Nanoparticles of iron trimesate metal organic framework (MIL100) for drugs encapsulation and delivery, comparisons between two different syntheses.

H. Willaime, V. Agostoni, P. Horcajada, C. Serre, R. Gref
Université Paris-Sud, FR

Keywords: microwave synthesis, green chemistry, nanoporous hybrid material, drugs delivery


Nanoparticles of metal-organic frameworks (MOF) are good candidates for biomedical applications. MOF are hybrid crystalline structures composed of metal ions connected with organic ligands. MOFs are family of highly porous materials. Here, we focus on a particular material (MIL100) made of biocompatible elements: iron and trimesic acid (TMA). MIL100 nanoparticles were first synthetized by an hydrothermal method by mixing TMA, solid iron and hydrofluoric acide (HF). Azidotimidine is a nucleoside reverse transcriptase inhibitor used for AIDS treatment. The administration of the active triphosphorylated metabolite (AZT-TP) is seriously limited by its poor intracellular penetration and its low stability in biological media. In this context, MIL100 nanoparticles have been identified as excellent candidates for the encapsulation of AZT-TP. However, non-toxic carriers are needed for biomedical applications. Thus, we propose an alternative ‘green’ method without HF and compare with the ‘classical’ method using toxic HF. We show that both synthesis routes form nanoparticles with similar physico-chemical properties. Moreover, they both encapsulate AZT-TP with excellent efficiencies and the release patterns of AZT-TP are similar. In conclusion, the excellent performance in terms of AZT-TP loading and release as well as the ‘green’ synthesis method, make MIL100 nanoparticles good candidates for highly active antiretroviral therapy.