MPEG-2000-DSPE

MPEG-2000-DSPE (methoxy poly(ethylene glycol)-2000-distearoylphosphatidylethanolamine) is a PEGylated phospholipid widely used as a functional excipient in drug delivery systems. Its main applications include:

1. Long‑circulating liposomes

When incorporated into liposome bilayers (typically 5–20 mol%), the PEG chain creates a steric barrier that reduces opsonization and uptake by the mononuclear phagocyte system (MPS), significantly prolonging circulation half‑life.

• Clinical example: Doxil® (pegylated liposomal doxorubicin) uses MPEG‑2000‑DSPE to achieve a half‑life of ~2.5 days in humans, compared to <0.1 day for conventional liposomes.

2. Polymeric micelles

MPEG‑2000‑DSPE has a very low critical micelle concentration (CMC), enabling it to self‑assemble into stable micelles that solubilize poorly water‑soluble drugs.

• Examples: Used to encapsulate edaravone, paclitaxel, and other hydrophobic agents, improving stability, bioavailability, and targeted delivery in conditions such as cancer and neurodegenerative diseases.

3. Surface modification for active targeting

The terminal methoxy group can be replaced with targeting ligands (e.g., antibodies, peptides) via functionalized PEG‑lipid derivatives, allowing active targeting of specific cells or tissues.

Key properties

• Appearance: White powder

• Solubility: Soluble in chloroform, methanol, and water (~3–4 g/100 mL)

• Storage: –20 °C, protected from light and oxidation