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Title

In vivo distribution and ex vivo permeation of cyclosporine A prodrug aqueous formulations for ocular application

Authors
El Sanharawi, Mohamed
Behar-Cohen, Francine
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 AWater formulationProdrugIn vivo distributionEx vivo permeationEye
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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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