PEG Lipids

Introduction

PEG lipids, also known as PEGylated lipids, refer to PEG molecules are attached to a lipid molecule through covalent bonding to form PEG derivatives. PEG lipids are widely used in drug delivery systems, which can effectively improve the physicochemical and biological stability of drug delivery systems due to their unique performance. And thus, prolonging the half-life of blood circulation, improving tumor targeting efficiency, enhancing drug efficacy, and reducing toxic and side effects.

Applications

PEG lipids are mainly used in drug delivery systems, which is highly favored in the field of biomedicine and pharmacy. Here, take the most representative and used kind of PEG lipids, poly (ethylene glycol)-distearoylphosphatidylethanolamine (PEG-DSPE) as an example ^[1].

Application of PEG-DSPE in the preparation of drug carriers

PEG-DSPE are biocompatible and amphiphilic polymers that can be widely utilized in the preparation of drug carriers such as liposomes, polymeric nanoparticles, polymer hybrid nanoparticles, solid lipid nanoparticles, lipid-polymer hybrid nanoparticles, and microemulsions. Some of them are shown in below.

Fig.1 Chemical structure of PEG-DSPE

• Liposomes. Conventional liposomes have low bioavailability and short blood-circulation time, and are easily absorbed by the RES. The incorporation of PEG-DSPE in the lipid-based carriers substantially prolongs the circulation lifetime of the liposomes due to high flexibility, favorable hydrophilicity, antiphagocytosis against macrophages, resistance to immunological recognition, noncombination with proteins, and biocompatibility of PEG.
• Polymeric nanoparticles. The amphiphilic polymers of PEG-DSPE can self-assemble into micelles and are easily modified. It is a type of satisfactory material for the preparation of polymeric nanoparticles and show many advantages.
• Microemulsions. The microemulsions prepared with PEG-DSPE have many advantages, such as enhancing the capacity of loading the hydrophobic drugs, increasing the blood-circulation time, and improving the bioavailability, in delivering drugs to tumors.

Fig.2 Structure diagram of PEG-DSPE microemulsions

Application of PEG-DSPE in delivering drugs

PEG-DSPE used in drug carriers can used to deliver nucleic acids, proteins and peptides, hydrophobic drugs. The details are shown in below.

• Transmission of nucleic acids. Nucleic acids, RNA, and DNA show huge potential in the treatment of cancer, the delivery of which would be inefficient to the target sites, though. PEG-DSPE used in the preparation of nanocarriers can as drug-carrier material for the effective delivery of nucleic acids, which can significantly prolong the circulation time in blood, reduce the RES absorption, increase the bioavailability of target organs, target tissues, target cells, or intracellular parts.
• Transmission of proteins and peptides. Protein and peptide drugs in development have covered many therapeutic areas, including oncology, metabolic disorders, and cardiovascular disease, however, they suffer the disadvantages of lack of oral bioavailability, poor stability and etc. PEG-DSPE was selected for the preparation of long-circulating liposomes can effectively overcome the above problems.
• Transmission of hydrophobic drugs. Many important active agents such as docetaxel and camptothecin are poorly soluble. In aqueous media, amphiphilic PEG-DSPE block copolymers can self-assemble into polymeric micelles with a core-shell structure. When deliver the poorly soluble drugs, the drugs would incorporate with the core of DSPE, which would increase the concentrations of hydrophobic drugs, improve bioavailability, and protect the drugs from inactivation in biological media.

Alfa Chemistry can offer all kinds of PEG lipids. You can click on our product list for a detailed view. If you do not find the product you want, we also provide you with custom synthesis service. Please contact us, if you are in need of assistance.

Reference

1. Wang R., et al. Application of poly (ethylene glycol)-distearoylphosphatidylethanolamine (PEG-DSPE) block copolymers and their derivatives as nanomaterials in drug delivery[J]. International Journal of Nanomedicine, 2012, 7: 4185-4198.