Wuya College of Innovation, Shenyang Pharmaceutical University, Wenhua Road No. 103, 110016 Shenyang, China.
Department of Pharmacy, Faculty of Health and Medical Sciences, University of Copenhagen, Universitetsparken 2, DK-2100 Copenhagen, Denmark.
Eur J Pharm Biopharm. 2020 Sep;154:283-289. doi: 10.1016/j.ejpb.2020.06.023. Epub 2020 Jul 4.
The electrospinning process is a promising approach to produce various drug-loaded orodispersible films (ODFs) with a rapid onset of their actions. However, there is only limited number of studies comparing the pharmacological performances of electrospun ODFs (eODFs) with traditional casting films (CFs). In this study, rizatriptan benzoate (RB), a pain relieving agent was formulated with PVP and PVA into ODFs using electrospinning and casting methods. The ODFs were subsequently characterized with respect to their morphology, solid state properties and mechanical characteristics. The uniformity of the dosage units, disintegration behavior and dissolution patterns of the ODFs were also evaluated prior to the pharmacokinetic study. The obtained CFs and eODFs were semitransparent and white in appearance, respectively. The scanning electron microscopy revealed that the eODFs contained nanoporous structure, while the CFs showed no observable pores. RB was amorphously dispersed in both these films without drug-polymer interactions. The uniformity of dosage units for both eODFs and CFs was complied with European Pharmacopeia. As compared to the CFs, the eODFs were more flexible and lesser rigid in nature and showed faster disintegration and dissolution rates. In addition, the eODFs exhibited a higher bioavailability with a shorter T relative to the CFs and commercial RB tablets. This study demonstrated that eODFs were superior to CFs with respect to in vivo pharmacological effects, which could be attributed to the submicron structure of eODFs obtained through the electrospinning process.
电纺工艺是一种很有前途的方法，可以生产具有快速起效作用的各种载药口溶膜（ODF）。然而，仅有少数研究比较了电纺 ODF（eODF）与传统铸膜（CF）的药理学性能。在这项研究中，瑞扎曲坦苯甲酸酯（RB）是一种止痛剂，它与 PVP 和 PVA 一起通过电纺和浇铸的方法被制成 ODF。随后，对 ODF 的形态、固体状态特性和机械特性进行了表征。在进行药代动力学研究之前，还评估了 ODF 单位剂量的均匀性、崩解行为和溶解模式。获得的 CF 和 eODF 分别为半透明和白色外观。扫描电子显微镜显示，eODF 含有纳米多孔结构，而 CF 则没有观察到孔。RB 在这两种膜中均无定形分散，没有药物-聚合物相互作用。eODF 和 CF 的单位剂量均匀性均符合欧洲药典。与 CF 相比，eODF 更具柔韧性和低刚性，崩解和溶解速度更快。此外，与 CF 和市售 RB 片剂相比，eODF 表现出更高的生物利用度，T 相对较短。这项研究表明，eODF 在体内药理学效应方面优于 CF，这可归因于电纺工艺获得的 eODF 的亚微米结构。
