Maliba Pharmacy College, Uka Tarsadia University, Surat 394350, India.
Maliba Pharmacy College, Uka Tarsadia University, Surat 394350, India.
Int J Pharm. 2022 Feb 5;613:121414. doi: 10.1016/j.ijpharm.2021.121414. Epub 2021 Dec 22.
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.
载药接触镜可以替代多次滴眼治疗。然而，由于载药（通过浸泡法）摄取率低，并且膨胀和光学性质发生改变，限制了其临床应用，因此将疏水性药物如环孢素载入接触镜非常具有挑战性。为了解决上述问题，在接触镜制造过程中加入氧化石墨烯（GO，具有含氧官能团的大表面积）。这些载有 GO 的接触镜（SM-GO-Cys）和空白接触镜（SM-Cys）分别浸泡在环孢素溶液中。或者，通过在制造过程中添加药物和药物-GO（GO 水平不同）分别制备载药接触镜（DL-Cys-20）和载药-GO 接触镜（DL-Cys-20-GO）。接触角和溶胀数据表明，载有 GO 的接触镜的保水能力增加。由于药物在 GO 片表面的分子分散，光学性能得到显著改善。通过浸泡法（SM-GO-Cys-400n），载有 GO 的接触镜可改善药物摄取和体外释放曲线，这是由于 GO 和药物之间的疏水相互作用。在制造过程中添加环孢素-GO（DL-Cys-20-GO-800n）可显著改善药物释放动力学，由于肿胀增加、药物在 GO 片上的溶解和分子分散增加，导致药物洗脱（在提取和灭菌过程中）更高。眼刺激性和组织病理学研究表明 GO 接触镜的安全性。在兔眼的体内药物释放研究中，与滴眼溶液相比，使用 DL-Cys-20-GO-800n 接触镜可显著提高平均驻留时间（MRT）和曲线下面积（AUC），并降低蛋白黏附值。该研究表明，将 GO 掺入接触镜中可以控制环孢素的释放，并改善镜片的膨胀和透光率特性。
