Antibiotic transport across bronchial epithelial cells: Effects of molecular weight, LogP and apparent permeability

Ultra‐thin, high strength, antibiotic‐eluting sutures for prevention of ophthalmic infection

“…We manufactured 1575 twist, 28 μm sutures composed of PCL and 8% of either moxifloxacin hydrochloride, dexamethasone, rapamycin, or bupivacaine hydrochloride. Moxifloxacin HCl (log P = 0.01) is a fourth generation fluoroquinolone with broad antibacterial efficacy currently administered via topical eye drops 36,49 . Dexamethasone (log P = 1.83) is a corticosteroid used for treatment of uveitis and diabetic macular edema 50‐53 .…”

“…Moxifloxacin HCl (log P = 0.01) is a fourth generation fluoroquinolone with broad antibacterial efficacy currently administered via topical eye drops. 38,51 Dexamethasone (log P = 1.83) is a corticosteroid used for treatment of uveitis and diabetic macular edema. [52][53][54][55] Rapamycin (log P = 4.3) is an immunosuppressant and anti-proliferative agent used in treatment of uveitis.…”

Antimicrobial Molecules in the Lung: Formulation Challenges and Future Directions for Innovation

“…The high solubility and low logP of tobramycin suggest it should have a long absorption halflife across the lung epithelium [30], facilitating high local concentrations of tobramycin. This has been demonstrated experimentally in an in vitro model of the human bronchial epithelium [48]. Tobramycin demonstrated limited permeability compared to other antibiotics studied, including rifampicin and moxifloxacin.…”

“…The modest molecular weight and increased lipophilicity when in its uncharged state at physiological pH would be expected to result in an increased permeation across the respiratory epithelium following inhalation [30], and this has been demonstrated in cell culture studies. In vitro transport studies of ciprofloxacin transport across the Calu-3 bronchial epithelial cell culture model showed ~81% of 10 µM ciprofloxacin and ~49% of 20 µM ciprofloxacin was transported in the apical to basal direction over 180 min exposure [48]. The rate of transport was not dependent on initial drug concentration, suggesting that the transport of ciprofloxacin may involve the role of drug transporters as well as passive diffusion.…”

“…Tobramycin's activity against gram negative bacteria, including P. aeruginosa, has made it a first-line treatment for chronic infection in the CF lung [47]. The oxygen and nitrogen-rich structure has a high aqueous solubility and a logP of -7.32 [48]. These physicochemical properties impart poor oral bioavailability [49], and thus systemic dosing must take place via intravenous administration.…”