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

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

Volume: 17 Issue: 25

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

Affiliation:

• Institut Galien Paris-Sud, UMR CNRS 8612, Université Paris-Sud, Université Paris Saclay, 5 Rue J.B. Clément, 92296, Châtenay-Malabry Cedex,France

Keywords: Squalenoylation, Prodrug, Nanoassemblies, Drug loading, Oncology, Intracellular infections, Neurological disorders.

Abstract: 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.

Cite this article as:

Feng Jiao , Lepetre-Mouelhi Sinda *, Couvreur Patrick , Design, Preparation and Characterization of Modular Squalene-based Nanosystems for Controlled Drug Release, Current Topics in Medicinal Chemistry 2017; 17 (25) . https://dx.doi.org/10.2174/1568026617666170719171728