Dexamethasone loaded R3V6 peptide micelles as a gene carrier

Abstract

R3V6 peptides formed self-assembled micelles in aqueous solution with a hydrophobic core of valines (Vs) and hydrophilic corona of arginines (Rs). R3V6 peptides could bind to DNA by electrostatic interactions and deliver DNA into cells. However, compared with poly-L-lysine, the DNA delivery efficiency of the R3V6 peptide micelles was not high, due to the instability of the peptide micelles. To overcome poor DNA delivery efficiency of the R3V6 peptide and add anti-inflammatory effect, dexamethasone was loaded as a model hydrophobic drug into the core of the peptide micelles. First, it was confirmed that hydrophobic fluorescent dye 5-dodecanoylaminofluorescein (DAF) was loaded into the R3V6 micelles, but hydrophilic dye Oregon Green was not. The dexamethasone loaded R3V6 peptide micelles had higher DNA delivery efficiency than the R3V6 peptide micelle control. This enhanced efficiency may be due to higher stability of the drug loaded micelles in aqueous solution. Considering that dexamethasone is an effective anti-inflammatory drug, the dexamethasone loaded R3V6 peptide micelles are effective co-delivery carriers of drug and DNA and will be useful for inflammatory disease gene therapy.