Wang Ying, Liu Lin, Zhu Yuanjie, Wang Liangzhe, Yu Deng-Guang, Liu Li-Ying
School of Materials and Chemistry, University of Shanghai for Science and Technology, Shanghai 200093, China.
Naval Medical Center, Naval Medical University, Shanghai 200433, China.
Pharmaceutics. 2023 Oct 31;15(11):2561. doi: 10.3390/pharmaceutics15112561.
Polymers are the backbone of drug delivery. Electrospinning has greatly enriched the strategies that have been explored for developing novel drug delivery systems using polymers during the past two decades. In this study, four different kinds of polymers, i.e., the water-soluble polymer poly (vinyl alcohol) (PVA), the insoluble polymer poly(ε-caprolactone) (PCL), the insoluble polymer Eudragit RL100 (ERL100) and the pH-sensitive polymer Eudragit S100 (ES100) were successfully converted into types of tri-layer tri-polymer core-shell fibers through bi-fluid coaxial electrospinning. During the coaxial process, the model drug metronidazole (MTD) was loaded into the shell working fluid, which was an emulsion. The micro-formation mechanism of the tri-layer core-shell fibers from the coaxial emulsion electrospinning was proposed. Scanning electron microscope and transmission electron microscope evaluations verified the linear morphology of the resultant fibers and their obvious tri-layer multiple-chamber structures. X-ray diffraction and Fourier transform infrared spectroscopy measurements demonstrated that the drug MTD presented in the fibers in an amorphous state and was compatible with the three polymeric matrices. In vitro dissolution tests verified that the three kinds of polymer could act in a synergistic manner for a prolonged sustained-release profile of MTD in the gut. The drug controlled-release mechanisms were suggested in detail. The protocols reported here pioneer a new route for creating a tri-layer core-shell structure from both aqueous and organic solvents, and a new strategy for developing advanced drug delivery systems with sophisticated drug controlled-release profiles.
聚合物是药物递送的核心。在过去二十年中,静电纺丝极大地丰富了利用聚合物开发新型药物递送系统的探索策略。在本研究中,通过双流体同轴静电纺丝成功地将四种不同类型的聚合物,即水溶性聚合物聚乙烯醇(PVA)、不溶性聚合物聚己内酯(PCL)、不溶性聚合物Eudragit RL100(ERL100)和pH敏感聚合物Eudragit S100(ES100)转变为三层三元共聚物核壳纤维。在同轴过程中,将模型药物甲硝唑(MTD)负载到作为乳液的壳层工作流体中。提出了同轴乳液静电纺丝制备三层核壳纤维的微观形成机制。扫描电子显微镜和透射电子显微镜评估证实了所得纤维的线性形态及其明显的三层多腔结构。X射线衍射和傅里叶变换红外光谱测量表明,药物MTD以无定形状态存在于纤维中,并且与三种聚合物基质相容。体外溶出试验证实,三种聚合物可以协同作用,使MTD在肠道中具有延长的缓释特性。详细阐述了药物控释机制。本文报道的方案开创了一种从水性和有机溶剂中制备三层核壳结构的新途径,以及一种开发具有复杂药物控释特性的先进药物递送系统的新策略。