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Europe | European ＆ international partnerships | Chemistry | Nanomedicine
Terpenoylation: an original concept for the discovery of new nanomedicines
The TERNANOMED project, involving Bernard Rousseau (former head of SCBM), aims at developing terpenoid-based nanoassemblies to improve the treatment of severe diseases such as cancer, infectious diseases. The approach consists in linking a terpene (synthetic or natural) to a biologically active drug in order to obtain a bioconjugate able to self-assemble in water in the form of nanoparticles.
Terpenoids are a group of natural compounds that are extraordinary diverse in chemistry, structure and function. Most of the natural terpenoids are flexible and biocompatible biopolymers, having physico-chemical characteristics able to adapt to a wide variety of biologically active compounds. Surprisingly, they have never been used previously in the nanotechnology field for drug delivery and targeting purposes, except very recently by us to design squalene-based nanoassemblies. Thus, the current project aims to develop terpenoid-based nanoassemblies to improve the treatment of severe diseases including cancer, infectious and metabolic diseases. The conceptual approach is to chemically link a terpenoid to a biologically active drug molecule in order to allow the resulting bioconjugate to self-assemble as nanoparticles in water. Noteworthy, the nature of the polyterpenoid (ie. number of isoprenoid units) may be adapted to the hydrophilic/lipophilic character of the drug molecule to be transported, whereas the nature of the linkage (ester, amide, disulfide bonds etc.) will be selected according to the enzymatic content of the targeted diseased area. From the ratio between drug's and polyterpene's molecular weights, it is deduced that the drug loading will be dramatically improved as compared to the currently available nanomedicines. In other words, the pro-drug will form the nanomedicine by selfaggregation without the need of any other transporter material. The project will involve the following interdisciplinary aspects:(i) synthesis of drug/polyterpene bioconjugates,(ii)design of the nanoassemblies and their functionalization with recognition ligands,(iii)cell and tissue imaging and(iv)pharmacological evaluation in vitro (cell culture) and in vivo. Such ambitious and challenging project will be performed under Patrick Couvreur s leadership who has settled up a worldwide recognized multidisciplinary research team, unique in the nanomedicine world.
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