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.
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 Aptamer-siRNA AsiC designs. (Kruspe S, et al., 2017)
Using siRNA-loaded nanocarriers with nucleic acid aptamers for targeted delivery offers multiple benefits.
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.
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.
Fig.2 Flow chart of aptamer-siRNA conjugate development. (CD Formulation)
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.
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.
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.
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.
Synthesis Platform | Analytical Platform |
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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. |
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 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.
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