Cannabidiol (CBD), a nonpsychoactive major component derived from Cannabis sativa, widely used in
neurodegenerative diseases, has now been proven to have growth inhibitory effects on many tumor cell lines, including
breast tumors. Meanwhile CBD can effectively alleviate
cancer-associated pain, anxiety, and depression, especially
tumor cachexia, thus it is very promising as an anti-
tumor drug with unique advantages.
20(S)-Protopanaxadiol (
PPD) derived from the best-known tonic Chinese herbal medicine Ginseng was designed to be co-loaded with CBD into
liposomes to examine their synergistic
tumor-inhibitory effect. The CBD-
PPD co-loading
liposomes (CP-
liposomes) presented a mean particle size of 138.8 nm. Further glycosyl-modified CP-
liposomes (GMCP-
liposomes) were prepared by the incorporation of n-Dodecyl β-D-maltoside (Mal) into the liposomal bilayer with
glucose residue anchored on the surface to act as a
ligand targeting the GLUT1 receptor highly expressed on
tumor cells. In vivo studies on murine
breast tumor (4T1 cells)-bearing BALB/c mice demonstrated good dose dependent anti-
tumor efficacy of CP-
liposomes. A high
tumor inhibition rate (TIR) of 82.2% was achieved with good tolerance. However, glycosylation modification failed to significantly enhance TIR of CP-
liposomes. In summary, combined
therapy with
PPD proved to be a promising strategy for CBD to be developed into a novel
antitumor drug, with characteristics of effectiveness, good tolerance, and the potential to overcome
tumor cachexia.