School of Materials Science & Engineering, University of Shanghai for Science and Technology, Shanghai 200093, China.
School of Materials Science & Engineering, University of Shanghai for Science and Technology, Shanghai 200093, China.
Eur J Pharm Sci. 2018 Sep 15;122:195-204. doi: 10.1016/j.ejps.2018.07.002. Epub 2018 Jul 3.
Structural nanocomposites that provide fast dissolving drug release profiles are highly in demand in pharmaceutics. In this study, a poorly water-soluble drug such as quercetin or tamoxifen citrate (TC) was selected as a model active pharmaceutical ingredient. Core-shell nanofibers with ultra-thin shells were designed and prepared using modified coaxial electrospinning. Polyvinylpyrrolidone (PVP) K90 or Polycaprolactone (PCL) was selected as core. The drugs and PVP K10 were selected as shell. All types of solutions can be used as the shell fluids in modified coaxial process regardless of their electrospinnability, which means the increasing functional ingredients and unspinnable matrix can be processed. Evaluations via SEM and TEM demonstrated that the core-shell nanofibers had linear morphology with a shell thickness smaller than 100 nm. XRD and FTIR results showed that the model drug was distributed in the polymeric matrix amorphously and that PVP K10 had good compatibility with quercetin or TC. In vitro dissolution tests suggested that the core-shell nanofibers with ultra-thin shells released the loaded cargoes in the dissolution media within 1 min. The present investigation paved a new way for implementing the modified coaxial processes, which can be utilized to fabricate structural nanocomposites with ultra-thin shells for enhancing the fast dissolution of poorly water-soluble drugs.
在药剂学中，具有快速溶解药物释放特性的结构型纳米复合材料有很大的需求。在本研究中，选择了一种难溶于水的药物，如槲皮素或枸橼酸他莫昔芬（TC）作为模型活性药物成分。使用改良同轴静电纺丝设计并制备了具有超薄壳的核壳纳米纤维。选择聚乙烯吡咯烷酮（PVP）K90 或聚己内酯（PCL）作为芯，药物和 PVP K10 作为壳。在改进的同轴工艺中，无论其可纺性如何，都可以选择所有类型的溶液作为壳液，这意味着可以处理更多的功能性成分和不可纺的基质。通过 SEM 和 TEM 评估表明，核壳纳米纤维具有线性形态，壳层厚度小于 100nm。XRD 和 FTIR 结果表明，模型药物以无定形状态分布在聚合物基质中，并且 PVP K10 与槲皮素或 TC 具有良好的相容性。体外溶解试验表明，具有超薄壳的核壳纳米纤维在 1min 内将负载的货物释放到溶解介质中。本研究为实施改良同轴工艺开辟了新途径，可用于制造具有超薄壳的结构型纳米复合材料，以增强难溶性药物的快速溶解。
