Penetration of moxifloxacin into the human aqueous humour after oral administration

Aims: To determine the pharmacokinetics of moxifloxacin, a new generation fluoroquinolone, in the anterior chamber of the human uninflamed eye. Methods: 35 patients undergoing cataract surgery received two doses of 400 mg of oral moxifloxacin with a 12 hour interval and were divided into six groups. Moxifloxacin levels in aqueous humour and serum were determined by a microbiological agar well diffusion technique at 2, 4, 6, 8, 10, and 12 hours after the second dose in each group respectively. Results: Mean moxifloxacin levels in the anterior chamber were 1.20 (SD 0.35) μg/ml at the 2 hours group, 1.22 (0.48) μg/ml at the 4 hours group, 1.20 (0.45) μg/ml at the 6 hours group, 1.58 (0.38) μg/ml at the 8 hours group, 1.37 (0.44) μg/ml at the 10 hours group, and 1.23 (0.55) μg/ml at the 12 hours group. The mean ratio of aqueous to serum moxifloxacin level was 38%. Conclusion: Moxifloxacin penetrates well into the anterior chamber of the human uninflamed eye after oral administration, reaching early significant levels, which are maintained for at least 12 hours and are much higher than the MIC(90) values of Gram positive and Gram negative pathogens commonly implicated in intraocular infections with the exceptions of fluoroquinolone resistant staphylococci, MRSA, and Pseudomonas aeruginosa

Penetration of moxifloxacin into the human aqueous humour after oral administration

Aims: To determine the pharmacokinetics of moxifloxacin, a new generation fluoroquinolone, in the anterior chamber of the human uninflamed eye. Methods: 35 patients undergoing cataract surgery received two doses of 400 mg of oral moxifloxacin with a 12 hour interval and were divided into six groups. Moxifloxacin levels in aqueous humour and serum were determined by a microbiological agar well diffusion technique at 2, 4, 6, 8, 10, and 12 hours after the second dose in each group respectively. Results: Mean moxifloxacin levels in the anterior chamber were 1.20 (SD 0.35) mg/ml at the 2 hours group, 1.22 (0.48) mg/ml at the 4 hours group, 1.20 (0.45) mg/ml at the 6 hours group, 1.58 (0.38) mg/ml at the 8 hours group, 1.37 (0.44) mg/ml at the 10 hours group, and 1.23 (0.55) mg/ml at the 12 hours group. The mean ratio of aqueous to serum moxifloxacin level was 38%. Conclusion: Moxifloxacin penetrates well into the anterior chamber of the human uninflamed eye after oral administration, reaching early significant levels, which are maintained for at least 12 hours and are much higher than the MIC90 values of Gram positive and Gram negative pathogens commonly implicated in intraocular infections with the exceptions of fluoroquinolone resistant staphylococci, MRSA, and Pseudomonas aeruginosa

Ocular Drug Delivery

Ocular drug delivery has been a major challenge to pharmacologists and drug delivery scientists due to its unique anatomy and physiology. Static barriers (different layers of cornea, sclera, and retina including blood aqueous and blood–retinal barriers), dynamic barriers (choroidal and conjunctival blood flow, lymphatic clearance, and tear dilution), and efflux pumps in conjunction pose a significant challenge for delivery of a drug alone or in a dosage form, especially to the posterior segment. Identification of influx transporters on various ocular tissues and designing a transporter-targeted delivery of a parent drug has gathered momentum in recent years. Parallelly, colloidal dosage forms such as nanoparticles, nanomicelles, liposomes, and microemulsions have been widely explored to overcome various static and dynamic barriers. Novel drug delivery strategies such as bioadhesive gels and fibrin sealant-based approaches were developed to sustain drug levels at the target site. Designing noninvasive sustained drug delivery systems and exploring the feasibility of topical application to deliver drugs to the posterior segment may drastically improve drug delivery in the years to come. Current developments in the field of ophthalmic drug delivery promise a significant improvement in overcoming the challenges posed by various anterior and posterior segment diseases