Peptide delivery using phospholipid micelles

Abstract Peptide based drugs are an important class of therapeutic agents but their development into commercial products is often hampered due to their inherent physico‐chemical and biological instabilities. Phospholipid micelles can be used to address these delivery concerns. Peptides self‐associate with micelles that serve to thwart the aggregation of these biomolecules. Self‐association with micelles does not modify the peptide chemically; therefore the process does not denature or compromise the bioactivity of peptides. Additionally, many amphiphilic peptides adopt α ‐helical conformation in phospholipid micelles which is not only the most favorable conformation for receptor interaction but also improves their stability against proteolytic degradation, thus making them long‐circulating. Furthermore, the nanosize of micelles enables passive targeting of peptides to the desired site of action through leaky vasculature present at tumor and inflamed tissues. All these factors alter the pharmacokinetic and biodistribution profiles of peptides therefore enhance their efficacy, reduce the dose required to obtain a therapeutic response and prevent adverse effects due to interaction of the peptide with receptors present in other physiological sites of the body. These phospholipid micelle based peptide nanomedicines can be easily scaled‐up and lyophilized, thus setting the stage for further development of the formulation for clinical use. All things considered, it can be concluded that phospholipid micelles are a safe, stable and effective delivery option for peptide drugs and they form a great promise for future peptide nanomedicines. WIREs Nanomed Nanobiotechnol 2012, 4:562–574. doi: 10.1002/wnan.1185 This article is categorized under: Therapeutic Approaches and Drug Discovery > Emerging Technologies Biology-Inspired Nanomaterials > Peptide-Based Structures