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Squalene-siRNA Conjugate Development

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CD Formulation harnesses the superior properties of squalene to enhance the delivery effectiveness of siRNA through their development services for squalene-siRNA conjugates, addressing the increasingly growing research demands.

About Squalene-siRNA Conjugates

Squalene (SQ), a natural triterpene and precursor in cholesterol synthesis, is recognized for its compatibility with biological systems, making it suitable for use in drug delivery applications. It acts as a foundational element for creating SQ-drug bioconjugates, which can naturally form into nanoparticles (NPs) in water-based environments, eliminating the need for extra carrier substances. In the realm of oligonucleotide conjugation, SQ is regularly equipped to join with the 3' end of siRNA/ASO via thiol-maleimide linkage. The resulting conjugated siRNA is capable of forming nanoparticles autonomously in aqueous settings, presenting innovative opportunities for drug transport strategies.

Explore Our Services for Squalene-siRNA Conjugate Development

Our services for squalene-siRNA conjugates utilize squalene's distinctive properties to boost siRNA delivery efficiency and targeting accuracy. We aim to enhance conjugate stability and cellular uptake, addressing the shortcomings of conventional delivery methods. Additionally, by modulating the chemical modifications of squalene, we have achieved precise control over the release rate of siRNA, enabling smart response across different biological environments.

Modification of Squalene-siRNA Conjugates

Items	Descriptions
Chemical Modification	Chemical modification involves enhancing the affinity of squalene-siRNA conjugates for target molecules by introducing functional groups like hydroxyl, amino, or carboxyl, which adjust their polarity and biocompatibility.
Polymer Grafting	Polymer grafting aims to improve molecular stability within organisms and enhance siRNA load capacity by attaching polymers to the squalene-siRNA, resulting in copolymers.
Fatty Acid Modification	Fatty acid chains can be introduced to increase the lipophilicity of squalene-siRNA conjugates, thereby improving membrane penetration capabilities and optimizing delivery efficiency.
Phosphorylation Modification	Phosphorylation is employed to boost the hydrophilicity of these conjugates, which heightens their solubility and bioavailability within biological environments.
PEGylation	PEGylation incorporates polyethylene glycol, creating long-chain, water-soluble structures that help in reducing immunogenic responses and prolonging the circulation time of the drug.
Cross-linking Modification	Cross-linking modification involves connecting squalene with other biomolecules, thereby creating complex structures that diversify the functionalities of the squalene-siRNA conjugates.

Development of Conjugates

By optimizing the linkage between squalene and siRNA, we enhance its stability and cellular uptake capability. Simultaneously, functional modifications are made to improve targeting specificity. Our services include rigorous purification and characterization, as well as bioactivity assessment, ensuring the development of efficient and safe conjugates that meet the needs of basic and therapeutic research.

Our Workflow of Squalene-siRNA Conjugate Development

Fig.1 Development flowchart of squalene-siRNA conjugates. Fig.1 Flow chart of squalene-siRNA conjugate development. (CD Formulation)

Target RNA

Pinpoint the RNA molecules for targeting, leveraging research and bioinformatics to verify biological significance.

siRNA Crafting

Construct siRNA complementary to target sequences with high precision and performance, employing computational predictions.

Modify Squalene

Add chemical functional groups or fatty acid chains to squalene for improved binding and compatibility with siRNA.

Conjugate Formation

Fuse the modified squalene with siRNA using suitable chemical reactions to create a robust conjugate.

Evaluate Performance

Assess the physicochemical and biological attributes of the conjugate to ensure its efficacy and safety in use.

Our Technology Platforms

Solid-Phase Synthesis	Enzymatic Synthesis
Employ chemical reactions on solid supports for the efficient synthesis of squalene-siRNA conjugates. This approach simplifies subsequent purification, ensuring the product's high purity and yield.	Catalyze the bonding of squalene with siRNA using specific enzymes, leveraging high selectivity and mild conditions to reduce side reactions, thus enhancing the conjugate's biocompatibility and activity.

Advantages of Squalene-siRNA Conjugate Development Services

Squalene-siRNA conjugates leverage squalene's natural properties to significantly enhance the intracellular delivery efficiency of siRNA, improve targeting capabilities, and optimize gene regulation effects.
As a natural component, squalene offers excellent biocompatibility, reducing potential immune responses and ensuring the safety and stability of the conjugate within biological systems.
Our service provides flexible design options tailored to clients' specific requirements, allowing adjustments to the structure and properties of the conjugates to suit various research objectives and application scenarios.
By employing advanced technologies such as solid phase and enzymatic synthesis, we ensure high purity and efficacy of squalene-siRNA conjugates, thereby enhancing the reliability and reproducibility of subsequent experiments.

Published Data

Technology: Development of Squalene-siRNA Conjugate Using Chemical Synthesis Technologies

Journal: International Journal of Pharmaceutics

IF: 5.44

Published: 2021

Results:

Through analysis via SAXS and SANS, researchers found that siRNA-SQ bioconjugates form supramolecular structures approximately 11 nm in size, which connect to create spherical nanoparticles of roughly 130 nm diameter. These siRNA-SQ nanoparticles remain stable in biological environments, engaging with serum components like albumin and low-density lipoproteins. The encapsulation of siRNAs within these squalene nanoparticles ensures high specificity in gene expression modulation and strong colloidal stability, presenting significant potential for gene-targeted therapeutic applications.

Fig.2 Interaction of squalene-siRNA nanoparticles with biological systems. Fig.2 Biological interaction of squalenoyl siRNA nanoparticles. (Caillaud M, et al., 2021)

CD Formulation's development services for squalene-siRNA conjugates leverage the advantageous properties of squalene to boost the delivery efficiency of siRNA, catering to the escalating demands of scientific research. For further information and collaboration, please reach out to us directly.

References

Caillaud M, Gobeaux F, Hémadi M, et al. Supramolecular organization and biological interaction of squalenoyl siRNA nanoparticles. Int. J. Pharm. 2021, 609: 121117.

How It Works

STEP 1

Submit a service request describing your specific research or development need.

STEP 2

We'll email you to provide your quote and confirm order details if applicable.

STEP 3

Execute the project with real-time communication, and deliver the final report promptly.

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