Research Institute for Biomaterials, Tech Institute for Advanced Materials, College of Materials Science and Engineering, Suqian Advanced Materials Industry Technology Innovation Center, NJTech-BARTY Joint Research Center for Innovative Medical Technology, Nanjing Tech University, Nanjing, China.
State Key Laboratory of Mechanics and Control of Mechanical Structures, Nanjing University of Aeronautics and Astronautics, Nanjing, China.
J Pharm Sci. 2023 Sep;112(9):2506-2515. doi: 10.1016/j.xphs.2023.04.007. Epub 2023 Apr 16.
Microneedles (MNs) are particularly attractive for transdermal administration because of the improved safety, patient compliance and convenience. Dissolving MNs could provide rapid transdermal delivery, but with relatively low mechanical strength and almost no sustainability. On the other hand, hydrogel MNs are complicated to fabricate and have risk concerns. Herein, we developed a biodegradable MNs array composed of biocompatible silk fibroin and poly(vinyl alcohol) to overcome these limitations. Finite element analysis was employed for parameter optimization. The MNs array fabricated by the optimal parameters and material displayed sufficient mechanical strength to disrupt stratum corneum and formed microchannels for transdermal delivery. Dual-release profile was observed in the MNs array, with rapid release in the beginning, and prolonged release afterward. This release behavior fits Weibull release model and is favorable for topical application. The initial immediate release can quickly deliver active compounds to reach the therapeutic effective concentration and facilitate skin penetration, and the sustained release may supply the skin with active compounds over a prolonged period. This biodegradable MNs array is easy to fabricate, mechanically robust, could eliminate safety concerns, and provide the sustainability and advantage for large-scale production.
微针（MNs）由于其改善的安全性、患者顺应性和便利性，特别适用于经皮给药。溶解型 MNs 可以提供快速的经皮递送，但机械强度相对较低，几乎没有可持续性。另一方面，水凝胶 MNs 制造复杂，存在风险问题。在此，我们开发了一种由生物相容性丝素蛋白和聚乙烯醇组成的可生物降解的 MNs 阵列，以克服这些限制。采用有限元分析进行参数优化。由最佳参数和材料制造的 MNs 阵列具有足够的机械强度，可破坏角质层并形成用于经皮给药的微通道。MNs 阵列中观察到双释放曲线，最初快速释放，随后缓慢释放。这种释放行为符合 Weibull 释放模型，有利于局部应用。初始即刻释放可以快速输送活性化合物以达到治疗有效浓度并促进皮肤渗透，而持续释放可以在较长时间内为皮肤提供活性化合物。这种可生物降解的 MNs 阵列易于制造，机械强度高，可以消除安全问题，并提供可持续性和大规模生产的优势。
