Amphiphilic pluronic F68 biomaterial augmented oral bioavailability and anticancer activity of genistein in lung cancer treatment

Abstract

AbstractMany phyto‐based drugs available suffer from adverse effects due to their lack of water solubility and poor bioavailability after oral administration. Genistein (Gen) is a plant‐derived isoflavone that possesses potent bioactive activity, including antioxidant, anti‐inflammatory, proapoptotic, and antiproliferative properties against cancer cells. However, due to its poor aqueous solubility and restricted bioavailability, its potential therapeutic utility is limited. Among various strategies, nanomicelles have played a significant role in enhancing solubility and bioavailability, as well as delivering drugs directly to the site of action. Therefore, our study aims to synthesize SA‐modified PF68 (PF68‐SA) polymer‐based nanomicelles and evaluate their effectiveness in cancer treatment. In brief, the Gen‐loaded PF68‐SA nanomicelles (GNM) were successfully fabricated and characterized by dynamic light scattering (DLS) and transmission electron microscopy (TEM) analysis. In vitro cytotoxicity assays performed on human lung A549 cancer cells showed that GNM exhibited higher anticancer effects compared with bolus Gen. Additionally, the observed maximum concentration (Cmax) for GEN suspension and GNM was 1.53 and 3.21 μg/mL, respectively, indicating that GNM was absorbed faster than the suspension formulation. GNM demonstrated enhanced area under the curve (AUC0−t) (16.5 vs. 6.38), half‐life (t1/2) (3.55 vs. 2.49), and mean residence time (5.52 vs. 4.34) compared with pure GEN suspension. Thus, the observed results clearly indicate an improvement in the anticancer activity and bioavailability of GEN after its administration as a nanomicelles formulation.