Controllable release of pirfenidone by polyvinyl alcohol film embedded soft contact lenses in vitro and in vivo.
Controllable release of pirfenidone by polyvinyl alcohol film embedded soft contact lenses in vitro and in vivo.
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DOI：
10.1080/10717544.2021.1895911
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发表时间：
2021-12
期刊：
影响因子：
6
通讯作者：
Yang Y
中科院分区：
文献类型：
--
作者：
Wu C;Or PW;Chong JIT;K Pathirage Don IK;Lee CHC;Wu K;Yu M;Lam DCC;Yang Y
目的：提高聚乙烯醇(PVA)薄膜包埋软性接触镜(SCL)中吡非尼酮(PFD)的载药量，并评价其体内外缓释作用。在312 nm波长处用紫外-可见分光光度计测载药率、体外释药情况以及体外释药参数和外界环境对释药效果的影响。用转化的人角膜上皮细胞体外评价SCLS的安全性。通过光学相干断层扫描和兔眼前段组织学检查来确定体内的安全性。用超高效液相色谱法测定泪液和房水中药物的释放度。SCLS表面光滑，适合实验兔使用。PVA膜和SCL膜的载药量分别为153.515 μg ± 12.508和127.438 μg ± 19.674，PVA膜的PFD显著高于SCL膜(p=0.006)，接近靶向载药量150 μg。SCLS的厚度、PVA的相对分子质量、PVA的用量对药物的体外释放有显著影响。PVA膜厚度和SCLS中载药量对体外释药没有影响。在体内外均安全，在泪液和房水中均可检测到12 h左右的药物释放，各时间点的药物浓度均高于滴眼液，而滴眼液中PFD的含量低于滴眼液。载药PVA膜包埋SCLS有望成为一种很有前途的眼部给药系统。
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 in vitro and in vivo. Drug loading efficiency within PVA film and SCLs, drug release from SCLs in vitro, and the effects of parameters of SCLs and external environment on drug release in vitro were evaluated by ultraviolet–visible spectrophotometer at 312 nm. Safety of SCLs was evaluated in vitro by transformed human corneal epithelial cell. Safety in vivo 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 (p=.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 in vitro significantly. Thickness of PVA film and amount of drug in SCLs had no effect on drug release rate in vitro. SCLs were safe in vitro and in vivo, 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.
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