Moxifloxacin in situ gelling microparticles–bioadhesive delivery system

Abstract

Antibiotic use for ocular treatments has been largely limited by poor local bioavailability with conventional eyedrops formulations. Here, we developed a controlled delivery system composed of moxifloxacin-loaded poly(lactic-co-glycolic acid) (PLGA) microparticles encapsulated in a chondroitin sulfate-based, two-component bioadhesive hydrogel. Using a simple and fast electrohydrodynamic spray drying (electrospraying) technique, surfactant-free moxifloxacin-loaded microparticles were fabricated with diameters on the order of 1 μm. A mixed solvent system of methanol/dichloromethane (MeOH/DCM) was employed to prepare the microparticles for the electrospraying processing. Extended release of moxifloxacin using a series of MeOH/DCM mixed solvents was accomplished over 10 days with release concentrations higher than the minimum inhibitory concentration (MIC). In contrast, moxifloxacin loaded directly in hydrogels was released rapidly within 24 h. We observed a decrease of the drug release rate from the microparticles when using an increased percentage of methanol in the mixed solvent from 10% to 30% (v/v), which can be explained by the mixed solvent system providing a driving force to form a gradient of the drug concentrations inside the microparticles. In addition, the delivery system developed in this study, which incorporates a bioadhesive to localize drug release by in situ gelling, may potentially integrate antibiotic prophylaxis and wound healing in the eye.

High Hydrostatic Pressure as Sterilization Method for Drug-Loaded Intraocular Lenses

“…Thus, a decrease in the swelling capacity of the material would be expected. Instead, slightly higher swelling was observed, which may be attributed to the hydrophilicity of the drugs 46,47 loaded in a significantly greater amount in the sterilized samples (60% for MXF and 138% for KTL). HHP sterilization did not change the sample's transmittance, did not induce activity loss of the antibiotic, and ensured sterility of all drug-loaded samples, meaning that HHP sterilization should be suitable as a terminal sterilization method for drug-loaded IOLs.…”

Endophthalmitis Prophylaxis Using a Single Drop of Thermoresponsive Controlled-Release Microspheres Loaded with Moxifloxacin in a Rabbit Model

“…9,10 Reformulated topical drops using mucoadhesive agents or gels tend to provide shorter windows of drug release, 11 which would necessitate additional instillation by the patient during the postoperative period. In general, longer drug release times require larger and potentially uncomfortable inserts, or more invasive methods to accommodate the degrading depot as it releases the entrapped drug.…”

Sulfated Hydrogels in Intervertebral Disc and Cartilage Research

“…In addition to alginate, CS and PEG microparticles loaded with moxifloxacin have been successfully fabricated through electrospraying techniques. The encapsulation in CS and PEG creates a bioadhesive to allow for the localization of microparticle distribution through in situ gelling [ 51 ].…”