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Cholesterol-siRNA Conjugate Development

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CD Formulation offers versatile cholesterol attachment to oligonucleotides, at any position. Leveraging extensive expertise, we integrate cholesterol into siRNA, ASO, and antagomirs to boost stability and uptake.

Why Cholesterol-siRNA Conjugate?

Cholesterol conjugation with siRNA enhances cellular uptake by enabling these hydrophilic molecules to cross hydrophobic cell membranes more effectively. This modification enables the cholesterol-modified siRNA to interact with HDL and LDL in the body and aids its cellular internalization via cholesterol receptors, therefore boosting uptake efficiency. Additionally, this approach helps to avoid quick renal clearance post-injection, extending the duration of its presence in the bloodstream and enhancing pharmacokinetic properties.

Fig.1 Diagram of siRNA cholesterol conjugation. Fig.1 Scheme of cholesterol conjugation with siRNA. (CD Formulation)

Explore Our Services for Cholesterol-siRNA Conjugate Development

Custom Synthesis of Cholesterol-siRNA Conjugate

CD Formulation offers cholesterol-siRNA conjugates to enhance drug delivery efficiency through cholesterol integration. This modification increases siRNA stability and enhances cellular uptake. When these conjugates bind to cell membranes, they penetrate cells more effectively, improving therapeutic impact and overall drug efficacy.

Cholesterol-siRNA Conjugate Enhancement

Our service enhances siRNA stability and effectiveness by modifying it with cholesterol, improving cell membrane affinity and uptake. We offer an array of ribose and base modifications to refine siRNA function. Options include 2'-OMe, 2'-MOE, 2'-F, LNA, GNA, PMO for ribose, and m6A, m5C, s2U for bases. For the phosphate backbone, we provide PS, PO, PS2, MP, and VP modifications. These enhancements improve siRNA stability and cellular uptake, while reducing in vivo clearance, leading to better therapeutic outcomes.

Our Workflow of Cholesterol-siRNA Conjugate Development

Fig.2 Flow diagram for developing cholesterol-siRNA conjugates. Fig.2 Flow chart of cholesterol-siRNA conjugate development. (CD Formulation)

Chemical Synthesis and Modification

Chemical synthesis is employed to attach the cholesterol moiety to the specified site of the siRNA, along with various ribose and base modifications to enhance stability and biocompatibility.

Purification and Identification

The synthesized products are purified using high-performance liquid chromatography (HPLC) and other methods. Their structures are verified and characterized through mass spectrometry and additional techniques.

Preliminary In Vitro Evaluation

The cellular uptake and stability of the cholesterol-siRNA conjugate were evaluated in a cellular model to assess its preliminary feasibility.

Optimization and Adjustment

Optimize the synthesis strategy and modifications based on the preliminary evaluation results to enhance both effectiveness and efficiency.

Batch Production and Quality Control

Establish a large-scale production process and implement rigorous quality control measures to ensure consistency and high quality in each batch.

Our Technology Platforms

Solid-Phase Synthesis	Enzymatic Synthesis
During solid-phase synthesis, cholesterol and siRNA are sequentially combined on a solid substrate. This platform allows for precise control over the design of sequence-specific siRNAs and the attachment of cholesterol moieties, thereby enhancing drug stability and bioefficacy in vivo.	With enzymatic synthesis, specific enzymes catalyze the binding reaction between cholesterol and siRNA, resulting in a more stable conjugate with high delivery efficiency. This approach allows for the adjustment of the reaction environment to enhance synthesis efficiency.

Advantages of Cholesterol-siRNA Conjugate Development Services

Efficient Cholesterol TEG Conjugates - Our services offer optimized conjugate design to improve the efficacy and stability of siRNA delivery.
Diverse Purification Options - A diverse array of purification specifications, including research-grade and cGMP-grade options, is available to meet the varying needs of experimentation and development.
Team of Experienced Professionals - A team of seasoned professionals ensures efficient project execution and provides technical support.
Strict Quality Control System - Rigorous quality control processes are implemented to ensure the product's high purity and consistency.

Published Data

Technology: Cholesterol-conjugated siRNA via chemical synthesis

Journal: Molecular Therapy

IF: 12.4

Published: 2018

Results:

This study investigates how cholesterol-conjugated siRNAs, along with other lipid conjugates like fatty acids and vitamins, enhance the loading of siRNAs into small extracellular vesicles (sEVs) and improve gene silencing in neurons. Hydrophobicity plays a crucial role in this loading efficiency, with vitamin E-conjugated siRNA showing the highest efficacy in facilitating RNA transport into neurons.

Fig.3 Cholesterol-linked hsiRNAs incorporate into sEVs. Fig.3 Cholesterol-Conjugated hsiRNAs Load into sEVs. (Biscans A, et al., 2018)

CD Formulation's cholesterol-siRNA conjugate service specializes in delivering efficient nucleic acid drug delivery solutions. For collaborations or more information about our services, feel free to get in touch with us.

References

Biscans A, Haraszti R A, Echeverria D, et al. Hydrophobicity of lipid-conjugated siRNAs predicts productive loading to small extracellular vesicles. Mol. Ther. 2018, 26(6): 1520-1528.

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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