Lipid & Cancer Therapy Solutions

Lipids play diverse and critical roles in the development and progression of cancer, and targeting lipid pathways has become a promising strategy for cancer treatment. Lipid-based nanoparticles, liposome encapsulation, lipid metabolism inhibitors, and lipid signaling pathway inhibitors have all been investigated as potential treatments for various cancer types. Among them, the drug delivery system based on lipid nanoparticles and liposome encapsulation is the most widely used in the field of drug discovery. With expertise in lipid chemistry and nanoparticle engineering, BOC Sciences can help advance the field of cancer treatment through innovative lipid nanoparticle-based drug delivery solutions.

Liposomes in Cancer Therapy

Liposomes are the earliest discovered nanodrug carriers, and they are also the most studied and versatile nanodrug carriers and can be used in targeted drug delivery systems. Liposomes are spherical vesicles composed of a phospholipid bilayer with hydrophilic and hydrophobic properties. Due to their amphiphilic characteristics, lipophilic drugs can be encapsulated in phospholipid bilayers or adsorbed on the surface of liposomes, while hydrophilic drugs can be encapsulated by the aqueous interior of vesicles. In addition, liposomes have good biocompatibility and biodegradability due to their phospholipid bilayer structure. In recent years, liposomes have made great progress as carriers of small molecule drugs, peptides, proteins, nucleic acids, etc. As drug carriers, liposomes exhibit targeted delivery, high biocompatibility, biodegradability, easy functionalization, low toxicity and immunogenicity, which greatly improve the sustained release and therapeutic index of drugs.

Fig. 1. Liposomes for drug delivery systems (Int J Mol Sci. 2023, 24(7): 6615).

Based on this, BOC Sciences launched a one-stop liposome solution for cancer therapy. We have the ability to support the synthesis, manufacturing and encapsulation services of a variety of functionalized liposomes, including long-circulating PEGylated liposomes, ligand-functionalized liposomes, stimuli-responsive liposomes for efficient targeted therapy, and advanced cell membrane-coated biomimetic nanocarriers. At the same time, various characteristics that affect the safety of liposomes, including their size, composition, surface charge, stability, etc., can also be obtained in our lipid analysis and characterization services.

Lipid Nanoparticles for Cancer Therapy

Lipid nanoparticles (LNPs) have been widely used in the pharmaceutical industry for decades. Compared with other gene and vaccine delivery systems, lipid nanoparticles are easier to mass-produce, have lower immunogenicity, and can carry larger payloads. This makes them successful carriers for a variety of drugs including small molecule, protein and nucleic acid drugs. Recently, lipid nanoparticles have been in the global spotlight for their role in two approved COVID-19 mRNA vaccines. It effectively facilitates the accurate delivery of mRNA, making lipid nanoparticle technology a cutting-edge technology in vaccine development platforms. In addition to mRNA vaccines, lipid nanoparticles are also widely used in cancer treatment. Currently, data show that anti-tumor treatment accounts for the largest proportion of lipid nanoparticle drug use. Among them, anti-tumor lipid nanoparticle preparations are most used in breast cancer, followed by ovarian cancer and lung cancer. Lipid nanoparticles have multiple therapeutic benefits, making them suitable for drug delivery in cancer treatment:

• Improving bioavailability and selectivity compared to free drug
• Reducing drug toxicity to normal surrounding tissues
• Increasing water solubility of hydrophobic drugs
• Extending drug residence time
• Improving control of drug release

BOC Sciences' lipid nanoparticle development services cover a wide range of capabilities, including lipid selection, nanoparticle formulation and characterization. Our experienced chemists and formulation scientists are dedicated to working closely with customers to design and optimize lipid nanoparticles for specific cancer targets and therapeutics. By leveraging expertise in lipid chemistry and nanoparticle engineering, BOC Sciences can develop custom lipid nanoparticle formulations to meet the unique requirements of each customer's drug development program.

PEGylation of Liposomes

PEGylation provides stealth properties for liposomes, including escaping the mononuclear phagocytic system and prolonging the cycle time that is sensitive to the length and density of PEG. Studies have shown that increasing the percentage of PEG grafted on liposomes (i.e., 2-5 mol%) and using PEG 2000 or PEG 5000 can significantly reduce protein adsorption, phagocytosis and cell adhesion of erythrocytes, lymphocytes and macrophages. Therefore, we also offer a broad range of PEGylated lipid products (DSPE PEG) to support our customers' research needs.

What Can We Offer?

• Surface modification of liposomes with antibodies
• Surface modification of liposomes with folic acid
• Surface modification of liposomes with peptides
• Surface modification of liposomes with aptamers
• Surface modification of liposomes with small molecules
• Surface modification of liposomes with DNA
• Surface modification of liposomes with mRNA
• Surface modification of liposomes with siRNA
• Surface modification of liposomes with oligonucleotides
• Surface modification of liposomes with fluorescent dyes

To achieve optimal drug delivery performance, our scientific team works to optimize the physicochemical properties of lipid nanoparticles to ensure effective drug encapsulation, controlled release and targeted delivery to cancer cells. We are equipped with advanced lipid characterization instruments, such as transmission electron microscopy (TEM), dynamic light scattering (DLS) and fluorescence correlation spectroscopy (FCS), to characterize the particle size distribution, zeta potential, drug loading efficiency and drug release kinetics of lipid nanoparticles.

Reference

1. Fulton, M.D. et al. Liposomes in cancer therapy: how did we start and where are we now. Int J Mol Sci. 2023, 24(7): 6615.