Abstract
Antibiotics delivered through conventional dosage against ophthalmic infections show lower therapeutic efficacy due to their low residence time. Therefore, there is a great need to design and develop novel dosage forms that would increase the ocular residence time of antibiotics at the site of infection. This study describes the development of nanoparticles laden in situ gelling solution, intended to sustain antibiotic release for improved therapeutic efficiency. Oxytetracycline-loaded gelatin-polyacrylic acid nanoparticles were prepared and incorporated in poloxamer-N407 solution. The rheological properties of the system were studied concerning time and temperature. Moreover, in vivo biocompatibility of the system was ascertained using the Draize test and histological studies. Finally, the optimized formulation was evaluated for in vitro antibacterial activity against one of the most common keratitis causing bacteria, Pseudomonas aeruginosa. Additionally, the in vivo efficacy was evaluated on the rabbit’s eye conjunctivitis model. The formulation showed a sustained effect against keratitis; furthermore, the antibacterial activity was comparable with the commercial product.
Highlights
An ocular drug delivery system is considered as challenging and difficult as the human eye is an isolated organ where the delivery of drugs is quite difficult
We developed poloxamer-based thermoresponsive in situ gel forming solutions for the delivery of oxytetracyclin loaded Poly acrylic acid (PAA)-gelatin NPs with the objective to sustain the release of antibiotics for improved therapeutic efficiency
5 mg of oxytetracycline and 10 mg gelatin were dissolved in 1 mL water at 50 ◦C, and the solution was added drop wise to a 4 mL dispersion medium composed of a water—ethanol mixture (1:2) containing 15 mg of PAA and specific amounts of the stabilizer (PVA 2% w/v)
Summary
An ocular drug delivery system is considered as challenging and difficult as the human eye is an isolated organ where the delivery of drugs is quite difficult. The conventional ophthalmic formulations must be administered very frequently to maintain optimum concentration at the site of infection since the rapid turnover of tears and extensive elimination of drugs through nasolacrimal drainage leads to poor bioavailability of ophthalmic drops [1] In conditions such as topical ocular infections, the insufficient antibiotic concentration at the site of infection may lead to bacterial resistance and treatment failure [2]. Oxytetracycline and other tetracycline derivatives have been extensively investigated for anti-protease activity, antimicrobial activity, and anti-angiogenic properties as well as their effects on corneal epithelial cell proliferation [9] These antibiotics have been administered topically in the form of eye drops, ointments, and gels for the treatment of various ocular infections. Due to the unique anatomy and physiology of the eye, various problems including low efficacy and low drug bioavailability have been associated with these topically administered drugs [10]
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