short interfering RNA-polyethylene glycol-luteinizing hormone-releasing hormone + polyethylenimine

This agent is a targeted nanoparticle-based delivery complex designed for gene silencing in cancer therapy. It consists of **small interfering RNA (siRNA)** covalently conjugated via a **polyethylene glycol (PEG)** linker to a **luteinizing hormone-releasing hormone (LHRH) peptide analogue** (a cancer-targeting ligand). This siRNA-PEG-LHRH conjugate is then complexed with **polyethylenimine (PEI)** via ionic interaction to form polyelectrolyte complex micelles. The formulation is developed to specifically target cancer cells overexpressing the LHRH receptor (for example, ovarian cancer cells), facilitating receptor-mediated endocytosis and intracellular delivery of siRNA for **silencing cancer-relevant genes** such as **vascular endothelial growth factor (VEGF)**. PEI enhances intracellular delivery and endosomal escape, while PEG-LHRH targets the complex to cancer cells. \nMechanism of action: Targeted delivery of siRNA to LHRH receptor-positive tumor cells, leading to selective mRNA degradation (RNA interference) and inhibition of target gene expression. \nPrimary indication: Targeted cancer gene therapy in LHRH receptor–positive tumors (e.g., ovarian cancer). \nStatus: Preclinical/experimental.

Other names

siRNA-PEG-LHRH + PEIsiRNA-PEG-LHRH/polyethylenimineLHRH-targeted siRNA-PEG + PEILHRH–siRNA-PEG/PEI complexLHRH-PEG-siRNA + PEILHRH-PEG-siRNA/polyethyleneimine micelles