Bhattarai Rajan Sharma, Das Amitesh, Alzhrani Rami M, Kang Dongjin, Bhaduri Sarit B, Boddu Sai H S
College of Pharmacy and Pharmaceutical Sciences, The University of Toledo Health Science Campus, Toledo, OH 43614, USA.
Department of Mechanical, Industrial and Manufacturing Engineering, University of Toledo, Toledo, OH 43606, USA.
Mater Sci Eng C Mater Biol Appl. 2017 Aug 1;77:895-903. doi: 10.1016/j.msec.2017.03.305. Epub 2017 Apr 1.
The purpose of this work was to develop, characterize and compare electrospun nanofiber inserts (ENIs) and solvent cast polymeric inserts (SCIs) for ocular drug delivery.
ENI and SCI of 1%, 5% and 10% w/w dexamethasone were fabricated using a blend of poly-lactic acid (PLA) and poly-vinyl alcohol (PVA). Inserts were characterized for morphology, thickness, pH, drug content, drug crystallinity, in vitro drug release, sterility, dimethylformamide (DMF) and chloroform content, and cytotoxicity.
The thickness of 1%, 5%, and 10% dexamethasone-loaded ENIs were found to be 50μm, 62.5μm, and 93.3μm, respectively, with good folding endurance. SCIs were brittle, with thickness values >200μm. Drug release rates from 1%, 5% and 10% ENIs were found to be 0.62μg/h, 1.46μg/h, and 2.30μg/h, respectively, while those from SCIs were erratic. DMF content in ENIs and SCIs were 0.007% w/w and 0.123% w/w, respectively, while chloroform was not detected. No cytotoxicity was observed from ENIs in cultured bovine corneal endothelial cells for up to 24h.
We conclude that ENIs are better than SCIs and could be utilized as a potential delivery system for treating anterior segment ocular diseases.
本研究旨在开发、表征和比较用于眼部药物递送的电纺纳米纤维插入物（ENIs）和溶剂浇铸聚合物插入物（SCIs）。
使用聚乳酸（PLA）和聚乙烯醇（PVA）的混合物制备1%、5%和10% w/w地塞米松的ENI和SCI。对插入物的形态、厚度、pH值、药物含量、药物结晶度、体外药物释放、无菌性、二甲基甲酰胺（DMF）和氯仿含量以及细胞毒性进行表征。
发现负载1%、5%和10%地塞米松的ENIs的厚度分别为50μm、62.5μm和93.3μm，具有良好的折叠耐受性。SCIs很脆，厚度值>200μm。发现1%、5%和10% ENIs的药物释放速率分别为0.62μg/h、1.46μg/h和2.30μg/h，而SCIs的药物释放速率不稳定。ENIs和SCIs中的DMF含量分别为0.007% w/w和0.123% w/w，未检测到氯仿。在培养的牛角膜内皮细胞中，长达24小时未观察到ENIs的细胞毒性。
我们得出结论，ENIs优于SCIs，可作为治疗眼前段眼部疾病的潜在递送系统。
