In vitro uptake and release studies of ocular pharmaceutical agents by silicon-containing and p-HEMA hydrogel contact lens materials.

The in vitro uptake and release behaviour of cromolyn sodium, ketotifen fumarate, ketorolac tromethamine and dexamethasone sodium phosphate with silicon-containing (lotrafilcon and balafilcon) and p-HEMA-containing (etafilcon, alphafilcon, polymacon, vifilcon and omafilcon) hydrogel contact lenses indicated that both drug and material affected the uptake and release behaviour. Rapid uptake and release (within 50 min) was observed for all drugs except ketotifen fumarate which was more gradual taking approximately 5h. Furthermore, the maximum uptake differed significantly between drugs and materials. The highest average uptake (7879+/-684 microg/lens) was cromolyn sodium and the lowest average uptake (67+/-13 microg/lens) was dexamethasone sodium phosphate. Partial release of the drug taken up was observed for all drugs except dexamethasone sodium phosphate where no release was detected. Sustained release was demonstrated only by ketotifen fumarate. Drug uptake/release appeared to be a function of lens material ionicity, water and silicon content. The silicon-containing materials released less drug than the p-HEMA-containing materials. The lotrafilcon material demonstrated less interactions with the drugs than the balafilcon material which can be explained by their different bulk composition and surface treatment.

Ciprofloxacin interaction with silicon-based and conventional hydrogel contact lenses.

PURPOSE: Hydrogel contact lenses can be used as bandage lenses to protect the corneal surface after injury. The use of novel silicon-based hydrogel lens materials as bandage lenses has not gained widespread acceptance. As a first step toward advocating their usefulness as bandage lenses, their interaction with ocular pharmaceuticals must be understood because topical agents are often administered in conjunction with bandage lenses. METHODS: The in vitro uptake and release of ciprofloxacin from silicone-based hydrogel (SH) and conventional pHEMA-based (CH) hydrogel contact lenses was examined by spectrophotometric evaluation of the drug concentration in saline solution. RESULTS: The hydrogel contact lenses tested showed similar drug uptake (average 1800 microg/lens) but different levels of drug release. Multiphoton laser microscopy indicated that ciprofloxacin was distributed throughout the lens thickness, with higher levels of drug at the surface owing to drug precipitation. The drug adsorption onto the lenses was partially reversible. The SH lenses released a lower amount of drug than CH lenses (72 vs. 168 microg/lens). Ionic lenses released less drug than non-ionic lenses (127 vs. 151 microg/lens). CONCLUSIONS: The differences in ciprofloxacin uptake and release between SH and CH materials may not be clinically significant because the amount of drug released from all lenses would be above the MIC(90) of ciprofloxacin for common ocular pathogens. These results indicate that material properties have a significant impact on drug-lens interactions.