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Title: An evaluation of inhaled antibiotic liposome versus antibiotic nanoplex in controlling infection in bronchiectasis
Authors: Tran, The-Thien
Yu, Hong
Vidaillac, Celine
Lim, Albert Y. H.
Abisheganaden, John A.
Chotirmall, Sanjay Haresh
Hadinoto, Kunn
Keywords: Engineering::Chemical engineering
Issue Date: 2019
Source: Tran, T.-T., Yu, H., Vidaillac, C., Lim, A. Y. H., Abisheganaden, J. A., Chotirmall, S. H., & Hadinoto, K. (2019). An evaluation of inhaled antibiotic liposome versus antibiotic nanoplex in controlling infection in bronchiectasis. International Journal of Pharmaceutics, 559, 382–392. doi:10.1016/j.ijpharm.2019.01.062
Journal: International journal of pharmaceutics 
Abstract: Inhaled 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 1 h). Both nanoparticles readily overcame the mucus barrier attributed to their nanosize and mucus-inert surface (50% permeation after 1 h), 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 aerosolization efficiency. The CIP nanoplex thus represented a superior formulation owed to its simpler preparation, higher CIP payload hence lower dosage, better aerosolization, and lower cytotoxicity.
ISSN: 0378-5173
DOI: 10.1016/j.ijpharm.2019.01.062
Schools: School of Chemical and Biomedical Engineering 
Lee Kong Chian School of Medicine (LKCMedicine) 
Rights: © 2019 Elsevier B.V. All rights reserved. This paper was published in International journal of pharmaceutics and is made available with permission of Elsevier B.V.
Fulltext Permission: open
Fulltext Availability: With Fulltext
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