Overview
DSPE-PEG is a synthetic phospholipid-polymer conjugate combining the hydrophobic DSPE (1,2-distearoyl-sn-glycero-3-phosphoethanolamine) with hydrophilic PEG (polyethylene glycol) chains. This amphiphilic structure enables unique self-assembling properties, making it invaluable for creating sterically stabilized drug carriers. First developed in the 1990s, it revolutionized nanomedicine by prolonging nanoparticle circulation time through reduced macrophage uptake. The conjugate exists in various PEG molecular weights (e.g., PEG2000, PEG5000), with the chain length impacting pharmacokinetics. Pharmaceutical-grade DSPE-PEG meets stringent purity standards (>95% by HPLC) and is manufactured under GMP conditions for clinical applications. Its versatility supports both passive and active targeting strategies in therapeutic formulations.
Physical and Chemical Properties
DSPE-PEG exhibits temperature-dependent phase behavior, with the DSPE moiety undergoing gel-to-liquid crystalline transition near 55°C. The PEG chains extend 3-10 nm from the surface (depending on MW), creating a hydration layer that sterically hinders opsonization. Critical micelle concentration (CMC) ranges from 0.001-0.01 mg/mL, with micelle sizes typically 10-30 nm. Chemical stability is maintained at pH 5-8, though PEG oxidation can occur under prolonged light exposure. The compound shows negligible cytotoxicity at concentrations below 1 mg/mL, as confirmed by ISO 10993-5 testing. Fourier-transform infrared spectroscopy (FTIR) confirms characteristic peaks at 1100 cm⁻¹ (PEG ether) and 1735 cm⁻¹ (ester carbonyl).
Main Applications
In drug delivery, DSPE-PEG forms the outer monolayer of long-circulating liposomes (e.g., Doxil®), reducing clearance by the reticuloendothelial system. It's also used to create PEGylated exosomes for targeted RNA delivery and stabilizes perfluorocarbon nanoparticles for ultrasound contrast imaging. Beyond therapeutics, DSPE-PEG2000-Maleimide enables antibody conjugation for immunoliposomes. In diagnostics, it prevents non-specific binding in quantum dot probes. Emerging applications include CRISPR-Cas9 delivery systems and COVID-19 mRNA vaccine formulations, where it stabilizes lipid nanoparticles (LNPs).
Safety and Storage
While generally recognized as safe (GRAS) by FDA for specific applications, bulk powder requires handling with nitrile gloves due to potential respiratory irritation. Aqueous solutions are stable for 1 week at 4°C but should be sterile-filtered (0.22 μm) for biological use. Long-term storage requires argon-purged vials with desiccant at -20°C. Degradation indicators include yellow discoloration (PEG oxidation) or clumping (hydrolysis). Material Safety Data Sheets (MSDS) classify it as non-hazardous, though waste disposal should follow local regulations for organic compounds.
B2B Procurement Guide
When sourcing DSPE-PEG, verify: 1) PEG molecular weight distribution (polydispersity index <1.05 preferred), 2) residual solvent levels (<500 ppm DCM), and 3) endotoxin testing (<0.1 EU/mg for injectables). Leading suppliers include Avanti Polar Lipids, NOF America, and CordenPharma. Technical specifications should include MALDI-TOF mass spectrometry data for PEG chain verification. For GMP-grade material, request Drug Master Files (DMF) references. Bulk orders (1kg+) typically have 8-12 week lead times. Consider pre-formed micelle solutions for small-scale R&D to avoid solubility challenges.
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