This study showed that conjugating the anticancer drug doxorubicin to squaline, a natural lipid precursor of cholesterol, improved its anticancer efficacy and reduced its cardiotoxicity. Doxorubicin–squalene (SQ–Dox) conjugates formed nanoassemblies that reduced pancreatic tumour growth by 95% when administered to a mouse model, compared to a 29% reduction with normal doxorubicin. Moreover, murine lung tumours that did not respond to normal doxorubicin treatment were inhibited by 90% with SQ–Dox. In addition, the nanomedicine had a fivefold higher maximum tolerated dose than the unmodified drug, and unlike doxorubicin it did not cause myocardial lesions.
References
Maksimenko, A. et al. A unique squalenoylated and nonpegylated doxorubicin nanomedicine with systemic long-circulating properties and anticancer activity. Proc. Natl Acad. Sci. USA 111, E217–E226 (2014)
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Harrison, C. Double boost for doxorubicin therapy. Nat Rev Drug Discov 13, 178 (2014). https://doi.org/10.1038/nrd4268
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DOI: https://doi.org/10.1038/nrd4268