An Evaluation of Inhaled Antibiotic Liposome versus Antibiotic Nanoplex in Controlling Infection in Bronchiectasis

Publication date: Available online 4 February 2019Source: International Journal of PharmaceuticsAuthor(s): The-Thien Tran, Hong Yu, Celine Vidaillac, Albert Y.H. Lim, John A. Abisheganaden, Sanjay H. Chotirmall, Kunn HadinotoAbstractInhaled antibiotic nanoparticles have emerged as an effective strategy to control infection in bronchiectasis lung owed to their mucus-penetrating ability. Using ciprofloxacin (CIP) as the model antibiotic, we evaluated dry powder inhaler (DPI) formulations of two classes of antibiotic nanoparticles (i.e. liposome and nanoplex) in their (1) physical characteristics (i.e. size, zeta potential, CIP payload, preparation efficiency), (2) dissolution in artificial sputum medium, (3) ex vivo mucus permeability, (4) antimicrobial activity against Pseudomonas aeruginosa in mucus, (5) cytotoxicity towards human lung epithelium cells, and (6) in vitro aerosolization efficiency. The results showed that the CIP nanoplex exhibited fast dissolution with CIP supersaturation generation, in contrast to the slower release of the liposome (80 versus 30% dissolution after 1h). Both nanoparticles readily overcame the mucus barrier attributed to their nanosize and mucus-inert surface (50% permeation after 1h), leading to their similarly high antipseudomonal activity. The CIP liposome, however, possessed much lower CIP payload than the nanoplex (84% versus 3.5%), resulting in high lipid contents in its DPI formulation that led to higher cytotoxicity and lower aerosoliza...
Source: International Journal of Pharmaceutics - Category: Drugs & Pharmacology Source Type: research