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J.D. Quintana–Hau, E. Cruz–Olmos, M.I. Lopez–Sanchez, J.R. Gonzalez, L. Baiza–Duran, V. Sanchez–Castellanos, R. Tornero–Montaño; In vitro study of corneal retention of Cyclosporine–A from different formulations . Invest. Ophthalmol. Vis. Sci. 2004;45(13):67.
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© ARVO (1962-2015); The Authors (2016-present)
Purpose: Compare the amount of Cyclosporine–A (CsA) retained in cornea after its topical application under different formulations. Methods: It was compared MODUSIK–A OftenoTM (0.05% and 0.1%) against the RestasisTM (0.05% CsA in castor oil; Allergan, Irvine CA) and MODUSIK–A OftenoTM (0.1%) against 2.0% CsA in olive oil as vehicle. Corneal passive diffusion was evaluated using a side–by–side chamber (Crow Glass Co., Somerville NJ) separated by a fresh cornea from New Zealand white rabbits. Corneal epithelium faced the donor chamber and endothelium faced the receptor chamber. CsA was extracted from the tissue using methanol, and its concentration was determined by HPLC. Results: The total amount of CsA was comparable when 0.05% MODUSIK–A OftenoTM and RestasisTM were used as donors (3.52 µg±1.87 versus 3.61 µg±2.61), but a slight increase of was observed when 0.1% MODUSIK–A OftenoTM was compared to RestasisTM. Also, no differences of CsA amount in cornea was observed when 0.1% MODUSIK–A OftenoTM and 2.0% CsA in olive oil were challenged as donors. Conclusions: These results suggest that 0.05%, 0.1% MODUSIK–A OftenoTM and RestasisTM worked very similar in terms of passive diffusion in cornea. This suggested than MODUSIK–A OftenoTM is a proper aqueous formulation to deliver CsA to the eye. Using 2.0% CsA in olive oil as donor do not improve the corneal CsA amount when it was compare to 0.1% MODUSIK–A OftenoTM. This indicates that cornea has limited passive diffusion capacity for CsA.
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