Yao Yang, Zimu Li, Ping Huang, Jiachan Lin, Jinyuan Li, Kexin Shi, Jiahui Lin, Jingwen Hu, Zhuoxian Zhao, Yongkang Yu, Hongzhong Chen, Xiaowei Zeng, Lin Mei. Rapidly separating dissolving microneedles with sustained-release colchicine and stabilized uricase for simplified long-term gout managementJ. Acta Pharmaceutica Sinica B, 2023, 13(8): 3454-3470. DOI: 10.1016/j.apsb.2023.02.011
Citation: Yao Yang, Zimu Li, Ping Huang, Jiachan Lin, Jinyuan Li, Kexin Shi, Jiahui Lin, Jingwen Hu, Zhuoxian Zhao, Yongkang Yu, Hongzhong Chen, Xiaowei Zeng, Lin Mei. Rapidly separating dissolving microneedles with sustained-release colchicine and stabilized uricase for simplified long-term gout managementJ. Acta Pharmaceutica Sinica B, 2023, 13(8): 3454-3470. DOI: 10.1016/j.apsb.2023.02.011

Rapidly separating dissolving microneedles with sustained-release colchicine and stabilized uricase for simplified long-term gout management

  • Despite growing prevalence and incidence, the management of gout remains suboptimal. The intermittent nature of the gout makes the long-term urate-lowering therapy (ULT) particularly important for gout management. However, patients are reluctant to take medication day after day to manage incurable occasional gout flares, and suffer from possible long-term toxicity. Therefore, a safe and easy-to-operate drug delivery system with simple preparation for the long-term management of gout is very necessary. Here, a chitosan-containing sustained-release microneedle system co-loaded with colchicine and uricase liposomes were fabricated to achieve this goal. This microneedle system was confirmed to successfully deliver the drug to the skin and maintain a one-week drug retention. Furthermore, its powerful therapeutic potency to manage gout was investigated in both acute gouty and chronic gouty models. Besides, the drug co-delivery system could help avoid long-term daily oral colchicine, a drug with a narrow therapeutic index. This system also avoids mass injection of uricase by improving its stability, enhancing the clinical application value of uricase. In general, this two-drug system reduces the dosage of uricase and colchicine and improves the patient's compliance, which has a strong clinical translation.
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