• 文献标题:   In vitro and in vivo evaluation of cyclosporine-graphene oxide laden hydrogel contact lenses
  • 文献类型:   Article
  • 作  者:   DESAI DT, MAULVI FA, DESAI AR, SHUKLA MR, DESAI BV, KHADELA AD, SHETTY KH, SHAH DO, WILLCOX MDP
  • 作者关键词:   cyclosporine, hydrogel contact lense, graphene oxide, animal studie
  • 出版物名称:   INTERNATIONAL JOURNAL OF PHARMACEUTICS
  • ISSN:   0378-5173 EI 1873-3476
  • 通讯作者地址:  
  • 被引频次:   3
  • DOI:   10.1016/j.ijpharm.2021.121414 EA JAN 2022
  • 出版年:   2022

▎ 摘  要

Drug-eluting contact lens can substitute the multiple eye drop therapy. However, loading hydrophobic drug like cyclosporine in the contact lens is very challenging, due to low drug uptake (via soaking method); and alteration in the swelling and optical properties which restricts its clinical application. To address the above issues, graphene oxide (GO, large surface area with oxygen containing functional groups) was incorporated in the contact lenses during fabrication. These GO-laden contact lenses (SM-GO-Cys) as well as blank contact lenses (SM-Cys) were soaked in the solution of cyclosporine. Alternatively, cyclosporine-laden contact lenses (DL-Cys-20) and cyclosporine-GO-laden contact lenses (DL-Cys-20-GO) were fabricated by adding drug and drug-GO (at various level of GO) during fabrication, respectively. Contact angle and swelling data showed increase in water holding capacity of GO laden contact lenses. Optical property was significantly improved due to molecular dispersion of drug on the surface of GO sheets. The drug uptake and in vitro release profile was improved with GO-laden contact lenses by soaking method (SM-GO-Cys-400n) due to hydrophobic interactions between GO and drug. Adding cyclosporine-GO (DL-Cys-20-GO-800n) during fabrication significantly improved drug release kinetics with higher drug leaching (during extraction and sterilization) due to increased swelling, improved dissolution and molecular dispersion of drug on GO sheets. Ocular irritation and histopathological studies demonstrated the safety of GO-contact lens. The in vivo drug release studies in the rabbit eye showed significant improvement in mean residence time (MRT) and area under the curve (AUC) using DL-Cys-20-GO-800n contact lens compared to eye drop solution with reduction in protein adherence value. The study demonstrated that the incorporation of GO into the contact lens can control the release of cyclosporine as well as improved the lens swelling and transmittance properties.