Effects of lipid composition on the properties of doxorubicin-loaded liposomes

• Published in: Therapeutic delivery 2015-07, Vol.6 (7), p.785-794
• Main Authors: Sakai-Kato, Kumiko, Nanjo, Kunie, Kawanishi, Toru, Okuda, Haruhiro, Goda, Yukihiro
• Format: Article
• Language: English
• Subjects: Adenosine Triphosphate - metabolism; Antibiotics, Antineoplastic - administration & dosage; Antibiotics, Antineoplastic - chemistry; Antibiotics, Antineoplastic - metabolism; Antibiotics, Antineoplastic - pharmacology; Cell Survival - drug effects; Chemistry, Pharmaceutical; Doxorubicin - administration & dosage; Doxorubicin - analogs & derivatives; Doxorubicin - chemistry; Doxorubicin - metabolism; Doxorubicin - pharmacology; HeLa Cells; Humans; Kinetics; Lipids - chemistry; Liposomes; Neoplasms - metabolism; Neoplasms - pathology; Polyethylene Glycols - administration & dosage; Polyethylene Glycols - chemistry; Polyethylene Glycols - metabolism; Polyethylene Glycols - pharmacology; Solubility; Technology, Pharmaceutical - methods
• ISSN: 2041-5990; 2041-6008
• DOI: 10.4155/tde.15.29

The liposomal lipid composition of doxorubicin-loaded liposome likely will influence its pharmacological activity. Results & methodology: We prepared 18 formulations of doxorubicin-loaded liposomes in which the lipid composition was varied. It was indicated that the intracellular uptake of doxorubicin is the primary property of doxorubicin-loaded liposome that affects its cytotoxicity in vitro. Furthermore, the release rate of doxorubicin from liposome and the biological activity of the lipid itself also affected the cytotoxicity. These findings provide an insight into how lipid composition influences the cytotoxicity of the doxorubicin-loaded liposomes. Our results provide valuable information that should help to enhance the therapeutic efficacy of liposomal anticancer drug products by optimizing their formulations.