Abstract
Conjunctivitis and endogenous bacterial endophthalmitis mostly occurred after ophthalmic surgery. Therefore, the present study aimed to maximize the ocular delivery of ciprofloxacin (CPX) using colloidal lipid-based carrier to control the post-surgical infection. In this study, CPX was formulated as ophthalmic liposomal drops. Two different phospholipids in different ratios were utilized, including phosphatidylcholine (PC) and dimyrestoyl phosphatidylcholine (DMPC). The physiochemical properties of the prepared ophthalmic liposomes were evaluated in terms of particle size, entrapment efficiency, polydispersity index, zeta potential, and cumulative CPX in-vitro release. In addition, the effect of sonication time on particle size and entrapment efficiency of CPX ophthalmic drops was also evaluated. The results revealed that most of the prepared formulations showed particle size in nanometer size range (460–1047 nm) and entrapment efficiency ranging from 36.4–44.7%. The antibacterial activity and minimum inhibitory concentration (MIC) were investigated. Ex vivo antimicrobial effect of promising formulations was carried out against the most common causes of endophthalmitis microorganisms. The pharmacokinetics of the prepared ophthalmic drops were tested in rabbit aqueous humor and compared with commercial CPX ophthalmic drops (Ciloxan®). Observed bacterial suppression was detected in rabbit’s eyes conjunctivitis with an optimized formulation A3 compared with the commercial ophthalmic drops. CPX concentration in the aqueous humor was above MIC against tested bacterial strains. The in vivo data revealed that the tested CPX drops showed superiority over the commercial ones with respect to peak aqueous humor concentration, time to reach peak aqueous humor concentration, elimination rate constant, half-life, and relative bioavailability. Based on these results, it was concluded that the prepared ophthalmic formulations significantly enhanced CPX bioavailability compared with the commercial one.
Highlights
Ciprofloxacin (CPX) is one of the most effective antibiotics, active against the vast range of infection causing ophthalmic pathogens
This study aims to design CPX loaded colloidal lipid-based carriers to enhance its ocular bioavailability in order to reduce and control surgical site infections after ophthalmic operation
The Polydispersity Index (PDI) and zeta potential values of different CPX-CLBFs formulations were determined as described in the experimental section
Summary
Ciprofloxacin (CPX) is one of the most effective antibiotics, active against the vast range of infection causing ophthalmic pathogens. It blocks the bacterial deoxyribonucleic acid (DNA) synthesis via inhibition of DNA gyrase [1,2]. CPX lipophilicity is high enough to permeate via ocular humors and it is the preferred therapy for intraocular infections [3]. CPX has been proposed for prophylactic use in cases of endogenous bacterial endophthalmitis. In order to prevent bacterial growth, CPX must be delivered at a high concentration to the infected area [7]
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