PEGylated Lipids

What are PEGylated Lipids?

PEGylated lipids are PEG derivatives containing lipid molecules that can be used for bioconjugation and lipid nanoparticle (LNP) drug delivery to improve the circulation time of liposome-encapsulated drugs. Lipid molecules are characterized by low toxicity and ease of preparation, and can be used as carriers for not only water-soluble but also lipid-soluble drugs. BOC Sciences offers the synthesis of PEGylated lipids and provides services for modification of functionalized PEG ends, including amines, carboxylic acids, azides, aldehydes, thiols and hydroxyls.

Fig. 1. Structures of the LP and PEGylated lipid. (Ho et al., 2018)

Why Need PEG Modification?

Polyethylene glycol (PEG) is an inert, non-carcinogenic polymer and is currently one of the polymers of choice for modifying the surface of bioactive molecules and nanoparticles. PEG is inexpensive, mass-producible, has an easily controlled molecular weight, and has good physicochemical properties, and PEG-derived lipids can reduce the leakage rate of liposomes, decrease aggregation and fusion, and prolong the expiration date. Moreover, the good stability of PEGylated liposomes allows them to be used in other drug delivery systems, such as encapsulating contrast agents in PEG liposomes for diagnostic imaging of organs such as the kidneys, or making sprays for the treatment of lung diseases such as tuberculosis.

BOC Sciences' PEGylated Lipids Synthesis Services

BOC Sciences offers a full range of integrated PEGylated lipids synthesis services, including the design of PEGylated lipids, modification of PEG terminal groups, and custom synthesis of PEGylated lipids, to help customers develop projects in the pharmaceutical field.

• Design of PEGylated lipids

The structure and length of the PEG chain as well as the functional end groups are factors that affect its function. Also, parameters such as PEG size and surface charge affect immunogenicity. For example, polyethylene glycolized carriers containing negatively charged phospholipids are more capable of stimulating the immune system through complement activation than uncharged vesicles.

In addition, as with the PEG fraction, the structure and length of the hydrophobic chains of lipids can determine not only the degree of immunogenicity but also its effectiveness. Whereas, polyethylene glycolated lipid nanoparticles produced using a specific lipid anchoring group (e.g., cholesterol as an anchoring group) have longer lasting permeability and higher systemic bioavailability in circulation. Attention also needs to be paid to the role of lipid bonding, which is an important parameter in lipid design and performance.

All these factors need to be considered during the design process of PEGylated lipids and the PEGylated lipids products need to be customized for specific structure, length and function.

• Modification of PEG terminal groups

Based on the various applications of PEGylated lipids, PEG terminal groups can be modified to impart specific functional and chemical properties to the PEGylated lipids molecule. We offer PEG terminal modifications including amino, hydroxyl, carboxyl, sulfur, alkynyl, ether and azide groups. These chemical reactions can be carried out in our specialized organic synthesis chemistry laboratory, guaranteeing you high-quality products.

• Synthesis of PEGylated lipids

Upon completion of the design of the target PEGylated lipids, BOC Sciences can provide custom synthesis of PEGylated lipids. The lipids need to be dissolved in an organic solvent first to form a clear solution. Then, the target polyethylene glycol is gradually added to the lipid solution and stirred until a homogeneous mixture is formed. The excess solvent is then removed and the lipid-polyethylene glycol mixture is resuspended with water to form a mixture of PEGylated lipids.

As a supplier of lipids synthesis, we provide many types of lipids customization services, if you are interested in our services, please feel free to contact us.