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Recent advances in the formulation of sphingolipid anticancer therapeutics

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Abstract

Background

The bioactive sphingolipids such as ceramide, sphingosine, and sphingosine-1-phosphate are of special interest as key regulators of cellular proliferation or apoptosis signaling. The balance between ceramide and sphingosine-1-phosphate is critical for the selection of proliferative or apoptotic signaling as well as for therapeutic efficacy against cancer cells.

Area covered

A number of drug candidates designed to regulate the balance between ceramide and sphingosine-1-phosphate have been developed and several (i.e., safingol, ABC294640, Sonepcizumab, and fingolimod) are under clinical investigation as anti-cancer drugs. Various nanotherapeutic challenges combined with the use of anticancer drugs and/or phospholipid metabolism inhibitors and short chain ceramide has been investigated to increase the cellular accumulation of ceramide, which acts as apoptotic signaling molecules.

Expert opinion

Many sphingolipid-containing nanotherapeutics have shown promising results as cancer treatments. These sphingolipid nanotherapeutics can include a synergistic combination of short chain ceramide and ceramide-forming anticancer agents or sphingolipid metabolism inhibitors. Sphingolipid nanotherapeutics could also be used to treat multidrug-resistant cancer cells as well as sensitive cancer cells.

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  1. College of Pharmacy, Dankook University, Cheonan, 31116, Republic of Korea

    Min-Koo Choi

  2. College of Pharmacy and Research Institute of Pharmaceutical Sciences, Kyungpook National University, Daegu, 41566, Republic of Korea

    Im-Sook Song

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Choi, MK., Song, IS. Recent advances in the formulation of sphingolipid anticancer therapeutics. J. Pharm. Investig. 50, 295–307 (2020). https://doi.org/10.1007/s40005-020-00475-y

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