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Nano into Micro Formulations of Tobramycin for the Treatment of Pseudomonas aeruginosa Infections in Cystic Fibrosis
Biomacromolecules ( IF 6.2 ) Pub Date : 2017-11-16 00:00:00 , DOI: 10.1021/acs.biomac.7b00945
Barbara Porsio 1 , Maria Grazia Cusimano 1 , Domenico Schillaci 1 , Emanuela Fabiola Craparo 1 , Gaetano Giammona 1, 2 , Gennara Cavallaro 1
Affiliation  

Here, nano into micro formulations (NiMs) of tobramycin for the treatment of Pseudomonas aeruginosa airway infections in cystic fibrosis (CF) are described. NiMs were produced by spray drying a solution containing polymers or sugars and a nanometric polyanion–tobramcyin complex (PTC), able to achieve a prolonged antibiotic release. NiMs properties were compared to TOBIPodhaler(Novartis), the only one commercially available dry powder inhalatory formulation based on porous microparticles. Produced NiMs showed adequate characteristics for pulmonary administration, as spherical shape, micrometric size, and high cytocompatibility toward human bronchial epithelial cells. Contrarily to TOBIPodhaler, some of produced NiMs, thanks to their specific chemical composition, are able to facilitate the drug diffusion through the mucus secretion, achieving, at the same time, a sustained tobramycin delivery. Moreover, NiMs showed pronounced antimicrobial activity against P. aeruginosa pathogens and their biofilm, if compared to free tobramycin and TOBIPodhaler, demonstrating the potential of obtained formulations as drug delivery systems for the treatment of pulmonary infections in CF patients.

中文翻译:

纳米妥布霉素微配方治疗囊性纤维化铜绿假单胞菌感染

在这里,妥布霉素的纳米微制剂(NiMs)用于治疗铜绿假单胞菌描述了囊性纤维化(CF)中的气道感染。NiMs是通过喷雾干燥包含聚合物或糖和纳米级聚阴离子-藤霉素复合物(PTC)的溶液来生产的,能够延长抗生素的释放时间。将NiMs性能与TOBIPodhaler(Novartis)进行了比较,TOBIPodhaler是唯一一种基于多孔微粒的市售干粉吸入制剂。产生的NiMs具有球形给药,微米级尺寸和对人支气管上皮细胞高度的细胞相容性等适合肺部给药的特性。与TOBIPodhaler相反,由于其特定的化学组成,一些生产的NiMs能够促进药物通过粘液分泌物扩散,同时实现持续的妥布霉素递送。而且,如果将铜绿假单胞菌病原体及其生物膜与游离妥布霉素和TOBIPodhaler进行比较,则表明所获得的制剂作为药物输送系统的潜力,可用于治疗CF患者的肺部感染。
更新日期:2017-11-17
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