Antifouling foldable acrylic IOLs loaded with norfloxacin by aqueous soaking and by supercritical carbon dioxide technology

作者：Gonzalez Chomon Clara; Braga Mara E M; de Sousa Herminio C; Concheiro Angel; Alvarez Lorenzo Carmen^*

来源：European Journal of Pharmaceutics and Biopharmaceutics, 2012, 82(2): 383-391.

DOI：10.1016/j.ejpb.2012.07.007

• Foldable IOLs
• Cataracts
• Endophthalmitis
• Norfloxacin controlled release
• Supercritical solvent impregnation/deposition
• Drug-medical device combination product

Cataracts treatment usually involves the extraction of the opaque crystalline lens and its replacement by an intraocular lens (IOL). A serious complication is the occurrence of endophthalmitis, a post-surgery infection mainly caused by Staphylococcus epidermidis, Staphylococcus aureus, and Pseudomonas aeruginosa. IOLs having the ability to load and to release norfloxacin in a controlled way and at efficient therapeutic levels may help to overcome these issues. In this work, acrylic hydrogels combining 2-hydroxyethyl mettmcrylate (HEMA) and 2-butoxyethyl methacrylate (BEM) at various ratios were prepared to attain biocompatible networks that can be foldable even in the dry state and thus insertable through minor ocular incision, and that load therapeutic amounts of norfloxacin. Acrylamide (AAm) and methacrylic acid (MAAc) were also incorporated as functional comonomers in small proportions. Water sorption, contact angle, protein adsorption, and optical properties of the networks were characterized. BEM notably decreased the T-g of the networks, but also the loading by immersion in aqueous solution (presoaking). Then, a scCO(2)-based impregnation/deposition (SSI) method was implemented to improve the uptake of the drug. Loading capacities were discussed in terms of the comonomers composition and the employed method and operational conditions. The networks prepared with HEMA/BEM 20:80 vol/vol and processed with supercritical fluids combine adequate mechanical properties, biocompatibility and norfloxacin loading/release, and seem to be suitable for developing norfloxacin-eluting IOLs.

• 出版日期2012-10