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Ligand-targeted Delivery for RNAi

RNA interference (RNAi) has been widely applied as a promising therapeutic approach to a number of pathologic conditions. Progress has been made in the investigation of target genes and the development of delivery systems for RNAi. However, challenges remain for the successful clinical application of RNAi-based therapeutics. In terms of the extensive experience in the research of the delivery system for RNAi, Creative Biolabs is devoted to developing effective delivery systems with ligand-targeted gene silencing with low or no toxicity in vivo. Our scientists are pleased to share our cutting-edge technology and extensive expertise to help our clients develop ligand (aptamer, peptide, and antibody)-targeted delivery systems for RNAi.

Ligand-targeted Delivery Systems

Although improvements in the biodistribution of nanoparticles could be acquired, most nanoparticle therapeutics will inevitably be concentrated in the reticuloendothelial organs. However, the therapeutic window of nanoparticles could be increased by targeted delivery to specific tissues, cells, or microenvironments. Targeted delivery can reduce off-target effects and increase the bioavailability of the therapeutic agent at the target site. This targeting ability is usually conferred by adding a ligand to the short dsRNA itself or to the nanoparticle. The molecules most commonly applied as these ligands are described below.

Ligand-targeted Delivery for RNAi

Aptamers are single-stranded short DNAs or RNAs that can specifically bind to various small molecules with high affinity. They are nucleotide analogs of antibodies, which bind with targets in a similar way, in antigen-antibody interactions. Moreover, aptamers are neither immunogenic nor toxic. Thus, they have been widely used for diagnosis and drug delivery. In terms of RNAi delivery, aptamers can facilitate targeted delivery by non-covalent conjugation, forming an aptamer-RNA complex or combination with nanoparticles. A lot of work has been done to explore the potential of aptamer-RNA in cancer treatment. In a recent study, RNA nanoparticles were constructed using anti-prostate-specific membrane antigen RNA aptamer as a targeting ligand and anti-miR-17 or anti-miR-21 as therapeutic modules. After being administered systemically, the complex bonded selectively with the tumor tissue and repressed tumor growth.

Conjugated with siRNA-loaded nanoparticles, peptides can directly be used for targeted delivery of RNAi. Studies have investigated the potential of peptides in siRNA delivery, and most have focused on cyclic Arg-Gly-Asp (RGD) peptides. The receptor of RGD, alpha V/beta integrin, is ubiquitously expressed in tumor endothelial cells and thus offers a potential target. Previous studies have indicated that small interference RNA (siRNA) can be selectively delivered to the tumor site using an RGD-modified liposomal-siRNA system, resulting in a substantial delay in tumor growth.

Owing to their superior stability and specificity, monoclonal antibodies and antibody fragments have attracted much attention as a powerful tool for targeted delivery. The coupling of siRNA against KRAS to anti-EGFR antibodies has been proved to be a promising approach for colon cancer in vitro and in vivo, which provides a novel therapeutic approach for cancer-specific siRNA application and personalized treatment of cancer entities.

Ligand-targeted Delivery for RNAi at Creative Biolabs

By linking specific ligands to nanocarriers, the tumor-specific recognition process could greatly enhance the effect of siRNA. In order to improve the efficiency of delivery systems for RNAi, Creative Biolabs owns lots of scientists who focus on tissue-specific ligands with greater stability and affinity. Our scientists have accumulated extensive experience in the development of ligand-targeted delivery systems for RNAi, including:


Experienced in the development of delivery systems for RNAi and with dedicated commitment to the scientific community, Creative Biolabs has perfected our technical pipelines for ligand-targeted delivery system for RNAi. We would like to share our knowledge and passion in this field to facilitate our clients’ research and project development. Please contact us for more information and a detailed quote.

For Lab Research Use Only, Not for Human or Animal Therapeutic Use.

Other Delivery Method Development Service for RNAi:

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