Metal-organic frameworks (MOFs), also called “hybrid porous crystallised solids”, are coordination polymers with a hybrid inorganic-organic framework comprising metal ions and organic ligands coordinated to said metal ions.

These materials are organised as mono-, bi- or tri-dimensional networks wherein the metal clusters are linked to each other by spacing ligands periodically. These materials have a crystalline structure and are generally porous.

In the present work, the research team have developped porous metal-organic frameworks with a modified surface loaded with a molecule of interest that show excellent results as drug carriers for drug delivery applications (bisulfan, AZTP, Cidofovir, Docetaxel, Gemcitabine…) or as marker carriers for imaging applications (rhodamine, fluorescein, luciferase, …). The particles of the present invention may also be used for applications in the cosmetic field.

Surface modifications offers additional delivery improvements such as biodistribution, bioadhesion and targetting.

The research team also developed porous nanoparticules of iron carboxylate metal-organic frameworks with or without a modified surface for the same purpose as depicted above.

There is a real need for compounds that :

• are capable of carrying active principles, notably active principles that have particular encapsulation difficulties linked to their instability, their strong tendency to crystallize, their poor solubility, their amphiphilic or hydrophilic nature…
• with sufficient loading capacities, especially if repeated administration of nanoparticles is envisioned
• can afford controlled release of the active principles
• are capable of vectorizing active principles toward specific targets, or of modifying the biodistribution of these active principles.

The present invention aims at answering each of these demands.

Pending patents

1310-01

Scope: nanoparticles of iron carboxylate metal-organic frameworks with or without modified surface as drug and marker carrier.

Priority application: french patent application FR0706873 filled on October 1, 2007 and entitled « nanoparticules hybrides organiques inorganiques à base de carboxylates de fer ».
Extensions in Europe (delivered), Japan, Canada and USA.

1310-02

Scope: metal-organic frameworks with modified surface as drug and marker carrier.
Priority application: french patent application FR0706875 filed on October 1, 2007 and entitled « Solide hybride organique inorganique à surface modifiée ».
Extensions in Europe (delivered), Japan, Canada and USA.
04666-01
Scope : metal-organic frameworks with improved modified surface as drug and marker carrier
Priority application: french patent application FR1255065 filled on May 31, 2012 and entitled « Solide hybride organique amélioré à surface externe modifiée »

Development stage

• In vitro and in vivo toxicity
• In vitro efficiency assays
• More recent results demonstrated improved surface modification involving cyclodextrines. This leads to more stable particles and the absence of surface agents located in the particles’ pores.

Scientific publications

• Angew. Chem. Int. Ed. 2010, 49, 6260 – 6266.
• Nature Materials 9, 172–178 (2010).

For further information, please contact us (Ref 01310-01-02 04666-01)