Extended Delivery of Pirfenidone with Novel, Soft Contact Lenses In Vitro and In Vivo
Extended Delivery of Pirfenidone with Novel, Soft Contact Lenses In Vitro and In Vivo
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DOI：
10.1089/jop.2020.0058
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发表时间：
2020-12-09
影响因子：
2.3
通讯作者：
Yang, Yangfan
中科院分区：
文献类型：
--
作者：
Wu, Caiqing;Or, Ping Wai;Yang, Yangfan
目的：本研究的目的是制备吡非尼酮（PFD）负载的软性接触镜（SCL），探讨其特性，并评价其在体外和体内延长PFD的释放效率。测量光学透明度、含水量和蛋白质沉积。转化的人角膜上皮细胞用于测试SCL的细胞毒性。采用紫外-可见分光光度计测定了PFD的体外释药速率。通过观察角膜接触透镜配戴前后对家兔眼表的刺激性来评价SCLs的毒性。用高效液相色谱法测定了30 μ L的0.5%PFD滴眼液和30 μ L的SCLs在兔眼泪液和房水中的PFD浓度随时间的变化。空白SCL的含水量较低（0.548% +/- 0.330），PVA膜加载SCL的含水量有所改善（11.022% +/- 1.508，P = 0.010）。SCL中未发现溶菌酶和人血清白蛋白。体外和体内试验表明，SCLs无明显毒性。与滴眼液相比，载药量约为滴眼液量的1/10时，可使PFD在兔眼泪液和房水中的滞留时间延长5倍以上。结论：载PFD的载药量可显著延长PFD在兔眼的滞留时间，有望成为一种新型的眼部给药系统。
Purpose: The aim of this study was to fabricate pirfenidone (PFD)-loaded soft contact lenses (SCLs), explore their characteristics, and evaluate their efficiency on extended delivery of PFD in vitro and in vivo.Methods: PFD-loaded SCLs were fabricated by embedding an insert of PFD and polyvinyl alcohol (PVA) into 2 layers of silicone elastomer. The optical transparency, water content, and protein deposition were measured. Transformed human corneal epithelial cells were used to test the cytotoxicity of SCLs. The release rate of PFD by SCLs in vitro was evaluated by an ultraviolet-visible spectrophotometer. Toxicity of SCLs was assessed by inspection of ocular surface irritation in rabbits before and after contact lens wear. The concentrations of PFD in tears and aqueous humor of rabbits' eyes as a function of time were determined by high-performance liquid chromatography for SCLs and 30 mu L of 0.5% PFD eye drops.Results: SCLs possessed good light transmittance. Blank SCLs had poor water content (0.548% +/- 0.330), and an improved water content was found in PVA film-loaded SCLs (11.022% +/- 1.508, P = 0.010). No lysozyme and human serum albumin were found in SCLs. There was no significant toxicity of SCLs in vitro and in vivo. SCLs prolonged the residence time of PFD in tears and aqueous humor of rabbit eyes by 5 times compared with the eye drop instillation while around 1/10 of the eye drop dosage was loaded in SCLs.Conclusions: PFD-loaded SCLs can significantly prolong the residence time of PFD and may be a promising ocular drug delivery system.