Anacardic acid enhances the anticancer activity of liposomal mitoxantrone towards melanoma cell lines - in vitro studies.
mitoxantrone loaded into liposomal carriers enriched with encapsulated anacardic acid in the liposomal bilayer using a vitamin C gradient. Anacardic acid is a potent epigenetic agent with anticancer activity. This is the first liposomal formulation to combine an actively encapsulated drug and anacardic acid. The liposomes were characterized in terms of basic parameters, such as size, zeta potential, optimal drug-to-lipid ratio, loading time and temperature, and stability at 4°C and in human plasma in vitro. The formulation was found to be stable, and the loading process was rapid and efficient (drug-to-lipid ratio of up to 0.3 with over 90% efficiency in 5 minutes). The cytotoxicity of these formulations was assessed using the human melanoma cell lines A375 and Hs294T and the normal human dermal fibroblast line. The results showed that anacardic acid and to a smaller extent vitamin C significantly increased the cytotoxicity of the drug towards melanoma compared to ammonium sulfate liposomes. On the other hand, vitamin C and anacardic acid both protected normal cells from damage caused by the drug. The formulation combining anacardic acid, vitamin C, and mitoxantrone showed promising results in terms of cytotoxicity and cytoprotection. Therefore, it has potential for anticancer treatment.
Department of Lipids and Liposomes, Faculty of Biotechnology, University of Wrocław, Wrocław, Poland.
Mateusz
M
Legut
Department of Lipids and Liposomes, Faculty of Biotechnology, University of Wrocław, Wrocław, Poland.
Dominik
D
Lipka
Department of Lipids and Liposomes, Faculty of Biotechnology, University of Wrocław, Wrocław, Poland.
Nina
N
Filipczak
Department of Lipids and Liposomes, Faculty of Biotechnology, University of Wrocław, Wrocław, Poland.
Adriana
A
Piwoni
Department of Lipids and Liposomes, Faculty of Biotechnology, University of Wrocław, Wrocław, Poland.
Arkadiusz
A
Kozubek
Department of Lipids and Liposomes, Faculty of Biotechnology, University of Wrocław, Wrocław, Poland.
Jerzy
J
Gubernator
D048729:Anacardic Acids / Q000008:administration & dosage; D000971:Antineoplastic Combined Chemotherapy Protocols / Q000008:administration & dosage* / Q000737:chemistry*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004058:Diffusion; D004357:Drug Synergism; D006801:Humans; D008081:Liposomes / Q000737:chemistry*; D008545:Melanoma / Q000188:drug therapy* / Q000473:pathology*; D008942:Mitoxantrone / Q000008:administration & dosage; D016896:Treatment Outcome
D048729:Anacardic Acids; D008081:Liposomes; C088115:anacardic acid; D008942:Mitoxantrone
anacardic acid; ascorbic acid; liposomes; melanoma; mitoxantrone; vitamin C