Enhancement in corneal permeability of riboflavin using cyclodextrin derivates complexes as a previous step to transepithelial cross-linking

Corneal cross-linking has been described as an effective treatment to slow the progression of keratoconus. The standard protocol entails corneal epithelial removal allow diffusion riboflavin into stroma. Although, de-epithelization can generate risks or complications that transepithelial tries solve avoid. Different formulations were developed after verifying hydroxypropyl-?-cyclodextrin (HP?CD) and sulfobuthylether-?-cyclodextrin (SBE?CD) in a 20% concentration, increased solubility practically insoluble water drugs such from 0.12 mg/mL 0.35 0.29 respectively. These values higher when chitosan arginine added formulation, showing 0.78 HP?CD concentration was not modified. Ex vivo permeability measured having kept contact bovine corneas with intact epithelium for 5 h 0.1 solution, reproduced nanoemulsion another work. Riboflavin’s cyclodextrins, chitosan, part formulations, compared control drug solution. best coefficient reached combined 40% (w/v) HP?CD, 0.5% (w/w) arginine, chitosan. After carried out toxicity studies opacity (BCOP) He?s Egg Test - Chorioallantoic Membrane (HET-CAM) it verified both, active ingredients excipients different harmful without generating irritation, loss transparency alterations. results show great potential ocular solution their use keratoconus treatment.