Jeong Da In, Lee Song Yi, Kim Sungyun, Jo Su-Min, Yang HeeSeon, You Jieun, Hwang ChaeRim, Huh Ji Won, Choi Yeoung Eun, Jo Wonjun, Choi In-Jeong, Hu Hae-Jin, Baek Seung-Ki, Na Woonsung, Park Jung-Hwan, Cho Hyun-Jong
Department of Pharmacy, Kangwon National University, Chuncheon 24341, Republic of Korea.
Department of Pharmacy, Kangwon National University, Chuncheon 24341, Republic of Korea; Kangwon Institute of Inclusive Technology, Kangwon National University, Chuncheon 24341, Republic of Korea.
Carbohydr Polym. 2025 Sep 15;364:123789. doi: 10.1016/j.carbpol.2025.123789. Epub 2025 May 23.
Separable and dissolvable microneedle array patch based primarily on hyaluronic acid is designed for the topical delivery of baricitinib in alopecia areata (AA) therapy. Locoregional application of a separable microneedle array patch (S-MAP) may avoid the systemic side effects of oral administration and can be administered without pain compared with typical intradermal injections. Baricitinib (which has poor aqueous solubility) is evenly suspended with sodium carboxymethylcellulose. Subsequently, the mixture is blended with other pharmaceutical excipients, such as hyaluronic acid, sucrose, and Tween 80, to fabricate the S-MAP. Crystalline baricitinib transformed into an amorphous state during the drying process, which may have contributed to complete drug dissolution in the aqueous buffer within 60 min. Proper insertion of a baricitinib-loaded S-MAP into porcine skin tissue and mouse skin is demonstrated using optical coherence tomography and near-infrared fluorescence imaging, respectively. Topical administration of the baricitinib-loaded S-MAP system to the AA lesion of mouse models resulted in significantly higher hair growth compared with the control group (S-MAP: 82 % vs. control: 31 %, p < 0.05). These findings suggest that the baricitinib S-MAP system can be used efficiently and safely, while affording pain-free and self-medication properties, for the AA therapy.
主要基于透明质酸设计的可分离且可溶解的微针阵列贴片,用于斑秃(AA)治疗中巴瑞替尼的局部给药。可分离微针阵列贴片(S-MAP)的局部应用可避免口服给药的全身副作用,并且与典型的皮内注射相比,给药时无痛。将巴瑞替尼(其水溶性差)与羧甲基纤维素钠均匀悬浮。随后,将该混合物与其他药用辅料,如透明质酸、蔗糖和吐温80混合,以制备S-MAP。结晶态的巴瑞替尼在干燥过程中转变为无定形状态,这可能有助于药物在60分钟内在水性缓冲液中完全溶解。分别使用光学相干断层扫描和近红外荧光成像证明了负载巴瑞替尼的S-MAP正确插入猪皮肤组织和小鼠皮肤。与对照组相比,将负载巴瑞替尼的S-MAP系统局部给药于小鼠模型的AA病变处,毛发生长显著更高(S-MAP:82%对对照组:31%,p<0.05)。这些发现表明,巴瑞替尼S-MAP系统可有效且安全地用于AA治疗,同时具有无痛和自我给药的特性。