School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, China.
School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, China.
Int J Pharm. 2018 Jun 10;544(1):100-111. doi: 10.1016/j.ijpharm.2018.04.004. Epub 2018 Apr 5.
In the present work the feasibility of using inner layer-embedded contact lenses (CLs) to achieve sustained release of highly water soluble drug, betaxolol hydrochloride (BH) on the ocular surface was investigated. Blend film of cellulose acetate and Eudragit S100 was selected as the inner layer, while silicone hydrogel was used as outer layer to construct inner layer-embedded contact lenses. Influence of polymer ratio in the blend film on in vitro drug release behavior in phosphate buffered solution or simulated tear fluid was studied and drug-polymer interaction, erosion and swelling of the blend film were characterized to better understand drug-release mechanism. Storage stability of the inner layer-embedded contact lenses in phosphate buffer solution was also conducted, with ignorable drug loss and negligible change in drug release pattern within 30 days. In vivo pharmacokinetic study in rabbits showed sustained drug release for over 240 h in tear fluid, indicating prolonged drug precorneal residence time. In conclusion, cellulose acetate/Eudragit S100 inner layer-embedded contact lenses are quite promising as controlled-release carrier of highly water soluble drug for ophthalmic delivery.
本工作研究了将内层嵌入式隐形眼镜（CL）用于在眼表面实现高水溶性药物盐酸倍他洛尔（BH）持续释放的可行性。选择醋酸纤维素和 Eudragit S100 的共混膜作为内层，而硅水凝胶则用作外层，以构建内层嵌入式隐形眼镜。研究了共混膜中聚合物比例对在磷酸盐缓冲溶液或模拟泪液中的体外药物释放行为的影响，并对药物-聚合物相互作用、共混膜的侵蚀和溶胀进行了表征，以更好地理解药物释放机制。还对内层嵌入式隐形眼镜在磷酸盐缓冲溶液中的储存稳定性进行了研究，在 30 天内药物损失可忽略不计，药物释放模式几乎没有变化。在兔体内药代动力学研究中，在泪液中观察到超过 240 小时的药物持续释放，表明药物在角膜前的滞留时间延长。总之，醋酸纤维素/Eudragit S100 内层嵌入式隐形眼镜作为高水溶性药物的控释载体，非常有希望用于眼部给药。
