Co-delivery of paclitaxel and melittin by glycopeptide-modified lipodisks for synergistic anti-glioma therapy

Abstract

Nanosized lipodisks with flat circular phospholipid bilayers surrounded by PEGylated edges have demonstrated promise in drug delivery. In the present work, a lipodisk-based paclitaxel and melittin co-delivery system functionalized with glycopeptide ⁹G-A7R (⁹G-A7R-Disk/PTX/melittin) was successfully constructed, in which melittin which was fully protected from proteolysis and hemolysis was effectively reduced. The ratio of paclitaxel to melittin in lipodisks could be accurately controlled through a film hydration–adsorption method. Paclitaxel combined with melittin showed synergism against U87 cells in vitro, and ⁹G-A7R-Disk/PTX/melittin demonstrated an enhanced anti-glioma effect in vivo, significantly prolonging the survival time of glioma-bearing mice. The results suggested a promising formulation for the co-delivery of paclitaxel/melittin and glioma-targeted therapy.