An antibiotic efficacy comparative study between market-prescribed and solid-lipid fluoroquinolone ophthalmic nanoformulation against conjunctivitis

Abstract

Besifloxacin hydrochloride (BSF) drug substance (DS), is effective against gram-positive and gram-negative microorganisms. BSF (liquid suspension form) is already available in two different market brands: Besivance and Besix. Both of these commercialized drug products (DP) have lower mucoadhesive characteristics, therefore they spend less time in contact with various ocular tissues (cornea and conjunctiva). This research work emphasized the design, development, and optimization of BSF-loaded solid-lipid nanoparticles (BSF@SLN) to increase antibacterial activity by enhancing drug absorption through passive diffusion techniques in the ocular organ compared to conventional dosage forms. The SLN was prepared through a very simple process hot homogenization process using glyceryl monostearate and polysorbate-80 along with poloxamer-188 and water for injection. Various characterization techniques like FTIR, DSC, and XRD were performed to check the compatibility between DS and excipients. The preliminary formulation of SLN was characterized through zeta potential, polydispersity index, and particle size techniques. The developed SLN was optimized following 32 factorial designs. Surface morphology and size of optimized BSF@SLN ophthalmic DP were confirmed by using advanced microscopic techniques such as SEM. In-vitro release of optimized BSF@SLN ophthalmic DP was performed by using two chambers of Franz diffusion cell. Stability studies of optimized BSF@SLN ophthalmic nanoformulations were tested for up to 6 months at 25°C ± 2°C/60% ± 5% RH. The antimicrobial activity of optimized ophthalmic nanoformulation was found 2.76 times more effective compared to the Besix eye drop. In-vivo study of BSF@SLN ophthalmic nanoformulations was carried out with an eye irritancy test and compared with marketed DP (Besix). and found significant pharmacological.