New antitumoral formulation

Nanoformulation designed to increase the bioavailability and in vivo antitumor activity of Fenretinide administered orally.

Title of the patent Bionanofenretinide come nuova formulazione antitumorale
Thematic area Pharmaceutical
Ownership Alma Mater Studiorum - Università Di Bologna, Istituto Superiore di Sanità
Inventors Isabella Orienti, Anna Pegna Zeuner, Adriana Eramo
Protection Italy (opportunity for seeking international patent protection)
Licensing status Available for licensing agreement
Keywords Fenretinide, antitumoral, tolerability, encapsulation
Filed on Jun 13, 2018

Most tumors are heterogeneous and contain a small population of cancer stem cells (CSCs) that exhibit distinctive features of self-renewal, proliferation and differentiation, which are believed to play a crucial role in tumor progression, drug resistance, relapse and  metastases. A huge effort has been made in the development of anti-CSC strategies and several potential approaches to kill therapy-resistant CSCs have been explored. A huge obstacle to the effectiveness of treatments is the limited distribution of drugs in the target cell environment due to the limited solubility in water, the short circulation time and the reduced stability of the compounds, as well as the systemic toxicity that does not allow the achievement of therapeutic concentrations within tumors.

Fenretinide is an excellent antitumor drug active towards a wide range of tumors, with excellent tolerability. However, its low water solubility limits its therapeutic use since, even the administration of high doses of the drug does not provide adequate plasma levels to produce an adequate therapeutic effect. Therefore the potential of this drug is, in fact, hampered by its low availability.

Bionanofenretinide is an innovative nanoformulation designed and built to increase the bioavailability of Fenretinide. This formulation is based on the technological platform of nano-encapsulation of drugs in amphiphilic carriers. These carriers are able to provide drug-carrier complexes with optimal chemical-physical characteristics for the solubilization of the drug in the fluids of the administration environment and the subsequent disposition of the drug in the organism until the specific therapeutic target is reached.

The patented bionanofenretinide, therefore, is prepared for nano-encapsulation of fenretinide in biocompatible and biofunctional carriers able to modify the chemical-physical characteristics of the molecule making it soluble and bioavailable in body fluids.

◾ Stable circulation throughout the gastrointestinal tract
◾ Possibility of oral administration
◾ Increased oral bioavailability
◾ Possibility of parenteral administration

  • Absorption of the drug by the lymphatic system
  • Use of the formulation together with conventional anticancer therapies to reinforce their effectiveness