A new era in siRNA drug development is now underway, thanks to advances in RNAi technology. With impeccable expertise, BOC Sciences is committed to providing siRNA drug design and in vivo delivery solutions for drug development, solving our clients' research challenges.
The ability of siRNAs to silence specific genes has generated significant interest in their use as research tools and therapeutic agents for diseases including cancer, infectious diseases, and metabolic disorders. siRNAs for effective delivery to appropriate target cells in vivo are an important component of these siRNA-based applications. Therefore, a variety of non-viral and viral systems are being developed for the delivery of siRNA to the liver, tumors, and other tissues in vivo. To avoid delivery of siRNA to a large number of non-target cells in the liver, researchers have used maleic anhydride to modify the amine groups of amphiphilic poly (vinyl ether), called PBAVE, to form acid-unstable maleic acid bonds. These bonds are cleaved in the acidic environment of endosomes, exposing the drug's amine and activating its endosomal solubility. The delivery vehicle is named siRNA dynamic multi couple to indicate that the siRNA, shielding agent, and targeting ligand are reversibly coupled to the polymer and that the endosomal solubilization properties of the polymer are triggered by its chemical environment.
Fig.1 Schematic showing the siRNA Dynamic PolyConjugate, its cellular uptake, disassembly in the low pH environment of the endosome, and release of the siRNA into the cytoplasm of the target cell. (David B. Rozema, 2007)
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Dynamic polyconjugates utilize pH-sensitive bonds that cleave in acidic endosomal environments, activating endosomal escape mechanisms and enabling efficient cytoplasmic siRNA release for improved gene silencing.
These systems provide modular design flexibility, reversible modification capabilities, reduced cytotoxicity, and triggered activation properties that enhance target-specific delivery while minimizing non-specific interactions.
Targeting ligands are reversibly coupled to the polymer backbone using acid-labile linkages, maintaining shielding during circulation while enabling specific cellular recognition and uptake upon reaching target tissues.
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