Cyclosporine A delivery to the eye: A pharmaceutical challenge

Systemic administration of cyclosporine A (CsA) is commonly used in the treatment of local ophthalmic conditions involving cytokines, such as corneal graft rejection, autoimmune uveitis and dry eye syndrome. Local administration is expected to avoid the various side effects associated with systemic...

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Bibliographic Details
Published in:European Journal of Pharmaceutics and Biopharmaceutics 2003-11, Vol.56 (3), p.307-318
Main Authors: Lallemand, F, Felt-Baeyens, O, Besseghir, K, Behar-Cohen, F, Gurny, R
Format: Article
Language:English
Subjects:
Administration, Topical
Animals
Biological and medical sciences
Cyclosporine - administration & dosage
Cyclosporine - pharmacokinetics
Cyclosporine A
Delivery system
Drug Carriers - administration & dosage
Drug Carriers - pharmacokinetics
Drug Delivery Systems - methods
Eye - drug effects
Eye - metabolism
Eye Diseases - drug therapy
Eye Diseases - metabolism
General pharmacology
Humans
Immunomodulators
Intraocular
Medical sciences
Ocular delivery
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Prodrug
Review
Topical
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Summary:Systemic administration of cyclosporine A (CsA) is commonly used in the treatment of local ophthalmic conditions involving cytokines, such as corneal graft rejection, autoimmune uveitis and dry eye syndrome. Local administration is expected to avoid the various side effects associated with systemic delivery. However, the currently available systems using oils to deliver CsA topically are poorly tolerated and provide a low bioavailability. These difficulties may be overcome through formulations aimed at improving CsA water solubility (e.g. cyclodextrins), or those designed to facilitate tissue drug penetration using penetration enhancers. The use of colloidal carriers (micelles, emulsions, liposomes and nanoparticles) as well as the approach using hydrosoluble prodrugs of CsA have shown promising results. Solid devices such as shields and particles of collagen have been investigated to enhance retention time on the eye surface. Some of these topical formulations have shown efficacy in the treatment of extraocular diseases but were inefficient at reaching intraocular targets. Microspheres, implants and liposomes have been developed to be directly administered subconjunctivally or intravitreally in order to enhance CsA concentration in the vitreous. Although progress has been made, there is still room for improvement in CsA ocular application, as none of these formulations is ideal.
ISSN:0939-6411
1873-3441
DOI:10.1016/S0939-6411(03)00138-3