Problems in pharmaceutical compounding of eye-drops with cyclosporine A

Cyclosporine A is very effective in treatment of many ophthalmic pathologies like immunological and inflammatory diseases of the cornea, conjunctive or uvea. It is also used to prevent corneal graft rejection and to treat dry eye syndrome. Local ocular administration significantly reduces the risk of systemic side effects. Currently on the market are two products in the form of eye drops: Restasis® (0.05% of cyclosporine) in US and Ikervis® (0.1% of cyclosporine) in the EU. Both are in the form of oil-in-water emulsion. Their availability is still limited and cyclosporine concentration is low. This is a reason that compounded formulations are prepared in hospital and retail pharmacies. The pharmacists do not have an access to the substance and use injectable (50 mg/ml cyclosporine), oral solutions (100 mg/ml cyclosporine) or even oral capsules (25-100 mg/capsule) as the source of cyclosporine. That allows to use of cyclosporine for topical ophthalmic applications in varies formulations, indications, concentration and posology. Due to the fact that cyclosporine is a highly lipophilic and poorly water soluble, it is mostly compounded and administered as an oily solution. Unfortunately, that dosage form is poorly tolerated after administration to the eye, mainly due to the fact of blurring vision commonly observed because of the high viscosity of the oils. However, for many patients use of compounded eye drops with cyclosporine can be the only hope to alleviate the symptoms of the disease, and sometimes even to avoid vision loss. When pharmaceutical compounding of eye drops with cyclosporine, the problem is the presence of auxiliary substances such as, for example, Cremophor, ethanol evaporation, or obtaining the exact dose of the active substance from capsules. This article gives an overview of different approaches for compounding of the cyclosporine eye drops in hospital and retail pharmacies using marketed products off-label. Benefits and the limitations of each method are presented with comments regarding the proper drug compounding.

Abstract licence: CC BY-NC

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