Abstract
The efficacy of conventional ocular formulations is limited by poor corneal retention and permeation, resulting in low ocular bioavailability. Mucoadhesive chitosan (CS)/ tripolyphosphatesodium (TPP) and chitosan (CS)/ tripolyphosphatesodium (TPP)-alginate (ALG) nanoparticles were investigated for the prolonged topical ophthalmic delivery of ofloxacin. A modified ionotropic gelation method was used to produce ofloxacin-loaded nanoreservoir systems. The ofloxacin-loaded CS/TPP and CS/TPP-ALG nanoparticles were characterized for particle size, morphology, zeta potential, encapsulation efficiency, subsequent release and corneal penetration study. The designed nanoparticles have a particle size from 113.8 nm to 509 nm and zeta potential from 16.2 mV to 40.3 mV and encapsulation efficiency values ranging from 19.7% to 33.1%. Nanoparticles revealed a release during the first hours, followed by a more gradual drug release. The ofloxacin-loading CS/TPP or CS/TPP-ALG NPs developed are pronounced penetration enhancing effect as compared to OFX solution (5-6.5 times). Thus, these nanoparticles have a strong potential for ocular drug delivery.
Highlights
Infections of the eye are caused by a number of different organisms and require effective treatment to avoid further complications and vision loss
We described the preparation of a chitosan nanoparticulate system that is able to incorporate ofloxacin, with appropriate mucoadhesiveness and antimicrobial characteristics for the treatment of ocular infections
Chitosan nanoparticles were produced by inotropic gelation, a method based on the formation of complexes between chitosan and TPP or chitosan and TPPALG, under mild conditions
Summary
Infections of the eye are caused by a number of different organisms and require effective treatment to avoid further complications and vision loss. Systemic treatment is not ideal due to systemic side effects and the low ocular bioavailability of the drug (Duxfield et al, 2016). The eye is a unique organ for drug delivery. According to the eye’s physiology and anatomy, a small percentage of prescription drug was absorbed, because the protection mechanisms, such as tearing, blinking reflex and tears streaming from the eyes, are expelled (Thakur, Kashiv, 2011). About 5% of the eye drugs in the cornea reaches the intraocular tissues, while a major fraction of the instilled dose is often absorbed systemically via the conjunctiva and nasolacrimal duct (Lang, 1995). The more topical aqueous solution and suspension forms after use impair vision
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