Release of N-acetylcysteine and N-acetylcysteine amide from contact lenses.

OBJECTIVE

To investigate the use of contact lenses to release N-acetylcysteine (NAC) and N-acetylcysteine amide (NACA) that have frequently used for the treatment of some eye diseases.

METHODS

Three commercial contact lenses were used: Soflens Multi-Focal, 1-Day ACUVUE TruEye, and Frequency 55. All contact lenses were individually kept for 3 days in 10 mL of 3 mM NAC or NACA solutions in phosphate-buffered saline (PBS). After the loading period, the lenses were removed from the solution and put into 5 mL of PBS for 3 days (static mode). During this period, samples were taken at specified times and analyzed by high-pressure liquid chromatography.

RESULTS

From the release profiles of NAC and NACA, it was found that both NAC and NACA could be released from the lenses within 72 hours. Frequency 55 released 95.9%±2.7% of loaded NAC and 60.0%±2.1% of loaded NACA in 24 hours, whereas 1-Day ACUVUE TruEye released 80.9%±1.2% of loaded NAC and 54.0%±1.9% of loaded NACA and Soflens Multi-Focal released 72.8%±2.8% of loaded NAC and 51.9%±2.3% of loaded NACA during that same period.

CONCLUSIONS

The lenses could achieve the appropriate delivery of drugs during their intended time of wear. The amount of released NACA was less than that of NAC because of the more hydrophobic structure of NACA. According to the power law, the values of the exponential constant n were found to be below 0.5, indicating that the behavior observed was "less Fickian".