 37°C have been evaluated.
机译：目的：以前的研究[1]表明，对呼吸道感染的最佳保护是通过将抗感染性和抗生素直接递送给肺部。在这项工作中;描述了一种新的肺递送颗粒。这些颗粒由核心纳米颗粒的多微米尺寸的化学连接附聚物组成。纳米颗粒之间的链接可以是永久性的（例如羰基）;或可裂解（例如二硫化物或酯）。可以通过控制链路的切割程度来调节来自组件的药物的释放速率。介绍了在体外这些附聚物中释放环丙沙星的数据。方法：将环丙沙星远程加载[2]含有PEG-NH2官能团的脂质体。然后使用硫脲可裂解的接头 - DTBP（二甲基3'-二硫代二硫仿→2HCl）粘聚这些装载的脂质体。使用光散射的尺寸表征作为气溶胶表征和对雾化的雾化（使用Parijet LC雾化器）的雾化物质的封装研究进行了加载的载体的载体。此外;已经评估了在37℃下从模拟肺介质中的凝聚物中的环丙沙星的体外释放曲线。

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