5'-DMT-dG(iBu)-Suc-CPG; 2000 Å

Clinical trials have demonstrated the benefits of ibuprofen therapy in cystic fibrosis (CF) patients, an effect that is currently attributed to ibuprofen's anti-inflammatory properties. Yet, a few previous reports demonstrated an antimicrobial activity of ibuprofen as well, although none investigated its direct effects on the pathogens found in the CF lung, which is the focus of this work. Determination of ibuprofen's in vitro antimicrobial activity against Pseudomonas aeruginosa and Burkholderia species strains through measurements of the endpoint number of CFU and growth kinetics showed that ibuprofen reduced the growth rate and bacterial burden of the tested strains in a dose-dependent fashion. In an in vitroPseudomonas biofilm model, a reduction in the rate of biomass accumulation over 8 h of growth with ibuprofen treatment was observed. Next, an acute Pseudomonas pneumonia model was used to test this antimicrobial activity after the oral delivery of ibuprofen. Following intranasal inoculation, ibuprofen-treated mice exhibited lower CFU counts and improved survival compared with the control animals. Preliminary biodistribution studies performed after the delivery of ibuprofen to mice by aerosol demonstrated a rapid accumulation of ibuprofen in serum and minimum retention in lung tissue and bronchoalveolar lavage fluid. Therefore, ibuprofen-encapsulated polymeric nanoparticles (Ibu-NPs) were formulated to improve the pharmacokinetic profile. Ibu-NPs formulated for aerosol delivery inhibited the growth of P. aeruginosa in vitro and may provide a convenient dosing method. These results provide an additional explanation for the previously observed therapeutic effects of ibuprofen in CF patients and further strengthen the argument for its use by these patients.

Ibuprofen (IBU) has been available as a topical skin preparation for more than two decades. Its primary indication is for the relief of pain and inflammation in rheumatic disease and other musculoskeletal conditions. This article reviews the various formulation strategies which have been investigated for percutaneous IBU delivery to date. The focus is on studies which have been conducted with IBU in the free base form on human or porcine skin as data from other species are known to overestimate likely permeation in man. Emerging technologies for enhanced dermal delivery of IBU are considered including methods which require physical disruption of the membrane. The role of biophysical techniques such as Confocal Raman Spectroscopy in the rational development of IBU formulations is also discussed.

Nonprescription ibuprofen is useful for managing minor aches and pains, reducing fever, and relieving symptoms of dysmenorrhea. For these indications, ibuprofen's effectiveness has been judged to be equal or superior to other available nonprescription analgesics. Ibuprofen is not recommended for self-treatment in children less than 12 years old.