besifloxacin and Keratitis

Topics: Animals; Anti-Bacterial Agents; Aqueous Humor; Azepines; Chromatography, High Pressure Liquid; Female; Fluorescence; Fluoroquinolones; Humans; Keratitis; Limit of Detection; Male; Rabbits; Tandem Mass Spectrometry; Tears

Novel drug delivery systems have emerged to treat bacterial keratitis, an acute infection of the cornea. In this study, besifloxacin HCl loaded insert formulations were designed and investigated in vitro, ex vivo and in vivo for the treatment of bacterial keratitis. Besifloxacin HCl (BH) or BH-hydroxypropyl-beta-cyclodextrin (HP-β-CD) complex containing poly(caprolactone)/polyethylene glycol (PLC/PEG) fibrous inserts were prepared with an electrospinning method. These fibrous inserts were coated with mucoadhesive polymers such as sodium alginate (SA) or thiolated sodium alginate (TSA). Developed inserts compared to commercially available drug and it was found that coating of the insert surfaces with SA and TSA, increases bioadhesion of the formulations. Insert formulations showed a burst release in the first 2 days followed by a slow-release profile. Ex vivo transport studies showed that HP-β-CD possessed a drug delivery level close to the commercial drug. Both TSA coated inserts as well as inserts containing HP-β-CD-drug complex were effectively reducing bacterial keratitis in rabbit eyes upon single-dose application compared to multiple dosing with the commercial drug. Consequently, TSA coated inserts as well as the inserts containing HP-β-CD-drug complex, may be potential alternatives to conventional market product by reducing the application frequency in the clinic leading to increased patient compliance.

Topics: 2-Hydroxypropyl-beta-cyclodextrin; Alginates; Animals; Anti-Bacterial Agents; Azepines; Bacteriological Techniques; Cell Survival; Dose-Response Relationship, Drug; Drug Delivery Systems; Drug Liberation; Female; Fluoroquinolones; Humans; Keratitis; Male; Nanofibers; Polyesters; Polyethylene Glycols; Rabbits; Technology, Pharmaceutical

The objective of this study was to collect and evaluate retrospective safety information about the use of besifloxacin ophthalmic suspension 0.6% for the treatment of bacterial keratitis.. This was a retrospective, postmarketing surveillance study conducted at 10 clinical centers in the United States. The study population included 142 patients treated with besifloxacin ophthalmic suspension 0.6% for bacterial keratitis in one or both eyes. For perspective, data on 85 patients treated at these centers with moxifloxacin ophthalmic solution 0.5% for bacterial keratitis were also included. The analysis was designed to measure the types and rates of adverse events (AEs) reported during the treatment of bacterial keratitis with besifloxacin ophthalmic suspension 0.6%. Other treatment outcomes of interest included the development of corneal scarring and corneal neovascularization, measured or presumed bacterial eradication, ending visual acuity, and duration of pain before and after treatment.. There was one reported AE of mild superficial punctate keratitis in a patient using besifloxacin ophthalmic suspension 0.6%. The difference in AE frequencies between groups was not significant (P>0.999). Additional treatment outcomes were similar for both groups. Limitations of this report include the retrospective nature of the study.. These retrospective data suggest that besifloxacin ophthalmic suspension 0.6% was well tolerated when included in the treatment of bacterial keratitis; no serious AEs were reported. A prospective clinical trial is needed to better isolate the contribution of besifloxacin to the therapeutic outcome and to confirm these observations.

Topics: Adolescent; Adult; Aged; Aged, 80 and over; Anti-Bacterial Agents; Azepines; Eye Infections, Bacterial; Female; Fluoroquinolones; Humans; Keratitis; Male; Middle Aged; Ophthalmic Solutions; Product Surveillance, Postmarketing; Retrospective Studies; Treatment Outcome; Young Adult