Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
9918955 | International Journal of Pharmaceutics | 2005 | 7 Pages |
Abstract
The corneal penetration of CS-088 was significantly enhanced in the presence of EDTA/boric acid by approximately 1.6-fold. The permeability-enhancing effect of EDTA/boric acid was apparently synergistic and concentration-dependent on both EDTA and boric acid. The penetration of FITC-dextran, a paracellular marker, and electrical resistance of corneal membranes were not affected in the presence of EDTA/boric acid. Furthermore, no enhancing effect of EDTA/boric acid was observed in de-epithelialized corneas, although de-epithelialized corneas exhibited a markedly higher permeability of CS-088 that was 24-fold greater than that for intact corneas. In conclusion, EDTA/boric acid synergistically enhances the transcellular permeability of CS-088 in the outer layer but not in the inner layers of the corneal membrane.
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Authors
Takayuki Kikuchi, Masahiko Suzuki, Akira Kusai, Ken Iseki, Hitoshi Sasaki,