This article reviews the innovative and original concept the “squalenoylation”, a technology
allowing the formulation of a wide range of drug molecules (both hydrophilic and lipophilic) as
nanoparticles. The "squalenoylation" approach is based on the covalent linkage between the squalene,
a natural and biocompatible lipid belonging to the terpenoid family, and a drug, in order to increase
its pharmacological efficacy. Fundamentally, the dynamically folded conformation of squalene triggers
the resulting squalene-drug bioconjugates to self-assemble as nanoparticles of 100-300 nm. In
general, these nanoparticles showed long blood circulation times after intravenous administration and
improved pharmacological activity with reduced side effects and toxicity. This flexible and generic
technique opens exciting perspectives in the drug delivery field.
Keywords: Squalenoylation, Prodrug, Nanoassemblies, Drug loading, Oncology, Intracellular infections, Neurological disorders.
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