Although mutant selection experiments indicated that gyrase is a primary target, further biochemical and genetic studies showed that besifloxacin has potent, relatively balanced activity against both essential DNA gyrase and topoisomerase IV targets in S. aureus and S. pneumoniae.

No abstract

In this rabbit study, the Retisert provides relatively constant levels of FA in the posterior pole, which is consistent with previous reports of its clinical utility.

BOL-303224-A is a novel fluoroquinolone that has never been used systemically and that possesses structural modifications intended to improve its potency compared to other fluoroquinolones. This investigation was conducted to evaluate the nonclinical pharmacokinetics, safety, and pharmacodynamics of BOL-303224-A. BOL-303224-A displayed activity in in vitro antimicrobial efficacy studies and also demonstrated efficacy in an in vivo murine infection model. BOL-303224-A demonstrated excellent ocular pharmacokinetics in rabbits, with ocular mean residence times >7 h, and conjunctival concentrations in excess of the MIC(90) for nonresistant ophthalmic isolates for >12 h following a single dose. Pharmacokinetic modeling from these data indicated that BOL-303224-A has the potential to demonstrate efficacy against ophthalmologic pathogens with a TID dosing regimen. BOL-303224-A also demonstrated reasonably low plasma protein binding in rat and human models, as well as good metabolic stability across species. In studies designed to explore the nonclinical safety profile of BOL-303224-A, the compound showed excellent topical ocular tolerance in rabbits and dogs, as well as a favorable genotoxicity and phototoxicity profile. In summary, BOL-303224-A exhibits an encouraging nonclinical pharmacodynamic, pharmacokinetic, and safety profile that supports clinical development as a topical agent for the potential treatment of ophthalmic infections.

This experiment shows that ReNu MultiPlus, SOLO-care Plus With Aqualube, Complete Moisture Plus, and AQuify 5 Minute contact lens solutions have a minimal effect on human corneal epithelial cells in culture, whereas OPTI-FREE Express has a higher negative effect on tight junctions, cell membranes, and overall metabolism of these human corneal epithelial cells.

This review tabulates the known studies, highlights key considerations in study design, and describes useful methods in characterization of the hypoxic response.

OPTI-FREE Express has the potential for deeper mitochondrial effects compared to ReNu MultiPlus No Rub and Hanks' balanced salt solution controls.

The effect of alginic acid addition to 1% or 2% carteolol solutions on the ocular penetration of the drug has been evaluated in the pigmented rabbit. During single dose studies, an increase in bioavailability ranging from 40% to 60% was observed in the aqueous humor and in the iris-ciliary body. During repeated dose studies, this increased ocular bioavailability of carteolol in the presence of alginic acid led to an equivalent concentration in the target tissue, although the dosage was only once a day compared with twice a day for the usual carteolol eyedrops. 14C-carteolol distribution studies demonstrated the binding of carteolol in pigmented ocular tissues. Thus, the presence of alginic acid as a new excipient supports a possible decrease in dosage regimen, while retaining sufficient ocular bioavailability to lower intraocular pressure.