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Encapsulation and release of zafirlukast from electrospun polyisobutylene-based thermoplastic elastomeric fiber mat
European Polymer Journal ( IF 5.8 ) Pub Date : 2018-01-01 , DOI: 10.1016/j.eurpolymj.2017.11.012
Aditya Jindal , Judit E. Puskas , Andrew McClain , Kyle Nedic , Matthew T. Luebbers , James R. Baker , Bruno Paiva dos Santos , Melissa Camassola , Wayne Jennings , Richard L. Einsporn , Nic D. Leipzig

Abstract This paper reports the discovery that free-standing rubbery fiber mats can be electrospun from polyisobutylene-based thermoplastic elastomer/poly(ethylene glycol) mixtures from a THF-toluene solution. Direct contact and elution cytotoxic assays of these mats showed no cytotoxic response. Electrospinning the polymers mixed with Zafirlukast (ZAF), an anti-inflammatory drug, resulted in complete encapsulation of ZAF into the fibers, without the need of coaxial spinning. Release profiles followed close to a Fickian diffusion model. Significantly, ZAF-eluting fiber mats successfully inhibited the target cysteinyl leukotriene receptors in vitro , known to reduce inflammation. Local application of these mats could have the potential to reduce capsular contracture, the major complication reported for silicone rubber breast prostheses due to inflammatory response. A recent study using a poly(lactic- co -glycolic acid) polymer coating with a similar drug demonstrated capsule thickness reduction in vivo , but suggested that higher doses and slower release rates would be more effective. We believe our slower releasing mats with higher loading could be better at mitigating capsular contracture.

中文翻译:

从电纺聚异丁烯基热塑性弹性纤维垫中包封和释放扎鲁司特

摘要 本文报道了一个发现,即可以从四氢呋喃-甲苯溶液中的聚异丁烯基热塑性弹性体/聚(乙二醇)混合物中电纺自立式橡胶纤维垫。这些垫子的直接接触和洗脱细胞毒性试验显示没有细胞毒性反应。将聚合物与消炎药扎鲁司特 (ZAF) 混合后进行静电纺丝,可将 ZAF 完全封装到纤维中,而无需同轴纺丝。释放曲线遵循接近 Fickian 扩散模型。值得注意的是,ZAF 洗脱纤维垫在体外成功抑制了目标半胱氨酰白三烯受体,已知可减少炎症。这些垫子的局部应用可能有可能减少包膜挛缩,硅橡胶乳房假体报告的主要并发症是由于炎症反应。最近一项使用聚(乳酸-共-乙醇酸)聚合物涂层和类似药物的研究表明,体内胶囊厚度减少,但表明更高的剂量和更慢的释放速度会更有效。我们相信我们的释放速度较慢且负荷较高的垫子可以更好地减轻包膜挛缩。
更新日期:2018-01-01
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