A Comparative Study of Quercetin/Rutin Loaded PEG Polymeric Nanoparticles: Controlled Drug Release and Its Biological Activity

Flavonoids are natural polyphenolic compounds that primarily possess antioxidant properties and play a significant role in opposing various diseases. Current chemotherapeutic approaches are largely ineffective, thus calling for the development of alternative strategies to combat this disease. In this regard, numerous studies have reported the anticancer effect of flavonoids in different types of cancer. To enhance its therapeutic value, polymeric nanoparticles (PEG NPs) represent an ideal delivery system. Further, surface modification of NPs with PEG holds tremendous potential for improving the bioavailability and circulation time of native drugs in the blood. The present study aimed to develop Quercetin/Rutin-loaded PEG polymeric NPs (Qu-PEG/Ru-PEG NPs) with enhanced encapsulation efficiency and sustained drug release. The synthesized Qu-PEG NPs & Ru-PEG NPs were characterized by UV-Vis Spectroscopy, FTIR spectrum, NMR, and XRD and SEM analysis. In-vitro drug release study exhibited a cumulative release of Quercetin & rutin for 24 h at pH 7.4. Further, the polymeric nano-formulations of Quercetin & Rutin showed enhanced antioxidant activity, leading to defense against oxidative stress. In-vitro cellular studies demonstrated that Qu-PEG NPs and Ru-PEG NPs significantly inhibit KB cell proliferation compared to free drugs alone. The current study also showed that Qu-PEG NPs & Ru-PEG NPs enhance intracellular ROS generation compared to the drug alone. Hence, our research findings revealed that successful encapsulation of Quercetin & Rutin in PEG NPs targets the tumor microenvironment and enhances the efficacy of drugs. Based on these preliminary results, flavonoid-loaded polymeric-based NPs might be potential therapeutic molecules against cancer in the future.