Sterically stabilized micelle (SSM) is a self-assembled nanoparticle ideal for the delivery of therapeutic peptides. The PEGylated phospholipid forming the particle, DSPE-PEG2000, is a safe, biocompatible, and biodegradable ingredient already approved for human use in the marketed product Doxil®. SSM can overcome formulation difficulties such as instability associated with peptide drugs, enabling their development for clinical application. The key advantage of this lipid-based nanocarrier is its simple preparation even at large scales, which allows easy transition to the clinics and the pharmaceutical market. In this chapter, we describe methods for preparation and characterization of peptides self-associated with SSM (peptide-SSM). We also discuss approaches to evaluate the biological activity of the peptide nanomedicines in vitro and in vivo.
Keywords: DSPE-PEG2000; Glucagon-like peptide 1; Glucose-dependent insulinotropic peptide; Micellar nanocarrier; Neuropeptide Y; Pancreatic polypeptide; Peptide drug delivery; Pituitary adenylate cyclase activating polypeptide; Sterically stabilized micelles; Vasoactive intestinal peptide.