Xu Yunli, Li Hongyi
Department of Ophtalmology, 74723Zhenjiang Hospital Affiliated to Nanjing University of Chinese Medicine (Zhenjiang Hospital of Traditional Chinese Medicine), Zhenjiang, Jiangsu Province, 212008, China.
Department of Ophtalmology, 12432Heilongjiang University Hospital, Heilongjiang University, Harbin, Heilongjiang Province, 150080, China.
J Biomater Appl. 2022 Aug;37(2):333-343. doi: 10.1177/08853282221090880. Epub 2022 Apr 28.
Glaucoma is treated by frequent instillation of 0.2% w/v brimonidine tartrate eye drop solution, which showed poor ocular bioavailability of 1-3%. Medicated contact lenses can be used to improve the ocular drug bioavailability. However, drug loading in the contact lens matrix showed high burst release and changes the optophysical properties of the contact lens material. In this paper, a novel brimonidine loaded silica nanoparticles-laden silicone contact lenses (Bri-Si) were designed to achieve controlled drug delivery without altering the optophysical properties of the contact lens. Silica nanoparticles were prepared by polymerizing octadecyltrimethoxysilane (OTMS) molecules at the oil/water interface of microemulsion. Traditional soaking method (Bri-SM), direct brimonidine-loading method (Bri-DL) and microemulsion-laden contact lens (Bri-ME) were developed for comparison. The Bri-Si lens showed improved swelling, transmittance, oxygen permeability and lysozyme adherence compared to Bri-SM, Bri-DL and Bri-ME lenses. The Bri-DL lens showed high brimonidine leaching during extraction and sterilization steps, with low cumulative drug release. While, Bri-Si lens show controlled brimonidine release for 144 h. In a rabbit tear fluid model, the Bri-Si lens showed high brimonidine concentration for 96 h compared to Bri-ME lens and eye drop therapy. Based on histopathological studies of cornea, the Bri-Si lens was found to be safe for human applications. The data demonstrated the novel application of silica nanoparticles to control brimonidine release from the contact lens without altering the optophysical properties of the contact lens.
青光眼通过频繁滴注0.2%（w/v）酒石酸溴莫尼定滴眼液来治疗，该滴眼液的眼部生物利用度较差，仅为1%-3%。药用隐形眼镜可用于提高眼部药物生物利用度。然而，隐形眼镜基质中的药物负载显示出高突释现象，并改变了隐形眼镜材料的光学物理性质。在本文中，设计了一种新型的负载酒石酸溴莫尼定的二氧化硅纳米颗粒的硅水凝胶隐形眼镜（Bri-Si），以实现药物的控释，同时不改变隐形眼镜的光学物理性质。通过在微乳液的油/水界面聚合十八烷基三甲氧基硅烷（OTMS）分子来制备二氧化硅纳米颗粒。开发了传统浸泡法（Bri-SM）、直接负载酒石酸溴莫尼定法（Bri-DL）和负载微乳液的隐形眼镜法（Bri-ME）进行比较。与Bri-SM、Bri-DL和Bri-ME隐形眼镜相比，Bri-Si隐形眼镜在溶胀性、透光率、透氧性和溶菌酶粘附性方面表现更佳。Bri-DL隐形眼镜在提取和灭菌步骤中显示出高的酒石酸溴莫尼定浸出率，累积药物释放量低。而Bri-Si隐形眼镜显示出144小时的酒石酸溴莫尼定控释。在兔泪液模型中，与Bri-ME隐形眼镜和滴眼液疗法相比，Bri-Si隐形眼镜在96小时内显示出高的酒石酸溴莫尼定浓度。基于角膜的组织病理学研究，发现Bri-Si隐形眼镜对人体应用是安全的。数据证明了二氧化硅纳米颗粒在不改变隐形眼镜光学物理性质的情况下控制酒石酸溴莫尼定从隐形眼镜中释放的新应用。
