Work

RGD peptide-functionalized micelles loaded with crocetin ameliorate doxorubicin-induced cardiotoxicity

Year: 2025

Type: article

Abstract: Doxorubicin (Dox)-induced cardiotoxicity presents a significant challenge to fully harnessing its chemotherapeutic potential. Crocetin (Cro), a dicarboxylic acid found in the crocus flower and gardenia fruit, has shown remarkable antioxidant and anti-inflammatory activities. However, its poor aqueous solubility and limited cellular uptake severely constrain its further application in treating diseases. In this study, we developed Arg-Gly-Asp (RGD) peptide-decorated nanomicelles delivering Cro to alleviate Dox-induced cardiac injury. The RGD@M(Cro) nanomicelles exhibited excellent aqueous solubility and a drug-loading efficiency of 93.3 %. RGD-decorated micelles could enhance the cellular uptake of Cro in cardiomyocytes and inhibit approximately 60 % of HL-1 cell apoptosis through efficient reactive oxygen species (ROS) scavenging. In a cardiomyopathy mouse model, RGD@M(Cro) substantially reduced cardiac damage and improved cardiac indicators. This study highlights the great potential of RGD-decorated micelles in treating cardiac injury and other diseases. • RGD peptide-decorated Crocetin micelles significantly enhance cellular uptake in cardiomyocytes. • RGD@M(Cro) nanoparticles demonstrated a potent inhibitory effect on Dox-induced apoptosis in cardiomyocytes. • RGD@M(Cro) nanoparticles significantly mitigated Dox-induced cardiotoxicity in vivo.S

Source: International Journal of Pharmaceutics X

DOI: 10.1016/j.ijpx.2025.100326