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Aptamer-siRNA Conjugate Development

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CD Formulation develops innovative conjugates by combining aptamers with siRNA in the exploration of novel drug delivery systems. Leveraging the unique potential of aptamer-siRNA conjugates, CD Formulation is dedicated to advancing gene-targeting technologies and offering exclusive technical support to customers around the globe.

Why Combine Aptamers with siRNA?

Nucleic acid aptamers are small DNA or RNA segments crafted from random libraries through the SELEX method. With sizes between 6-30 kDa and diameters of 1-2 nm, they have low immunogenicity and flexible structures, ideal for interacting with small targets. Aptamers and siRNAs can form chimeras through covalent attachment or base complementation. Enhancing stability involves applying chemical modifications like changing the 3' and/or 5' ends to guard against hydrolysis, adjusting the 2' position of sugar components, or transforming phosphodiester links into thiophosphodiester ones to boost nuclease resistance.

Fig.1 Designs for Aptamer-siRNA AsiCs.Fig.1 Aptamer-siRNA AsiC designs. (Kruspe S, et al., 2017)

Advantages of Aptamer-siRNA Conjugates

Using siRNA-loaded nanocarriers with nucleic acid aptamers for targeted delivery offers multiple benefits.

  • Nanocarriers linked with aptamers can precisely transport substances to specific cells.
  • By encapsulating siRNA, nanocarriers provide protection against degradation.
  • The delivery of siRNA is improved by nanomaterials, which also extend its presence in the system.
  • For better treatment and imaging at the molecular level, nanomaterials can combine therapeutic elements and diagnostic probes.

Explore Our Services for Aptamer-siRNA Conjugate Development

Biosynthetic Aptamer-siRNA Conjugate Services

Biosynthetic methods typically utilize biological systems for synthesis. The advantage of this approach is its ability to produce molecules with natural post-translational modifications or intricate structures that are challenging to synthesize through conventional chemical methods. However, this process may necessitate longer and more complex production conditions.

Chemical Synthesis of Aptamer-siRNA Conjugates Services

The chemical synthesis method employs chemical reactions to gradually assemble nucleic acid molecules in vitro. This method offers high controllability and stable purity, making it particularly suitable for synthesizing shorter nucleic acid molecules with simpler structures. Additionally, the chemical synthesis technique enables precise modifications at specific sites within the molecular structure, contributing to its widespread use in research and development.

Workflow of Aptamer-siRNA Conjugate Development

Fig.2 Diagram of the Development Process for Aptamer-siRNA Conjugates.Fig.2 Flow chart of aptamer-siRNA conjugate development. (CD Formulation)

  • Aptamer Screening and Optimization

Through a series of in vitro selection techniques, such as SELEX, aptamers with a strong binding affinity for target molecules are screened and structurally modified to enhance binding specificity and stability.

  • siRNA Sequence Design

Design siRNA sequences that are complementary to the target RNA, and evaluate their effectiveness using bioinformatics tools. This approach will ensure that the selected sequences can accurately target and silence the intended genes.

  • Ligation Technology Development

Develop suitable chemical cross-linking methods to effectively link the aptamer to the siRNA, ensuring that the resulting complex possesses the necessary stability and activity in both its physical and chemical properties.

  • Evaluation of Physicochemical Properties

The synthesized aptamer-siRNA complexes are analyzed for their detailed physicochemical properties, including solubility, stability, and particle size distribution, to ensure their suitability for subsequent applications.

Our Technology Platforms

Synthesis Platform Analytical Platform
Our platform utilizes diverse synthetic methods for aptamer-siRNA conjugates, including solid-phase synthesis, enzymatic synthesis for efficiency, and genetic engineering for complex assembly production. CD Formulation employs advanced analytical facilities, including HPLC, NMR, MS, UV-Vis, SEM, IR, TGA, and GC platforms, to monitor the synthesis process and verify the purity and identity of the final product.

Advantages of Aptamer-siRNA Conjugate Development Services

  • Aptamer-siRNA conjugation is designed to be flexible and can target a wide range of molecular targets.
  • Optimized chemical modifications enhance stability and increase persistence in vivo.
  • High binding efficiency and reduced immunogenicity are attributed to its smaller size and flexible structure.
  • The synthesis and testing can be conducted quickly and efficiently using customized processes.
  • Covalent linkage or base complementation is employed to create stable chimeras through advanced technical methods.

Published Data

Technology: Aptamers conjugated with siRNA using chemical synthesis technology

Journal: Chemical Biology & Drug Design

IF: 3.2

Published: 2023

Results:

RNA interference offers significant potential for developing effective cancer therapeutics. Silencing HER2 and its downstream genes with exogenously delivered siRNAs shows promise, but challenges in stability and site-specific delivery must be addressed. Aptamers provide advantages over traditional delivery vectors like antibodies. This paper reviews the development and application of aptamer-siRNA chimeras for HER2 targeting and gene silencing, offering a schematic process for new researchers. A deeper understanding of the HER2 signaling pathway is essential for broader studies aimed at silencing additional genes. The goal is to stimulate further research on aptamer-siRNA chimeras targeting HER2 for effective cancer therapies.

Fig.3 Aptamer-siRNA Hybrids.Fig.3 Aptamer-siRNA chimeras. (Dhanya C R, et al., 2023)

CD Formulation combines cutting-edge technology with the expertise of dedicated scientists to offer you comprehensive support and innovative solutions. Contact us, our team consistently stays updated on the latest experimental findings and research developments.

References

  1. Kruspe S, Giangrande P H. Aptamer-siRNA chimeras: discovery, progress, and future prospects. Biomedicines. 2017, 5(3): 45.
  2. Dhanya C R, Mary A S, Madhavan M. Aptamer-siRNA chimeras: Promising tools for targeting HER2 signaling in cancer. Chem Biol Drug Des. 2023, 101(5): 1162-1180.
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