Lipid-siRNA Conjugate Development

CD Formulation's Lipid-siRNA conjugate development service optimizes lipid-siRNA couplers for biological research and drug delivery.

What is Lipid-siRNA Conjugate?

Covalent coupling of lipid conjugates enhances siRNA delivery. Cholesterol at the 3' end of the passenger chain is used for hepatic gene silencing, while other lipid derivatives like vitamin E also improve delivery. The in vivo activity of lipid-conjugated siRNAs relies on binding to lipoprotein particles (e.g., HDL and LDL), utilizing endogenous lipid transport systems. Preassembly of cholesterol siRNA with HDL particles enhances liver gene silencing, while cholesterol siRNA alone improves jejunal silencing. Furthermore, LDL siRNA particles are mainly taken up by the liver, whereas HDL siRNA particles are absorbed by the liver, adrenal glands, ovaries, kidneys, and small intestine.

Fig.1 Cholesterol-Conjugated hsiRNAs Load into sEVs. (Biscans A, et al., 2018)

Benefits of Lipid-siRNA Conjugates

• Cationic lipids boost siRNA uptake in challenging cell types via electrostatic attraction.
• Lipid encapsulation protects siRNA, improving its bioavailability and half-life.
• By selecting different lipids and adjusting the formulation, delivery systems can achieve targeted and sustained siRNA release.
• Lipid-siRNA systems enhance efficacy and targeting in combination therapy with other agents.

Explore Our Lipid-siRNA Conjugate Development Services

The preparation of lipid-siRNA couplings through chemical synthesis involves the modification of the siRNA guide strand by introducing neutral and cationic lipids at its 3' and 5' ends, thereby enhancing its biocompatibility and cellular uptake efficiency. Specific methods include esterification reactions and the use of thiol compounds to link lipids to siRNAs, forming stable lipid-siRNA complexes that have potential applications in gene silencing and drug delivery.

General Workflow for Lipid-siRNA Conjugate Development Services

Fig.2 Flow chart of lipid-siRNA conjugate development. (CD Formulation)

• Step 1 - Lipid Synthesis and siRNA Modification

Synthesize the desired lipid and attach it to the 3' and 5' ends of the siRNA to facilitate coupling.

• Step 2 - Complex Preparation

Bind the lipid to siRNA through a chemical reaction to create a stable lipid-siRNA complex.

• Step 3 - Physicochemical Characterization

Evaluate the particle size, ζ-potential, and binding efficiency of the complexes to ensure that their properties meet the necessary requirements.

• Step 4 - Biological Activity

Assess the transfection efficiency and cytotoxicity of the lipid-siRNA complexes.

Advantages of Our Lipid-siRNA Conjugate Development Services

• Lipid-siRNA conjugates have a modular design, allowing adaptation to various experimental conditions, including different lipid structures and siRNA sequences.
• Lipid-siRNA conjugates enhance chemical stability, reducing siRNA degradation risk in vitro.
• Lipid-siRNA conjugates can be synthesized in batches in a lab, ensuring consistency in large-scale studies.

Our Analytical Platforms

Published Data

CD Formulation offers efficient lipid-siRNA conjugate development for researchers, including design, synthesis, modification, characterization, and bioactivity assessment. For more information, please contact us.

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.