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Abstract
Background: 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. Summary: 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.
Acknowledgements
The authors thank Dr K Un for assisting with data acquisition.
Financial & competing interests disclosure
This work was supported in part by Research on the Development of New Drugs and by Health and Labour Sciences Research Grants from the Ministry of Health, Labour, and Welfare of Japan and by the Japan Society for the Promotion of Science (KAKENHI grant number 24590070). The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed. The manuscript has been edited by native-English-speaking professional editors with the support of research grant, Research on the Development of New Drugs from the Ministry of Health, Labour, and Welfare of Japan.