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Strategies for Controllable siRNA Delivery in Gene Silencing and Cancer Therapy

Authors: FENG Nana; LIU Yang

DOI: 10.1007/s40843-026-4211-yStatus: Verified Translated Edition
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Key Findings in This Report

• • Endosomal escape efficiency is a critical bottleneck: even with high cellular uptake, siRNA must escape endosomes before lysosomal degradation to achieve functional gene silencing; inefficiencies at this step result in high uptake but weak silencing. • • Carrier-free systems leverage coordination chemistry, molecular self-assembly, or peptide conjugation to achieve stable siRNA delivery and intracellular dissociation, offering a simplified formulation without additional excipients. • • Stimuli-responsive carriers utilize endogenous cues (pH, GSH, enzymes, ATP) or exogenous triggers (light, ultrasound, magnetic fields) to enable spatiotemporally controlled release, enhancing RISC loading and gene silencing efficacy. • • The tumor microenvironment is heterogeneous, presenting variable levels of pH, GSH, and enzymes; therefore, delivery systems must be designed to respond to a combination of cues to ensure robust release across different tumor regions.