The purpose of this study was to investigate corneal mucoadhesion, pharmacokinetics in lacrimal fluid and aqueous humor, the immune suppression induced by corneal transplantation of mycophenolate mofetil (MMF) nanosuspensions (NS), and the use of a chitosan-modified MMF nanosuspension (C-NS) as an ophthalmic delivery system. The results indicated that NS had a higher drug concentration in corneal muscoadhesive samples, lacrimal fluid and aqueous humor samples than the MMF ophthalmic suspension. In addition, C-NS had a much higher concentration than the NS. The mean survival time of cornea in corneal allografts was extended remarkably in the NS and C-NS trial groups. The results confirm that the C-NS and NS markedly increase corneal mucoadhesion and drug absorption, prolong the survival time of high-risk allografts, and significantly inhibit corneal immune rejection in a rabbit model of penetrating keratoplasty. In this model, C-NS was more effective than NS.
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