Liposome Encapsulated mRNA

In recent years, the use of messenger RNA (mRNA) as a therapeutic agent has attracted widespread attention, especially in the field of vaccine development. mRNA vaccines, such as Pfizer-BioNTech and Moderna COVID-19 vaccines, have shown remarkable efficacy in preventing infectious diseases. However, the delivery of mRNA therapy poses major challenges, including instability, rapid degradation, and poor cellular uptake. To address these limitations, researchers turned to liposome encapsulation as a promising way to enhance the delivery and efficacy of mRNA therapy. BOC Sciences is a leading provider of custom synthesis and contract research services to the pharmaceutical, biotechnology and academic research communities. With an experienced team of scientists and state-of-the-art facilities, we are well-equipped to support the development of liposome-encapsulated mRNA formulations for a wide range of applications.

What is Liposome-Encapsulated mRNA?

Liposomes are spherical vesicles composed of lipid bilayers that can encapsulate hydrophilic and hydrophobic molecules. These lipid nanoparticles are widely used as drug delivery carriers due to their biocompatibility, biodegradability, and ability to protect active molecules from degradation. When mRNA is encapsulated in liposomes, it is protected from enzymatic degradation and can be effectively delivered to target cells.

Fig. 1. Liposome-based lipid nanoparticles for mRNA delivery (Nat Rev Mater. 2021, 6: 1078-1094).

The liposome encapsulation process of mRNA involves the formation of lipid nanoparticles by self-assembly of lipids in an aqueous environment. The mRNA molecules are then encapsulated in the lipid bilayer or the aqueous core of the liposome. This encapsulation protects mRNA from degradation and promotes its delivery to the cytoplasm of target cells, where it can be translated into the corresponding protein.

Advantages of Liposome-Encapsulated mRNA

• Protecting mRNA from degradation by enzymes and other biological processes.
• Enhancing the stability of mRNA and prolonging its circulation time in the body.
• Improving cellular uptake of mRNA.
• Improving mRNA bioavailability and overall effectiveness.
• Targeted delivery of mRNA to specific tissues or cell types.
• Reducing the immunogenicity of mRNA.
• Improving the safety of mRNA-based therapies.
• Achieving controlled release of mRNA.

Our Liposome-Encapsulated mRNA Services

BOC Sciences' liposome-encapsulated mRNA services cover a comprehensive range of capabilities, including mRNA synthesis, liposome formulation, and in vitro and in vivo characterization. Our team of experts works closely with customers to design and optimize liposome-encapsulated mRNA formulations for their specific therapeutic targets and applications.

mRNA Synthesis Services

One of the key advantages of BOC Sciences' liposome-encapsulated mRNA services is our expertise in mRNA synthesis. Our scientists have extensive experience in the design and synthesis of mRNA molecules with high purity, stability, and translation efficiency. In addition, we also provide a full range of high-quality raw materials for mRNA synthesis, including nucleosides, nucleotides, oligonucleotides, etc. This expertise is critical for the successful development of liposome-encapsulated mRNA formulations, as the quality of the mRNA molecule directly affects the efficacy and safety of the final therapeutic product.

Liposome Formulation Services

In addition to mRNA synthesis, BOC Sciences offers a range of liposome formulation services to encapsulate and protect mRNA molecules. Our scientists are well-versed in lipid selection, preparation of liposome formulations, and optimization of encapsulation efficiency to ensure stability and bioavailability of the mRNA payload. By leveraging our expertise in liposome formulations, BOC Sciences can develop liposome-encapsulated mRNA formulations with customized physicochemical properties, including particle size, surface charge, and stability, to meet the specific requirements of different therapeutic applications.

Lipid Analysis and Characterization

BOC Sciences' liposome-encapsulated mRNA services include comprehensive in vitro and in vivo characterization to evaluate the performance and safety of the developed formulations. Our scientists use a range of analytical techniques, including dynamic light scattering, zeta potential analysis, and transmission electron microscopy, to evaluate the physical properties of liposome-encapsulated mRNA formulations. In addition, in vitro studies were performed to evaluate the cellular uptake, intracellular trafficking, and gene expression efficiency of the encapsulated mRNA molecules in relevant cell lines. BOC Sciences also offers in vivo studies to evaluate the pharmacokinetics, biodistribution and therapeutic efficacy of liposome-encapsulated mRNA formulations in animal models. These studies provide important insights into the in vivo behavior of the agent, including its tissue targeting, systemic circulation, and potential toxicity, to support the development of safe and effective mRNA-based therapeutics.

Our Liposome Preparation Process

• Thin film hydration method
• Detergent removal (depletion) method
• Solvent injection method (ethanol injection method, ether injection method)
• Multiple emulsion method
• Active drug loading method
• Microfluidics
• Supercritical fluid technology
• Reverse-phase evaporation method
• Freeze-drying (lyophilization) method
• Membrane contactor method

Application of Liposome-Encapsulated mRNA

mRNA Vaccine Development

The potential applications of liposome-encapsulated mRNA are diverse and far-reaching. One of the most prominent applications is the development of mRNA vaccines. Liposome encapsulation can significantly enhance the stability and immunogenicity of mRNA vaccines, thereby improving efficacy and efficacy. This has been demonstrated by Pfizer-BioNTech and Moderna COVID-19 vaccines, which use lipid nanoparticles to deliver mRNA encoding the spike protein of SARS-CoV-2 virus.

Fig. 2. Liposome mRNA formulations for COVID-19 vaccines (Nat Rev Mater. 2021, 6: 1078-1094).

Cancer Treatment Development

In addition to vaccines, liposome-encapsulated mRNAs have also shown promise in the treatment of various diseases, including cancer, genetic diseases and infectious diseases. For example, researchers have been exploring the use of mRNA therapy for cancer immunotherapy, in which liposome encapsulation can enhance the delivery of tumor-specific antigens to immune cells, thereby generating an effective anti-tumor immune response. Similarly, in the field of gene therapy, liposome-encapsulated mRNA can be used to deliver therapeutic genes to target cells, providing potential therapeutic methods for genetic diseases such as cystic fibrosis and muscular dystrophy.

Diagnostic Analysis Development

In addition, the use of liposome-encapsulated mRNA is beyond the scope of therapeutic applications. It can also be used to deliver mRNA encoding a variety of proteins, enzymes or antibodies for research, diagnostic or biotechnological purposes. This includes the production of recombinant proteins, the generation of induced pluripotent stem cells, and the development of new diagnostic assays.

Case Study

One success story of BOC Sciences' liposome-encapsulated mRNA services involves the development of a novel mRNA-based vaccine for a viral disease. The client, a biotechnology company, approached BOC Sciences with the goal of developing an efficient and safe mRNA vaccine against a specific virus.

The BOC Sciences team worked closely with customers to design custom liposome encapsulation strategies for this mRNA vaccine. This involves selecting appropriate lipids and optimizing the formulation to ensure efficient encapsulation and delivery of the mRNA to target cells. Through a series of in vitro and in vivo studies, the BOC Sciences team demonstrated that liposome-encapsulated mRNA vaccines are highly effective in inducing strong immune responses in animal models. The vaccine also demonstrated an excellent safety profile with minimal systemic side effects. The client successfully advanced a liposome-encapsulated mRNA vaccine into preclinical and clinical development, which showed promising results in early clinical trials.

FAQ

1. What is the encapsulation efficiency of mRNA in lipid nanoparticles?

The efficiency of encapsulation of mRNA in lipid nanoparticles may vary depending on the specific formulation and manufacturing process used. However, in general, lipid nanoparticles are able to achieve high encapsulation efficiencies for mRNA, often exceeding 90%. This high efficiency is one of the key advantages of using lipid nanoparticles as a delivery system for mRNA-based therapeutics, as it allows successful encapsulation and delivery of a large portion of the mRNA payload to target cells.

2. What are cationic liposomes for RNA delivery?

Cationic liposomes are lipid-based nanoparticles that are positively charged due to the presence of cationic (positively charged) lipids in their structure. These liposomes are used as delivery vehicles for RNA, specifically for the delivery of small interfering RNA (siRNA) and mRNA to target cells. The cationic nature of these liposomes allows them to interact with negatively charged RNA molecules, forming stable complexes that protect the RNA from degradation and facilitate its delivery into cells. Once inside the cell, the cationic liposomes can release the RNA payload, allowing it to exert its therapeutic effect.

3. What is the difference between liposomes and nanoparticles?

Liposomes are small vesicles made of phospholipids that can encapsulate drugs or other substances, while nanoparticles are small particles made of various materials such as lipids, polymers, metals or ceramics. Liposomes are typically made from lipid bilayers and can encapsulate hydrophilic and hydrophobic drugs, while nanoparticles can be made from a variety of materials and can be used to deliver drugs, imaging agents, or other therapeutic substances. Furthermore, liposomes have a well-defined lipid bilayer structure, whereas nanoparticles can have a variety of structures and compositions.

Reference

1. Hou, X. et al. Lipid nanoparticles for mRNA delivery. Nat Rev Mater. 2021, 6: 1078-1094.