A Nanomedicine-Enabled Ion-Exchange Strategy for Enhancing Curcumin-Based Rheumatoid Arthritis Therapy

Angew Chem Int Ed Engl. 2023 Sep 14:e202310061. doi: 10.1002/anie.202310061. Online ahead of print.ABSTRACTCurcumin (Cur) has been clinically used for rheumatoid arthritis treatment by the means of reactive oxygen species (ROS) scavenging and immune microenvironment regulation. However, this compound has a poor water solubility and moderate antioxidative activity, favoring no further broadened application. Metal complexes of curcumin such as zinc-curcumin (Zn-Cur) features enhanced water solubilities, while copper-curcumin (Cu-Cur) shows a higher antioxidant activity but lower solubility than Zn-Cur. Based on their inherent biological properties, this work proposes a nanomedicine-based ion-exchange strategy to enhance the efficacy of Cur for rheumatoid arthritis treatment. Copper silicate nanoparticles with hollow mesoporous structure were prepared to load water-soluble Zn-Cur for constructing a composite nanomedicine, which can degrade in acidic microenvironment of arthritic region, releasing Cu2+ and Zn-Cur. Cu2+ then substitute for Zn2+ in Zn-Cur to form Cu-Cur with a significantly enhanced antioxidative effect, capable of efficiently scavenging ROS in M1 macrophages, promoting their transition to an anti-inflammatory M2 phenotype. In addition, the silicate released after nanocarrier degradation and the Zn2+ released after ion exchange reaction synergistically promote the biomineralization of osteoblasts. This work provides a new approach for enhancing the antiarthritic ef...
Source: Angewandte Chemie - Category: Chemistry Authors: Source Type: research