Conjugates of lipids and antimicrobial or antineoplastic drugs

Details Conjugates of lipids and antimicrobial or antineoplastic drugs Conjugates of lipids and antimicrobial or antineoplastic drugs

A - Human Necessities

61

K

A61K 47/48 (2006.01)

Patent

CA 2353832

This invention herein describes polar lipid conjugates and methods of achieving delivery to and accumulation of biologically active compounds including drugs into organs, tissues and cells, particularly at physiologically protected sites, at pharmicokinetically useful levels. These polar lipid conjugates of this invention permit drug concentrations to be achieved, especially in such physiologically protected sites, at levels at which such compounds are therapeutically effective after administration of systemic levels much lower than currently attainable otherwise. This technology is appropriate for use with antiproliferative, antineoplastic, antibiotic, antibacterial, antimycotic or antiviral drugs, agents and compounds, for rapid and efficient introduction of such agents, for example across the blood-brain barrier.

Cette invention décrit des conjugués lipidiques polaires et des procédés permettant d'effectuer l'apport et l'accumulation de composés biologiquement actifs, tels que des médicaments, dans des organes, des tissus et des cellules, notamment au niveau de sites physiologiquement protégés, à des niveaux utiles d'un point de vue pharmacocinétique. Ces conjugués lipidiques polaires permettent d'atteindre des concentrations de médicaments, notamment au niveau de ces sites physiologiquement protégés, à des niveaux auxquels ces composés sont thérapeutiquement efficaces après administration de quantités systémiques très inférieures à ce qui peut être obtenu couramment. Cette technique convient pour des médicaments, des agents et des composés antiprolifératifs, antinéoplasiques, antibiotiques, antibactériens, antimycotiques ou antiviraux, en vue d'une introduction rapide et efficace de ces agents, par exemple à travers la barrière hémato-encéphalique.

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