State Key Laboratory of Ophthalmology, Zhongshan Ophthalmic Center, Sun Yat-sen University, Guangzhou, China.
Department of Mechanical and Aerospace Engineering, The Hong Kong University of Science and Technology, Kowloon, Hong Kong.
Drug Deliv. 2021 Dec;28(1):634-641. doi: 10.1080/10717544.2021.1895911.
To increase the amount of pirfenidone (PFD) loaded in polyvinyl alcohol (PVA) film embedded soft contact lens (SCL), and evaluate its function of sustaining delivery of drug and . Drug loading efficiency within PVA film and SCLs, drug release from SCLs , and the effects of parameters of SCLs and external environment on drug release were evaluated by ultraviolet-visible spectrophotometer at 312 nm. Safety of SCLs was evaluated by transformed human corneal epithelial cell. Safety was determined by optical coherence tomography and histology of anterior segment of rabbits. Drug release study in tear fluid and aqueous humor were measured by ultra-performance liquid chromatography. SCLs had smooth surface and were fit for experimental rabbits. Amount of PFD in PVA film and SCLs were 153.515 μg ± 12.508 and 127.438 μg ± 19.674, respectively, PFD in PVA film was significantly higher than SCLs (=.006) and closed to 150 μg (targeting amount of PFD to be loaded). Thickness of SCLs, molecular weight of PVA, and amount of PVA used in SCLs affected drug release significantly. Thickness of PVA film and amount of drug in SCLs had no effect on drug release rate . SCLs were safe and , PFD released from SCLs could be detected around 12 hours in tears and aqueous humor, and the concentration of drug was higher than eye drop at all detected time points while amount of PFD in SCLs was lower than eye drop. Drug loaded PVA film embedded SCLs may be a promising ocular drug delivery system.
为了增加聚维酮（PVA）薄膜中负载的吡非尼酮（PFD）的量，并评估其维持药物输送的功能。通过紫外可见分光光度计在 312nm 处评估了 PVA 薄膜和软隐形眼镜（SCL）中的药物载药量、SCL 中药物释放、SCL 及外部环境参数对药物释放的影响。采用转化人角膜上皮细胞评估 SCL 的安全性。采用光学相干断层扫描和兔眼前节组织学评估安全性。采用超高效液相色谱法测量泪液和房水中的药物释放研究。SCL 表面光滑，适合实验用兔。PVA 薄膜和 SCL 中的 PFD 含量分别为 153.515μg±12.508 和 127.438μg±19.674，PVA 薄膜中的 PFD 明显高于 SCL（=0.006），接近 150μg（目标 PFD 载药量）。SCL 的厚度、PVA 的分子量和 SCL 中 PVA 的用量对药物释放有显著影响。PVA 薄膜的厚度和 SCL 中的药物含量对药物释放速率没有影响。SCL 是安全的，PFD 从 SCL 释放的药物在泪液和房水中可在 12 小时左右检测到，在所有检测时间点的药物浓度均高于滴眼剂，而 SCL 中的 PFD 含量低于滴眼剂。载药 PVA 薄膜嵌入式 SCL 可能是一种有前途的眼部药物传递系统。
