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Title

In vivo distribution and ex vivo permeation of cyclosporine A prodrug aqueous formulations for ocular application
Authors
Rodriguez Aller, Marta Ruth
Guillarme, Davy
El Sanharawi, Mohamed
Behar-Cohen, Francine
Veuthey, Jean-Luc
Gurny, Robert
Published in Journal of Controlled Release. 2013, vol. 170, no. 1, p. 153-159
Abstract Cyclosporine A is a poorly water-soluble, immunosuppressive drug used to treat a variety of ocular diseases. Its limited solubility makes challenging the development of a cyclosporine A-based eye drop for ocular topical application. Based on the prodrug strategy, the practically insoluble cyclosporine A was converted into a freely soluble prodrug. Such a water-soluble prodrug made it possible to develop water-based concentrated eye drops. The prodrug formulations were tested for their ex vivo permeation and in vivo distribution at three concentrations (equivalent to 0.05%, 0.50% and 2.00% w/v cyclosporine A). The ex vivo permeation experiments were performed on corneal and conjunctival epithelia. The in vivo distribution evaluated the total cyclosporine A present in the ocular structures as well as in serum, spleen and cervical lymphatic ganglions. Each prodrug formulation was compared to conventionally used cyclosporine A eye drops at an equivalent concentration. The experimental results showed that the tested eye drops behaved differently. The prodrug formulation was characterized by the following: i) preferential conjunctival penetration, ii) an interesting capacity to create large tissue deposits and iii) a lower risk of systemic complications and immunosuppression. The prodrug aqueous eye drop was demonstrated to be a patient-friendly option for the treatment of ocular diseases requiring high ocular levels of cyclosporine A, pushing the boundaries of the current therapeutic arsenal.
Keywords Cyclosporine A — Water formulation — Prodrug — In vivo distribution — Ex vivo permeation — Eye
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Article (Published version) (837 Kb) - document accessible for UNIGE members only Limited access to UNIGE
Other version: http://linkinghub.elsevier.com/retrieve/pii/S0168365913002381
Structures
Faculté des sciences / Section des sciences pharmaceutiques
Research group Sciences analytiques
Citation
(ISO format) 		RODRIGUEZ ALLER, Marta Ruth et al. In vivo distribution and ex vivo permeation of cyclosporine A prodrug aqueous formulations for ocular application. In: Journal of Controlled Release, 2013, vol. 170, n° 1, p. 153-159. https://archive-ouverte.unige.ch/unige:28616

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Deposited on : 2013-06-17

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