Nanoparticles of therapeutic agents having low water solubility

A water-dispersible derivative of a therapeutic active agent of low water solubility formed from at least one molecule of said active agent covalently coupled to at least one molecule of a hydrocarbon-based compound of squalene structure or an analog thereof, said active agent having a solubility of less than 100 μg/ml in pure water, measured at room temperature.

A water-dispersible nanoparticle of at least one therapeutic active agent of low water solubility in which said active agent is present therein in a form combined with at least one hydrocarbon-based compound of squalene structure or an analog thereof.

An aqueous dispersion of water-dispersible nanoparticles of at least one therapeutic active agent of low water solubility in which said active agent is present therein in a form combined with at least one hydrocarbon-based compound of squalene structure or an analog thereof.

A process for preparing water-dispersible nanoparticles of at least one therapeutic active agent of low water solubility in which said active agent is present therein in a form combined with at least one hydrocarbon-based compound of squalene structure or an analog thereof, wherein it comprises at least:

• dissolution of at least one water-dispersible derivative of a therapeutic active agent of low water solubility formed from at least one molecule of said active agent covalently coupled to at least one molecule of a hydrocarbon-based compound of squalene structure or an analog thereof, said active agent having a solubility of less than 100 μg/ml in pure water, measured at room temperature in at least one organic solvent at a concentration that is sufficient to obtain, during the addition of the corresponding mixture, with stirring, to an aqueous phase, the instantaneous formation of nanoparticles suspended in said aqueous phase, and
• where appropriate, the isolation of said nanoparticles.

A pharmaceutical composition comprising, as active material, at least one water-dispersible derivative of a therapeutic active agent of low water solubility formed from at least one molecule of said active agent covalently coupled to at least one molecule of a hydrocarbon-based compound of squalene structure or an analog thereof, said active agent having a solubility of less than 100 μg/ml in pure water, measured at room temperature or water-dispersible nanoparticles of at least one therapeutic active agent of low water solubility in which said active agent is present therein in a form combined with at least one hydrocarbon-based compound of squalene structure or an analog thereof in combination with at least one pharmaceutically acceptable vehicle.