Development of Effective Ocular Preparations of Antifungal Agents

Abstract

In treating ophthalmic mycoses, the ultimate aim is to preserve vision, and this depends on rapid diagnosis and efficient antifungal therapy. Antifungal agents are used both for their superficial action as well as to treat infections of the internal eye. Their clinical efficacy would depend on the concentration achieved in ocular tissue, which, in turn, depends on the molecular mass, route of administration, duration of contact, and ability of the compound to penetrate the eye. Several of these agents have a high molecular mass exceeding 500 Da (such as amphotericin B, natamycin, and ketoconazole), resulting in their poor penetration (even if they are lipophilic in nature). In the present review, we present the physiochemical and pharmacokinetic profile and also the spectrum of antifungal activity of representative antifungal agents recommended for use in treatment of ocular infections. Suitable delivery systems, which can improve the effectiveness of these agents, are suggested as per the nature of each agent. These include liposomes/niosomes, lipid emulsions, nanoparticles including solid lipid nanoparticles, and use of cyclodextrin complexes. The advances made therein, followed by a critical appraisal and suggestions for achieving better therapy as per our expertise, are also included.