Zhou Qi Tony, Sun Si-Ping, Chan John Gar Yan, Wang Ping, Barraud Nicolas, Rice Scott A, Wang Jiping, Li Jian, Chan Hak-Kim
†Advanced Drug Delivery Group, Faculty of Pharmacy, The University of Sydney, Sydney, NSW 2006, Australia.
‡JHL Biotech, Inc., Zhubei City, Hsinchu County 302, Taiwan, R.O.C.
Mol Pharm. 2015 Aug 3;12(8):2594-603. doi: 10.1021/mp500586p. Epub 2014 Dec 24.
Colistin has been increasingly used for the treatment of respiratory infections caused by Gram-negative bacteria. Unfortunately parenteral administration of colistin can cause severe adverse effects. This study aimed to develop an inhaled combination dry powder formulation of colistin and rifapentine for the treatment of respiratory infections. The combination formulation was produced by spray-drying rifapentine particles suspended in an aqueous colistin solution. The combination dry powder had enhanced antimicrobial activities against planktonic cells and biofilm cultures of Pseudomonas aeruginosa, with both minimum inhibitory concentration (MIC) and minimum biofilm inhibitory concentration (MBIC) values (2 and 4 mg/L, respectively) being half that of pure colistin (MIC 4 mg/L and MBIC 8 mg/L) and 1/16th that of pure rifapentine (MIC 32 mg/L and MBIC 64 mg/L). High aerosol performance, as measured via an Aerolizer device, was observed with emitted doses>89% and fine particle fraction (FPF) total>76%. The proportion of submicron particles of rifapentine particles was minimized by the attachment of colistin, which increased the overall particle mass and aerodynamic size distribution. Using the spray-drying method described here, stable particles of amorphous colistin and crystalline rifapentine were distributed homogeneously in each stage of the impinger. Unlike the colistin alone formulation, no deterioration in aerosol performance was found for the combination powder when exposed to a high relative humidity of 75%. In our previous study, surface coating by rifampicin contributed to the moisture protection of colistin. Here, a novel approach with a new mechanism was proposed whereby moisture protection was attributed to the carrier effect of elongated crystalline rifapentine particles, which minimized contact between hygroscopic colistin particles. This inhaled combination antibiotic formulation with enhanced aerosol dispersion efficiency and in vitro efficacy could become a superior treatment for respiratory infections.
黏菌素越来越多地用于治疗由革兰氏阴性菌引起的呼吸道感染。不幸的是,肠胃外给药的黏菌素会引起严重的不良反应。本研究旨在开发一种用于治疗呼吸道感染的黏菌素和利福喷汀吸入联合干粉制剂。该联合制剂是通过喷雾干燥悬浮在黏菌素水溶液中的利福喷汀颗粒而制备的。该联合干粉对铜绿假单胞菌的浮游细胞和生物膜培养物具有增强的抗菌活性,其最低抑菌浓度(MIC)和最低生物膜抑菌浓度(MBIC)值(分别为2和4 mg/L)是纯黏菌素(MIC 4 mg/L和MBIC 8 mg/L)的一半,是纯利福喷汀(MIC 32 mg/L和MBIC 64 mg/L)的1/16。通过Aerolizer装置测量,观察到高气溶胶性能,发射剂量>89%,细颗粒分数(FPF)总计>76%。黏菌素的附着使利福喷汀颗粒的亚微米颗粒比例最小化,这增加了整体颗粒质量和空气动力学尺寸分布。使用此处描述的喷雾干燥方法,无定形黏菌素和结晶利福喷汀的稳定颗粒均匀分布在撞击器的每个阶段。与单独的黏菌素制剂不同,当暴露于75%的高相对湿度时,联合粉末的气溶胶性能没有恶化。在我们之前的研究中,利福平的表面包衣有助于黏菌素的防潮。在此,提出了一种具有新机制的新方法,即防潮归因于细长结晶利福喷汀颗粒的载体效应,这使吸湿性黏菌素颗粒之间的接触最小化。这种具有增强的气溶胶分散效率和体外疗效的吸入联合抗生素制剂可能成为呼吸道感染的一种优质治疗方法。