Advancement of Self-Reporting Polymer Nanoparticles for Melanoma Therapy and Biosensing

Abstract

Enzyme inhibitors have emerged as promising therapeutic agents and valuable tools for commercial applications due to their effectiveness. Despite their success, these agents often require delivery vehicles to enhance their efficacy, reduce the effective dose, and enable controlled release. Nanoparticles have been employed as drug carriers, offering not only improved delivery but also additional functionalities such as cellular tracking. Tyrosinase, a multifunctional enzyme, plays a critical role in cellular processes including melanin synthesis. It is closely associated with dermatological conditions such as melanoma, making tyrosinase inhibitors potential candidates for treating such diseases. Tranexamic acid (TXA), widely used to reduce melanin synthesis, has also gained attention as a key raw material for functional melanin-inhibiting cosmetics. In this study, a conjugated polymer with thiophene and fluorene units in its main chain was synthesized, characterized, and subsequently conjugated with TXA to prepare p-(Fle:3-TAl) NPs-TXA. This TXA-conjugated nanoparticle exhibits multiple functionalities. Its inherent electrochemical properties make it an ideal candidate for use in electrochemical sensors to monitor tyrosinase activity and detect tyrosinase-related diseases. Enzyme kinetic analysis revealed a mixed inhibition profile, achieving 60% inhibition of tyrosinase activity. Furthermore, p-(Fle:3-TAl) NPs was administered to melanoma cells, where its fluorescent properties enabled cellular tracking. The nanoparticles demonstrated a 62% reduction in melanin production and a significant decrease in metastatic factors at the gene level and cancer cell viability. These findings highlight the multifunctional capabilities of the designed nanoparticles, showcasing their potential for broader applications in medical research and therapy.