UTILIZACION DEL ACIDO ESCUALENICO PARA LA FORMULACION DE UN PRINCIPIO ACTIVO EN ESTADO DE NANOPARTICULAS

• Main Authors: CATTEL, LUIGI, ROCCO, FLAVIO, RENOIR, JACK-MICHEL, STELLA, BARBARA, ROSILIO, VERONIQUE, COUVREUR, PATRICK
• Format: Patent
• Language: Spanish
• Published: 16.01.2012
• Subjects: CHEMISTRY; DERIVATIVES THEREOF; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; NUCLEIC ACIDS; NUCLEOSIDES; NUCLEOTIDES; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SUGARS

Utilización del ácido escualénico o de un derivado hidrocabonado por lo menos de C18, acíclico, no lineal e insaturado del radical escualenoilo apropiado para compactarse cuando se pone en presencia de un disolvente polar para formular por lo menos un principio activo de naturaleza polar y de peso molecular superior a 100 Da en estado de nanopartículas, siendo dicho principio un nucleósido o uno de sus análogos. 2',2'-Difluoro-2'-deoxycytidine derivatives (I) are new. 2',2'-Difluoro-2'-deoxycytidine derivatives of formula (I) are new. R 1-R 3 each : hydrogen or hydrocarbyl acyl of at least 18C with a conformation that imparts the capacity for (I) to adapt a compacted form in polar solvent, provided at least one is other than hydrogen. Independent claims are also included for the following: (1) nanoparticles (NP) of (I); (2) method for preparing NP; and (3) use of squalenic acid (II), or its derivatives, for formulating at least one polar active agent of molecular weight over 100 as nanoparticles. [Image] ACTIVITY : Cytostatic; Virucide. MECHANISM OF ACTION : (I) is converted intracellularly into its triphosphate and when this is incorporated into replicating DNA, elongation is stopped, resulting in cell death.