双层 PLGA/HA 微针系统作为多酚的长效制剂,有效且长期地管理特应性皮炎。
Double-layered PLGA/HA microneedle systems as a long-acting formulation of polyphenols for effective and long-term management of atopic dermatitis.
机构信息
Department of Chemical Engineering, National Cheng Kung University, Tainan, Taiwan.
出版信息
Biomater Sci. 2023 Jul 12;11(14):4995-5011. doi: 10.1039/d3bm00182b.
Atopic dermatitis (AD) is a chronic, relapsing inflammatory disorder that requires long-term treatment to achieve optimal control. Topical corticosteroids or calcineurin inhibitors are the mainstay of treatment, but the safety and efficacy of their daily use remain a concern. Here, we report a double-layered poly(lactic--glycolic acid) (PLGA)/sodium hyaluronate (HA) microneedle (MN) patch as a long-acting formulation for sustained delivery of natural polyphenols, curcumin (CUR) and gallic acid (GA), into the inflamed skin. Upon insertion into the skin, the HA layer is rapidly dissolved within 5 min for triggering GA release; the PLGA tip is embedded into the dermis for sustained release of CUR for 2 months. Initially, CUR and GA are simultaneously released from the MNs to exert synergistic antioxidant and anti-inflammatory effects, thus promptly relieving AD symptoms. After the complete release of GA, the extended CUR release can maintain the improvement obtained for at least 56 days. Our results revealed that compared with the CUR-only MN and untreated AD groups, the administration of CUR/GA-loaded MNs not only rapidly reduced the dermatitis score from Day 2 but also significantly inhibited epidermal hyperplasia and mast cell accumulation, reduced serum IgE and histamine levels, and downregulated reactive oxygen species production in the skin lesions of Nc/Nga mice on Day 56. These findings demonstrated that the double-layered PLGA/HA MN patch can serve as an effective dual-polyphenol delivery system for rapid and long-term management of AD.
特应性皮炎(AD)是一种慢性、复发性炎症性疾病,需要长期治疗才能达到最佳控制效果。局部皮质类固醇或钙调神经磷酸酶抑制剂是治疗的主要手段,但它们的日常使用的安全性和疗效仍令人担忧。在这里,我们报告了一种双层聚(乳酸-乙醇酸)(PLGA)/透明质酸钠(HA)微针(MN)贴片,作为一种长效制剂,用于持续递送至发炎皮肤的天然多酚姜黄素(CUR)和没食子酸(GA)。插入皮肤后,HA 层在 5 分钟内迅速溶解,引发 GA 释放;PLGA 尖端嵌入真皮中,持续释放 CUR 长达 2 个月。最初,CUR 和 GA 同时从 MN 中释放,发挥协同抗氧化和抗炎作用,从而迅速缓解 AD 症状。GA 完全释放后,延长的 CUR 释放可以维持至少 56 天的改善。我们的结果表明,与仅 CUR MN 和未治疗的 AD 组相比,CUR/GA 负载 MN 的给药不仅能迅速从第 2 天降低皮炎评分,而且还能显著抑制表皮增生和肥大细胞积累,降低血清 IgE 和组胺水平,并下调皮肤病变中的活性氧物质产生在 Nc/Nga 小鼠上第 56 天。这些发现表明,双层 PLGA/HA MN 贴片可作为一种有效的双重多酚递送系统,用于快速和长期管理 AD。