Experimental studies on soft contact lenses for controlled ocular delivery of pirfinedone: in vitro and in vivo
Experimental studies on soft contact lenses for controlled ocular delivery of pirfinedone: in vitro and in vivo
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DOI：
10.1080/10717544.2016.1204570
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发表时间：
2016-11-01
期刊：
影响因子：
6
通讯作者：
Yu, Minbin
中科院分区：
文献类型：
--
作者：
Yang, Mei;Yang, Yangfan;Yu, Minbin
背景：吡非酮(Pirfinedone，PFD)是一种新型药物，具有防止眼睛瘢痕形成的潜力。0.5%PFD滴眼液的生物利用度较低。目的：为了评价软性接触镜(SCL)体内缓释PFD的效果，在体外筛选出最适合用于PFD的人工晶体材料。材料与方法：将11种不同的软性接触镜(-1.00屈光度)分别浸泡在2ml 0.05%的PFD载药液中24小时，使药物完全吸收，然后放置于新鲜的磷酸盐缓冲盐水(PBS)中释放药物。用310 nm紫外法测定PBS中PFD的浓度。然后，将0.00度的多晶硅晶状体浸泡在2ml的0.5%PFD滴眼液中24小时，然后将其放置在新西兰兔的角膜上。结果：PFD对含PHEMA的晶状体有一定的亲和力，在体外，Polymacon晶状体比其他晶状体释放更多的PFD(p<；0.001)。与滴眼剂相比，载药SCL显著延长了PFD在角膜和房水中的滞留时间和浓度，从而提高了PFD的生物利用度。结论：聚乳酸SCL有望成为一种有效的PFD眼部给药载体。
Context: Pirfinedone (PFD) is a novel agent which has the potential to prevent scarring in the eyes. The 0.5% PFD eye drops exhibits poor bioavailability. Whereas, the feasibility of using contact lens as ocular drug delivery device initiated novel possibilities.Objective: To evaluate the delivery of PFD by soft contact lens (SCL) in vivo, we screened the most suitable lens material for PFD among various commercially available SCL materials in vitro.Material and methods: Firstly, 11 different SCLs (-1.00 diopter) were respectively soaked in 2ml of 0.05% PFD-loading solution for 24h to fully absorb drug, and then placed in fresh phosphate buffered saline (PBS) to release the drug. PFD concentration in PBS was determined by ultraviolet absorbance at 310nm. Secondly, by immersing in 2ml of 0.5% PFD eye drops for 24h, the polymacon lens (0.00 diopter) was then placed on the cornea of New Zealand rabbits. PFD concentrations were detected by high performance liquid chromatography (HPLC) in tears, aqueous humor, conjunctiva, cornea, and sclera at different time points.Results: PFD showed some affinity for pHEMA-based lenses and the polymacon lens more slowly released more amount of PFD than any other lens in vitro (p < 0.001). Compared with eye drops, drug-loaded SCLs greatly enhanced the retention time and concentrations of PFD in cornea and aqueous humor and consequently improved the bioavailability of PFD.Conclusion: Polymacon-based SCL is probably a promising vehicle to be an effective ophthalmic delivery system for PFD.