PDF(Pubmed)
Abstract：
Hyperpigmentation (HP) is an unfavorable skin disease that typically caused by injury, inflammation, or photoaging and leads to numerous physical and psychological issues in patients. Recently, development and application of natural whitening substances, particularly compound curcumin (CUR), is one of the most prevalent treatments for HP. However, it is still a formidable challenge to improve the percutaneous delivery of CUR due to its inadequate solubility in water and excellent barrier function of skin. To overcome the limitations of conventional delivery and increase the percutaneous absorption of CUR, the efficient delivery of CUR is urgently required. Herein, we developed a new malic acid-sorbitol deep eutectic solvent (MS/DES) gel microneedle loaded with CUR as a transdermal delivery system for HP treatment. The MS/DES gel produces three-dimensional (3D) network structure by self-assembly of hydrogen bond interactions, which conferred the CUR-MS/DES-GMN with sufficient mechanical properties to successfully penetrate skin tissue while also helping to enhance the drug\'s release rate. The CUR-MS/DES-GMN exhibit high biocompatibility and mechanical property in vivo of mice. The zebrafish experiments also show that CUR-MS/DES gel has significant effect of anti-pigmentation. Therefore, the designed CUR-MS/DES-GMN system provides a novel strategy for HP treatment based on self-assembly of naturally molecules.
摘要：
色素沉着（HP）是一种不利的皮肤病，通常由损伤引起，炎症,或光老化并导致患者的许多生理和心理问题。最近,天然美白物质的开发和应用，特别是复方姜黄素（CUR），是HP最普遍的治疗方法之一。然而,由于CUR在水中的溶解度不足和优异的皮肤屏障功能，改善CUR的经皮递送仍然是一个巨大的挑战。为了克服常规给药的局限性，增加CUR的经皮吸收，迫切需要CUR的有效交付。在这里，我们开发了一种新型的苹果酸-山梨醇低共熔溶剂（MS/DES）凝胶微针，该微针载有CUR作为HP治疗的透皮给药系统。MS/DES凝胶通过氢键相互作用的自组装产生三维（3D）网络结构，这赋予了CUR-MS/DES-GMN足够的机械性能，以成功地穿透皮肤组织，同时也有助于提高药物的释放速率。CUR-MS/DES-GMN在小鼠体内表现出高的生物相容性和机械性能。斑马鱼实验还表明CUR-MS/DES凝胶具有显著的抗色素沉着作用。因此,设计的CUR-MS/DES-GMN系统提供了一种基于天然分子自组装的HP治疗新策略。
