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Peptide-siRNA Conjugate Development

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CD Formulation has extensive experience in delivering high-quality personalized peptide-siRNA conjugates globally. We provide a full range of services for the development and mass production of these conjugates, with various peptide types available for siRNA linkage.

Why Develop Peptide-siRNA Conjugates?

Peptide-siRNA coupling uses peptides to deliver siRNAs and inhibit gene expression. The 20 natural amino acids create diverse combinations, resulting in various 3D structures and properties that enable essential functions like binding to siRNAs, penetrating cell membranes, and targeting cells. These characteristics are vital for precise siRNA delivery, and peptides, as natural biomolecules, can be screened from extensive protein libraries for specific functions.

Fig.1 Peptide-associated nucleic acids as a delivery system. (Hall R, et al., 2021)

Explore Our Peptide-siRNA Conjugate Development Services

Peptide-siRNA Conjugate Synthesis

siRNA oligonucleotides can covalently link to peptides (N-, intermediate, or C-terminal) at various positions (5', middle, or 3') using pre-activated small molecules. These molecules contain functional groups that enable cross-linking through stable or cleavable linkages via various chemical reactions, including photochemical or cycloaddition reactions. Although other coupling methods may be similarly priced, additional modifications may be needed at a higher cost to achieve stable or cleavable linkages in modified peptides and oligonucleotides.

Peptide-siRNA Conjugation Optimization

siRNA and peptide functionalization are produced under strict quality control. Analytical HPLC and MS analyses occur during each development cycle. Depending on the binding chemistry, conjugates undergo buffer exchange and are gel-filtered or centrifuged to remove excess cross-linking reagents and oligonucleotides. They are then processed using size exclusion chromatography (SEC) or reversed-phase HPLC to eliminate excess reagents or isolate and characterize cross-linking products.

We perform independent quality control (QC) and quality assurance (QA) to ensure each coupling meets high standards. Final quantities are verified using UV absorbance at 260 nm, and a dedicated technical account manager will guide your project and keep you updated on its progress.

Peptide-siRNA Conjugate Types

Double-stranded siRNA-peptide conjugates	Single-stranded siRNA-peptide conjugates
Double-stranded siRNA-peptide conjugates provide a stable platform for RNA interference, improving gene silencing efficiency.	Single-stranded siRNA-peptide conjugates enable targeted delivery and reduce non-specific binding interference due to their lightweight structure.

Available Types of Peptides

Cell-Penetrating Peptides (CPPs) - Including hydrophilic CPPs, amphiphilic CPPs, targeted ligand-CPP conjugates, and activatable CPPs.
Endosome-Disrupting Peptides - Such as bee venom peptides.
Targeting Peptides - Peptides with specific affinity for disease-associated biomolecules, including examples like BBN.

General Workflow for Process of Peptide-siRNA Conjugates Development

Fig.2 Process diagram of peptide-siRNA conjugate formation. Fig.2 Flow chart of Peptide-siRNA conjugate development. (CD Formulation)

siRNA Design

Synthesize efficient siRNA molecules that inhibit target gene expression.

Peptide Screening

Design peptide sequences to improve siRNA delivery efficiency and stability.

Conjugation Strategy

Explore stable conjugation methods for peptides and siRNAs that maintain functionality, such as chemical conjugation and bioconjugation techniques.

Conjugation Efficiency

Evaluate conjugates for binding efficiency and stability in vitro, and optimize their structure for peak performance.

Our Technology Platforms

Items	Descriptions
Solid-Phase Synthesis	Peptide-siRNA conjugates can be synthesized efficiently with solid-phase carriers, simplifying purification and enhancing yield and consistency for large-scale production.
Enzymatic Synthesis	Biocatalysts connect peptides to siRNA, ensuring structural biocompatibility. Mild enzymatic conditions reduce biomolecule damage and enhance the final product's biological activity.
Analytical Platforms	Various analytical techniques, such as high-performance liquid chromatography (HPLC) and mass spectrometry (MS), are used to confirm the quality and functionality of Peptide-siRNA conjugates, ensuring the purity and identity of the synthesized product.

Advantages of Peptide-siRNA Conjugate Development Services

A peptide-siRNA conjugate improves targeting to specific cells or tissues with tailored peptide sequences.
The conjugate is modified to improve siRNA stability in vivo and reduce degradation.
The development process allows for the customization of peptide and siRNA sequences and structures to meet targeting needs.
The conjugate design process is simple and scalable, reducing costs.

Published Data

Technology: CPPs conjugated with siRNA using chemical synthesis technology

Journal: Colloids and Surfaces B: Biointerfaces

IF: 5.4

Published: 2015

Results:

The clinical use of siRNA faces hurdles due to ineffective in vivo delivery systems. To address this, a new approach was developed for targeting EphA2-positive tumors, utilizing ultrasound-sensitive nanobubbles (NBs) combined with CPPs. This system traps CPP-siRNA within ephrin-mimicking peptide-modified NBs, masking its penetration until triggered by ultrasound, which releases and activates the CPP-siRNA. Results showed CPP-siRNA/YSA-NBs are about 200 nm, with over 85% siRNA entrapment. Upon ultrasound, 90% of the CPP-siRNA was released, whereas only 1.5% was released without ultrasound. Enhanced uptake was observed in EphA2-positive MCF-7 cancer cells. In mice, systemic CPP-siRNA/YSA-NB administration resulted in tumor targeting, increased c-Myc silencing, and slowed tumor growth, suggesting a promising method for siRNA delivery.

Fig.3 YSA-modified nanobubbles carrying cell-penetrating peptide-siRNA conjugates. Fig.3 Cell-penetrating peptide-siRNA conjugate loaded YSA-modified nanobubbles. (Xie X, et al., 2015)

CD Formulation provides a full range of services for Peptide-siRNA Conjugate development, backed by innovative technology and a professional team. Contact us for more information.

References

Hall R, Alasmari A, Mozaffari S, et al. Peptide/lipid-associated nucleic acids (PLANAs) as a multicomponent siRNA delivery system. Molecular Pharmaceutics. 2021, 18(3): 986-1002.
Xie X, Yang Y, Lin W, et al. Cell-penetrating peptide-siRNA conjugate loaded YSA-modified nanobubbles for ultrasound triggered siRNA delivery. COLLOID SURFACE B. 2015, 136: 641-650.

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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