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Current Topics in Medicinal Chemistry


ISSN (Print): 1568-0266
ISSN (Online): 1873-4294

Review Article

Design, Preparation and Characterization of Modular Squalene-based Nanosystems for Controlled Drug Release

Author(s): Jiao Feng, Sinda Lepetre-Mouelhi * and Patrick Couvreur

Volume 17, Issue 25, 2017

Page: [2849 - 2865] Pages: 17

DOI: 10.2174/1568026617666170719171728

Price: $65


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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