Key Laboratory of Basic and Application Research of Beiyao (Heilongjiang University of Chinese Medicine), Ministry of Education, Harbin 150040, China.
Key Laboratory of Basic and Application Research of Beiyao (Heilongjiang University of Chinese Medicine), Ministry of Education, Harbin 150040, China.
Int J Pharm. 2022 Jul 25;623:121899. doi: 10.1016/j.ijpharm.2022.121899. Epub 2022 Jun 13.
Dissolving microneedles (MNs) are an efficient, safe, and generally painless method for transdermal distribution of poorly permeable medicines. Here, dissolving composite MNs were prepared from sinapine thiocyanate (ST)-loaded gelatin microspheres (GMS) and hyaluronic acid (HA). To immobilize ST in MNs, we used a two-step centrifuging and molding method. When ST-GMS/ST-HA MNs were placed on the skin, they showed extraordinary mechanical strength and dissolved slowly. In vitro, skin implantation ability was assessed with fluorescein isothiocyanate staining, which revealed progressive penetration from the puncture site into deeper tissues. The feasibility of transdermal delivery of ST-GMS/ST-HA MNs in allergic asthma guinea pigs was then determined through in vivo pharmacodynamic and pharmacokinetic tests. The results indicated that ST-GMS/ST-HA MNs, in comparison with the traditional subcutaneous application approach, achieved both high efficiency and continuous release of ST. Therefore, this device is promising for the delivery ST for allergic asthma therapy.
溶解微针 (MNs) 是一种高效、安全且通常无疼痛的透皮给药方法，可用于传递通透性差的药物。本研究中，我们使用负载芥子碱硫氰酸盐 (ST) 的明胶微球 (GMS) 和透明质酸 (HA) 制备了溶解复合 MNs。为了将 ST 固定在 MNs 中，我们采用了两步离心和成型方法。当 ST-GMS/ST-HA MNs 置于皮肤上时，它们表现出非凡的机械强度，并且溶解缓慢。体外，通过荧光素异硫氰酸酯染色评估皮肤植入能力，结果显示荧光素从穿刺部位逐渐渗透到更深的组织中。随后，通过体内药效学和药代动力学试验确定了 ST-GMS/ST-HA MNs 在过敏性哮喘豚鼠中的透皮传递的可行性。结果表明，与传统的皮下应用方法相比，ST-GMS/ST-HA MNs 实现了 ST 的高效和持续释放。因此，该装置有望用于传递 ST 治疗过敏性哮喘。
