用于增强透皮给药的多孔硅微针,Advanced Therapeutics

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用于增强透皮给药的多孔硅微针
Advanced Therapeutics ( IF 3.7 ) Pub Date : 2022-09-27 , DOI: 10.1002/adtp.202200156
Nazia Tabassum _{1,

2} , Maria Alba ₁ , Li Yan ₁ , Nicolas H. Voelcker _{1,

3}

Affiliation

透皮途径对于小分子和大分子的微创给药很有吸引力。微针 (MN) 因其直接、经济高效且安全的给药方式而特别有前途。但精确控制它们在皮肤内的降解速度仍然是一个挑战。在这里，引入了具有受控降解速率、可调孔隙率、高有效载荷能力和机械稳定性的多孔硅微针 (pSi MNs)，用于生物活性分子的透皮递送。pSi MNs 是通过结合干法和湿法蚀刻方法制造的。通过深反应离子蚀刻创建 MN 后，通过电化学阳极氧化获得多孔表面，产生长度约为 42 µm、尖端直径 < 1 µm 和共形多孔层的 pSi MN。pSi MNs 的生物降解性和机械性能通过改变多孔层的厚度从 1.5 到 4.0 µm 来调整。小分子和大分子药物分子均匀地加载到 pSi MN 阵列的多孔层中。猪组织的离体渗透实验证明使用 pSi MNs 可以有效地经皮递送。具有可调孔隙率、生物降解性和机械强度的新型 pSi MNs 为通过皮肤输送生物治疗药物提供了机会，从而促进了制药科学的创新。

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Porous Silicon Microneedles for Enhanced Transdermal Drug Delivery

The transdermal route is attractive for the minimally invasive administration of small and large molecules. Microneedles (MNs) are particularly promising because of their straightforward, cost-effective, and safe administration. But precise control over their degradation rate within the skin remains a challenge. Here, porous silicon microneedles (pSi MNs) with controlled degradation rate, tunable porosity, high payload capacity, and mechanical stability are introduced for transdermal delivery of bioactive molecules. pSi MNs are fabricated by combining dry and wet etching methods. After creating MNs via deep reactive ion etching, a porous surface is obtained by electrochemical anodization, producing pSi MNs of about 42 µm length, tip diameter < 1 µm, and conformal porous layers. The biodegradability and the mechanical properties of pSi MNs are adjusted by changing the thickness of the porous layer from 1.5 to 4.0 µm. Both small and macromolecular drug molecules are uniformly loaded into the porous layer of the pSi MN arrays. Ex vivo penetration experiments on porcine tissue demonstrate efficient transdermal delivery using pSi MNs. The novel pSi MNs with tunable porosity, biodegradability, and mechanical strength offer opportunities for the delivery of biotherapeutics through the skin, engendering innovations in pharmaceutical sciences.

更新日期：2022-09-27

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