Ketoprofen Lysinate

Stigliani M, et al. International Journal of Pharmaceutics, 2013, 448(1), 198-204.

Ketoprofen lysinate, a non-steroidal anti-inflammatory drug (NSAID), has been engineered into inhalable microparticles for targeted pulmonary delivery, addressing chronic inflammation in cystic fibrosis (CF) patients. Using a co-spray drying process, ketoprofen lysinate was combined with leucine (85:15 w/w) as a dispersibility enhancer, creating respirable powders optimized for deep lung deposition. The formulations were prepared from water or hydro-alcoholic mixtures, achieving high process yields and consistent particle morphology suitable for aerosolization.
Comprehensive evaluation using an Andersen cascade impactor demonstrated the ability of these particles to reach the lower airways efficiently. An artificial CF mucus model showed that while the mucus layer delayed drug dissolution and permeation, leucine did not influence these dynamics. Importantly, cell viability assays on ΔF508 CF human airway epithelial cells (CuFi1) revealed that the spray drying process reduced the cytotoxicity of the raw drug, enhancing biocompatibility.