Huang Wan-Ying, Hibino Toshiya, Suye Shin-Ichiro, Fujita Satoshi
Department of Frontier Fiber Technology and Science, Graduate School of Engineering, University of Fukui 3-9-1 Bunkyo Fukui 910-8507 Japan
Life Science Innovation Center, University of Fukui Fukui 910-8507 Japan.
RSC Adv. 2021 Feb 2;11(10):5703-5711. doi: 10.1039/d0ra08353d. eCollection 2021 Jan 28.
The development of sustained control drug release for delivering hydrophilic drugs has been challenging due to a burst release. Nanofibers are used as materials that enable efficient drug delivery systems. In this study, we designed drug-encapsulated core-shell nanofibers comprising a hydrophilic core of collagen (Col) incorporated with berberine chloride (BC), an anti-inflammatory and anti-cancer agent used as a model drug, and a hydrophobic shell of poly-l-lactic acid (PLLA). Long-term drug release profiles under both the physiological and hydrolysis-accelerated conditions were measured and analyzed using a Korsmeyer-Peppas kinetics model. We found that the Col/PLLA core-shell fiber achieved a controllable long-term release of the hydrophilic drug incorporated inside the core by the slow degradation of the PLLA shell to prevent the burst release while PLLA monolithic fibers showed early release due to the dissolution of drug and the following rapid hydrolysis of fibers. As shown by the results of Col/PLLA core-shell fiber under a hydrolysis-accelerated condition to promote the release of drugs test, it would provide sustained release over 16 days under physiological conditions. Here, the development of the nanomaterial for the long-term drug release of hydrophilic drugs was achieved, leading to its potential medical application including cancer treatment.
由于突释现象，开发用于递送亲水性药物的持续控释制剂一直具有挑战性。纳米纤维被用作能够实现高效药物递送系统的材料。在本研究中，我们设计了药物包封的核壳纳米纤维，其包含掺入了黄连素（BC）的亲水性胶原（Col）核心，黄连素是一种用作模型药物的抗炎和抗癌剂，以及聚-L-乳酸（PLLA）的疏水性外壳。使用Korsmeyer-Peppas动力学模型测量并分析了生理条件和水解加速条件下的长期药物释放曲线。我们发现，Col/PLLA核壳纤维通过PLLA外壳的缓慢降解实现了核心内亲水性药物的可控长期释放，从而防止突释，而PLLA整体纤维由于药物溶解以及随后纤维的快速水解而呈现早期释放。如Col/PLLA核壳纤维在水解加速条件下促进药物释放试验的结果所示，它在生理条件下可实现超过16天的持续释放。在此，实现了用于亲水性药物长期药物释放的纳米材料的开发，这使其在包括癌症治疗在内的潜在医学应用成为可能。
