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Online InquiryWhat is Peptide-Functionalized Liposome?
The conjugation of peptides with liposomal systems has become a major component of nanomedicine delivery technologies in cancer therapy development. Peptide-modified liposomes are a type of nanomedicine delivery system characterized by the attachment of peptides to the outer layer of liposomes. This modification imparts targeting functionality to liposomes, allowing precise delivery of drugs to tumor sites or other specific cells or tissues. Peptides, being small molecules with specific structures and biological functions, can confer targeting properties to liposomes. In cancer therapy, these peptides are typically designed to target cancer cells, cancerous tissues, or the vascular systems associated with cancer, as these sites often overexpress receptors that interact with these peptides.
Figure 1. Schematic representation of the drug delivery mechanism of functionalized peptide-targeted liposomes. (Sonju, J. J.; et al, 2021)
BOC Sciences' Peptide-Functionalized Liposome Services
In the relentless pursuit of effective therapeutic interventions, the convergence of cutting-edge science and innovative technologies has ushered in a new era of precision medicine. At BOC Sciences, a trailblazer in the field of life sciences, we are proud to introduce our custom peptide-modified liposome service - a transformative solution poised to revolutionize targeted drug delivery. At the heart of our custom peptide-modified liposome service lies a commitment to delivering tailored solutions that address the unique challenges of drug delivery. By harnessing the versatility of liposomal formulations and the specificity of peptide targeting, we empower researchers and pharmaceutical developers to design precision-engineered drug delivery systems finely tuned to their research and development targets.
Types of Peptide Modification Available in BOC Sciences
Types of Peptides | Description | Examples | Price |
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Homing Peptides (HPs) | Homing peptides (HPs), also known as homing peptides, are a class of peptides that bind specifically to tumor cells or tumor microenvironmental factors.HPs have been widely used in the field of drug delivery, and among them, the targeting-active peptide composed of arginine (R)-glycine (G)-aspartate (D) tripeptide (RGD) is the most typical one.RGDs can selectively bind to integrin receptors (αvβ3, αvβ5, and αvβ1), and thus promote the interaction of RGD-modified LPs with extracellular matrix and cell membrane. , αvβ5, and αvβ1) selectively, which in turn prompts RGD-modified liposomes to interact with the extracellular matrix and cell membrane. Further, cyclic RGD peptides (cRGD) bind integrins better than linear RGD peptides. | RGD, cRGD | Inquiry |
Cell-Penetrating Peptides (CPPs) | Cell-penetrating peptides (CPPs) are a class of peptides with small molecular size and short amino acid sequences. They exhibit high affinity to lipid bilayers, and when CPPs bind to the cell membrane, these peptide sequences are responsible for membrane translocation, thereby facilitating the internalization of CPPs into the cells. Transactivator of transcription (TAT) is a peptide discovered from the human immunodeficiency virus (HIV), which contains a rich sequence of arginine residues and exhibits properties similar to CPPs. | Transactivative Transcription Protein (TAT) | Inquiry |
Cell-Penetrating Homing Peptides (CPHPs) | Cell-penetrating homing peptides (CPHPs) possess both cell-targeting and cell-penetrating functionalities. One such peptide is internalizing RGD (iRGD), where "i" denotes internalization. Its amino acid sequence is CRGDKGPDC, capable of actively targeting tumor cells that overexpress integrin αvβ3 receptors and also exhibiting membrane-penetrating abilities. iRGD follows a multi-step tumor targeting mechanism. Initially, the intact peptide binds to the cell surface expressing integrin αvβ3 receptors. Subsequently, it undergoes protein hydrolysis, producing the CRGDK fragment. This fragment exhibits lower affinity to integrin αvβ3 receptors but higher affinity to neuropilin-1, facilitating the transfer of CRGDK from integrin αvβ3 receptors to neuropilin-1, thereby generating membrane-penetrating activity. | iRGD | Inquiry |
Nuclear Localization Signal Peptides | A nuclear localization signal is another form of signal peptide that can be located at any part of a peptide sequence. Typically consisting of 4-8 amino acids and lacking specificity, its function is to assist nuclear proteins in entering the cell nucleus. These peptides can guide drugs into the cell nucleus, thereby enhancing their action inside the cell. For example, the SV40 nuclear localization signal is a commonly used nuclear localization signal peptide. | SV40 | Inquiry |
Aggregation-Prone Peptides | Aggregation-prone peptides have the ability to aggregate under specific conditions and can be used to regulate the morphology and properties of liposomes. For instance, amyloid-like peptides (such as KLVFF) can be utilized to prepare liposomes with specific structures and functions. | Amyloid-like Peptides (eg. KLVFF) | Inquiry |
Receptor-Targeting Peptides | Peptide-functionalized liposomal formulations target a wide range of selective receptors, which are often overexpressed in cancer cells, tissues, or cancerous vascular systems. These peptide targets can be divided into three distinct categories: G protein-coupled receptors (GPCRs), growth factor receptors (GFRs), and integrin receptors (αvβ3, αvβ5). Among these, GPCRs are membrane receptors that are overexpressed in tumor tissues, such as gastrin-releasing peptide (GRP) receptors, gastrin/cholecystokinin (CCK A and CCK B) receptors, somatostatin (SSTR2 or SSTR5) receptors, and neurotensin type 1 receptors (NTS1). The family of growth factor receptors includes epidermal growth factor receptors (EGFR/ErbB/HER). One of the ideal targets in the cancerous vascular system is integrin receptors that are overexpressed on the tumor vascular system and endothelial cells involved in blood vessel formation. | GPCR-targeting peptides, GFR-targeting peptides, and integrin receptor-targeting peptides, etc. | Inquiry |
Applications of Peptide-Modified Liposomes
The application of peptide-modified liposomes encompasses a wide range of strategies for targeted drug delivery and diagnostic imaging in cancer therapy.
Targeted Drug Delivery
Peptide-modified liposomes are tailored to deliver drugs precisely to cancer cells by homing in on specific receptors, thereby minimizing off-target effects and enhancing therapeutic efficacy. Peptides, designed to recognize receptors overexpressed on cancer cells, empower liposomes to deliver drugs selectively to tumor sites, harnessing the potential of personalized medicine to combat cancer.
Enhanced Stability and Efficacy
Peptides incorporated into liposomes shield encapsulated drugs from enzymatic degradation, while the inclusion of cholesterol bolsters structural integrity, ensuring optimal drug delivery and efficacy.
Diagnostic Imaging
Peptide-functionalized liposomes serve as carriers for imaging agents, enabling highly targeted visualization of cancerous tissues, thus facilitating accurate diagnosis across different stages of cancer.
Advantages of Peptide-Functionalized Services from BOC Sciences
Tailored Solutions
BOC Sciences' Custom Peptide-Modified Liposome Service offers unparalleled flexibility and customization, allowing researchers to design drug delivery systems precisely tailored to their therapeutic targets. From peptide design to liposome formulation, each aspect of our service is meticulously optimized to meet the unique requirements of our clients' projects.
Expertise and Collaboration
Backed by over two decades of experience in the pharmaceutical industry, our team of scientists brings unparalleled expertise to every project. We collaborate closely with clients, providing comprehensive support and guidance throughout the development process, from project conception to final delivery. Our commitment to excellence ensures that every project meets the highest standards of quality and efficacy.
Cutting-Edge Technologies
BOC Sciences remains at the forefront of technological innovation, continually investing in state-of-the-art equipment and methodologies to ensure the highest quality results. Our commitment to excellence drives us to explore novel approaches and push the boundaries of drug delivery science, empowering our clients with the tools they need to succeed.
Case Study
Case Study 1 Enhanced Therapeutic Efficacy of Docetaxel through Bi-functional Liposomes Targeting Integrin (α4β1) and Ephrin (EphA2) Receptors in Melanoma Cells
Figure 2. Schematic representation of dual functionalized liposome targets both integrin (α4β1) and ephrin (EphA2) receptors of the melanoma cell. (Sonju, J. J.; et al, 2021)
The study aimed to improve the activity of docetaxel (DTX) in melanoma cells by utilizing dual-targeting peptide-functionalized liposomes. Researchers prepared dual-functional liposomes carrying DTX, targeting both integrin (α4β1) and EphA2 receptors. Two peptide-conjugated lipids, C16-LDV and C16-YSA, were incorporated into three modified liposome formulations: LDV-DX (LDV-conjugated), YSA-DX (YSA-conjugated), and TL-DX (combining LDV and YSA). TL-DX contained docetaxel as the anticancer agent. The study demonstrates the potential of dual-targeting peptide-functionalized liposomes, particularly TL-DX, to enhance the delivery and efficacy of DTX in melanoma treatment. By targeting integrin and EphA2 receptors simultaneously, TL-DX offers a promising approach to improve drug delivery and combat drug resistance in cancer therapy. Further research is warranted to validate these findings and explore the translational potential of this innovative drug delivery system in melanoma and other cancer types.
Case Study 2 Enhanced Anticancer Effect of Dual Peptide-Modified Liposomes
Figure 3. Schematic representation of two receptor-specific peptides, Angiopep-2 and tLyP-1, mediated liposomes and their tumor-targeting delivery mechanism. ( Sonju, J. J.; et al, 2021)
The study aimed to enhance the efficacy of anticancer therapy by utilizing dual-targeting peptide-functionalized liposomes containing a combination of docetaxel (DTX) and siRNA, specifically targeting brain tumors. Researchers conducted a study utilizing dual-peptide-modified liposomes, incorporating docetaxel and siRNA along with two receptor-specific peptides, namely tLyP-1 (targeting neuropilin-1 receptor) and Angiopep-2 (targeting low-density lipoprotein receptor-related protein). These liposomes were designed to target brain tumors and accumulate within the tumor tissue. The study revealed the synergistic delivery of two drugs with different solubility characteristics: a large hydrophilic molecule and a small lipophilic molecule. The former involved endocytosis followed by release from endosomes or lysosomes, while the latter entered through passive diffusion upon release. The peptide-modified liposomes effectively bound to glioma cells, facilitated internalization via receptor-mediated endocytosis, and demonstrated superior efficacy compared to unmodified or singly modified liposomes due to the dual functionality of carrying VEGF siRNA and DTX.
FAQ
1: What are the points of interest of peptide-functionalized liposomes?
Peptide-functionalized liposomes offer numerous preferences. To begin with, they can give profoundly particular focused on conveyance, subsequently decreasing unfavorable impacts on typical cells. Second, they can make strides sedate dissolvability and soundness and improve sedate bioavailability. In addition, peptide-functionalized liposomes can move forward neighborhood conveyance of drugs and encourage medicate discharge inside target cells.
2: How are peptide-functionalized liposomes prepared?
Preparation of peptide-functionalized liposomes regularly includes covalently or non-covalently connecting peptide particles to the surface of liposomes. This may be finished through chemical amalgamation strategies or post-modification of the liposome. Strategies of connecting peptides may incorporate amide bond arrangement, hydrophobic intuitive, or other chemical bond arrangement.
3: What is a Peptide-Functionalized Liposome?
A peptide-functionalized liposome may be a sedate conveyance framework in which liposomes are altered or functionalized to carry peptide atoms. These peptide particles are particular and can be focused on to recognize and bind to particular cell surface receptors or particles.
Reference
- Sonju, J. J.; et al. Peptide-Functionalized Liposomes as Therapeutic and Diagnostic Tools for Cancer Treatment. J Control Release. 2021, 329: 624-644.