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N2

Nanoparticles coated by bile salt modulating their uptake by macrophages

Prof. Eliana Grazia Leo, University of Modena and Reggio Emilia; Dr Valentina Iannuccelli, University of Modena and Reggio Emilia; Dr Eleonora Maretti, University of Modena and Reggio Emilia; Prof. Alessandro Delpiaz, University of Ferrara; Dr Barbara Pavan, University of Ferrara; Prof. Marco Fogagnolo, University of Ferrara; Dr Guglielmo Paganetto, University of Ferrara

University of Modena and reggio Emilia


Challenge

The proposed invention consists of nanoparticles made of therapeutic agents insoluble in aqueous environment, able to modulate their phagocytosis by macrophage cells thanks to a bile acid salt corona.


Technology

Polymer-free nanoparticles consist of an insoluble drug / prodrug in an aqueous medium covered by a bile acid salt corona; the different types of bile salt-corona modulate the intensity of phagocytosis of nanoparticles by macrophages. Depending on the choice of coating bile salt, the nanoparticles may constitute a method to delivery in the macrophages the therapeutic agent of which they are made, or prevent their capture by the macrophage cells allowing to obtain potential "long circulation" nanoparticles able to selectively direct themselves into specific tissues, such as tumor tissues according to a classic passive targeting process.


Commercial Opportunity

The polymer-free nanoparticles developed are of interest to the pharmaceutical companies since they have demonstrated various important features including the opportunity to select the target, no toxicity; high biocompatibility and low side effects; easy to formulate with low production cost. Hence, these nanoparticles, according to the drug used to produce them, could be used in the treatment of different diseases (eg: caused by viral and / or bacterial pathogens, from fungi or parasites belonging to protozoa) that can affect macrophages. Furthermore, the nanoparticles could also be used in the treatment of tumor pathologies by passive targeting of the drug.


Development Status

In vitro data.


Patent Situation

A International patent application has been filed recently. Worldwide patent protection is possible.


Further Reading

1. A. Dalpiaz. Bile acids: new opportunities for the drug targeting? Pharmaceutics, 11 (48): 7-8, 2019
2. A. Dalpiaz, B. Pavan, M. Fogagnolo, L. Ferraro, F. Sacchetti, E. Maretti, V. Iannuccelli, E. Leo. Bile acids modulation of nanoparticle macrophage uptake. 11th World Meeting on Pharmaceutics, Biopharmaceutics and Pharmaceutical Technology, 19-22-March 2018, Granada, Spain.
3. A. Dalpiaz. Bile acids: new opportunities for the drug targeting? CRS Italy Chapter Annual Workshop - Advances in Drug Deliveryand Biomaterials: facts and vision, 18-20 October 2018, Padova, Italy


 

Nanoparticles coated by bile salt modulating their uptake by macrophages