| Patent title | The nanocapsulation of fenretinide in nanomicelles allows for increased bioavailability and achieves high hepatic concentrations following accumulation, through extravasation, of the nanomicelles injected into the venous blood. |
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| Thematic area | Health |
| Ownership | Institute of Liver and Biliary Sciences, ALMA MATER STUDIORUM - UNIVERSITA' DI BOLOGNA |
| Inventors | Isabella Orienti, Giovanna Farruggia |
| Filed on | 12 April 2022 |
Fenretinide is a synthetic derivative of retinoic acid with antitumor, anti-inflammatory, and antiviral activities, exhibiting minimal systemic toxicity and excellent tolerability. Its efficacy has been demonstrated in liver pathologies such as hepatoblastoma, hepatocellular carcinoma, liver fibrosis, and cirrhosis. Despite its excellent pharmacological properties, this drug has not entered clinical use due to its poor aqueous solubility and consequent low bioavailability, preventing the attainment of plasma levels sufficient for therapeutic activity. In liver pathologies, an additional obstacle to its use is the extensive metabolism of fenretinide, hindering the achievement of therapeutic concentrations even with high doses of the drug.
Fenretinide nanomicellar is a novel pharmaceutical nanoformulation capable of increasing the bioavailability of fenretinide and providing high drug concentrations to the liver.
The pharmaceutical applications in liver pathologies, such as hepatoblastoma, hepatocellular carcinoma, liver fibrosis, and cirrhosis, involve the use of fenretinide nanomicelles. This enables the achievement of high drug levels in the liver with increased therapeutic efficacy, avoiding uncontrolled distribution to other areas of the body. The high drug concentrations obtained with nanomicellar accumulation in the liver allow for reaching therapeutic levels even in the presence of hepatic metabolism. Additionally, the gradual release of the drug from the nanomicelles does not induce the expression of metabolizing enzymes. Moreover, nanomicelles allow the incorporation of other drugs in combination with fenretinide, enabling the development of organ-targeted therapies with increased therapeutic efficiency and devoid of off-target effects.