Department of Biotechnology, Yonsei University, 50 Yonsei-ro, Seoul, 08389, Republic of Korea.
JUVIC Inc., 272 Digital-ro, Seoul, 08389, Republic of Korea.
Adv Healthc Mater. 2021 Apr;10(7):e2001691. doi: 10.1002/adhm.202001691. Epub 2021 Feb 15.
Dissolving microneedles (DMN) supplemented with therapeutic molecules have been developed to enhance transdermal delivery efficiency of topically applied drugs in a minimally invasive manner. However, the dose of the drugs in DMN system is limited owing to the low solubility of drug. In fact, although triamcinolone acetonide (TA) is one of the most widely prescribed drugs for relieving atopic dermatitis (AD), its poor dissolving nature makes it difficult to design and fabricate DMN containing therapeutic dosage of TA. In this study, TA suspension is introduced to encapsulate therapeutic dosage of TA. Sonication and composition optimization of polymers is key to fabricate high dose TA-DMN to induce particle size reduction and dispersion stability of suspension, respectively. After confirming the physical performance of TA-DMN using the selected formulation in vitro, the anti-inflammatory effects of TA-DMN are evaluated in vivo using a mouse model affected with skin inflammation to mimic AD in humans. Herein, high-dose TA-DMN is presented as a candidate agent for relieving AD and, furthermore, for wide application in the treatment of skin inflammatory diseases in which high-dose steroid drugs are required.
已开发出添加治疗分子的溶解微针 (DMN),以微创方式提高局部应用药物的经皮传递效率。然而,由于药物的溶解度低,DMN 系统中的药物剂量受到限制。事实上,尽管曲安奈德 (TA) 是治疗特应性皮炎 (AD) 的最广泛使用的药物之一,但由于其溶解性质差,因此难以设计和制造含有治疗剂量 TA 的 DMN。在这项研究中,引入 TA 混悬液来包封治疗剂量的 TA。超声处理和聚合物组成优化是分别制备高剂量 TA-DMN 以诱导悬浮液的粒径减小和分散稳定性的关键。在用选定的配方在体外确认 TA-DMN 的物理性能后,使用模拟人类 AD 的皮肤炎症的小鼠模型评估 TA-DMN 的抗炎作用。本文提出了高剂量 TA-DMN 作为缓解 AD 的候选药物,并且可广泛应用于需要高剂量类固醇药物治疗的皮肤炎症性疾病。