A - Human Necessities – 61 – K
Patent
A - Human Necessities
61
K
A61K 9/127 (2006.01) A61K 8/14 (2006.01)
Patent
CA 2665783
An amphoteric liposome composed of a mixture of lipids, said mixture comprising a cationic amphiphile, an anionic amphiphile and optionally one or more neutral amphiphiles, at least one of said cationic and anionic amphiphiles being chargeable and the respective amounts of said cationic and anionic amphiphiles being selected such there is a stoichiometric excess of positively charged cationic amphiphile at a first lower pH, a stoichiometric excess of negatively charged anionic amphiphile at a second higher pH and said mixture has an isoelectric point intermediate said first and second pHs; characterised in that said positively charged cationic and negatively charged anionic amphiphiles are adapted to form a lipid salt with one another at said isoelectric point. Also disclosed are methods of predicting the fusogenicity of an amphoteric liposome at a given pH, formulating an amphoteric liposome and loading an amphoteric liposome with a cargo moiety.
L'invention concerne un liposome amphotère composé d'un mélange de lipides, ledit mélange comprenant un amphiphile cationique, un amphiphile anionique et éventuellement un ou plusieurs amphiphiles neutres, au moins un desdits amphiphiles cationique et anionique pouvant être chargé. Les quantités respectives desdits amphiphiles cationique et anionique sont choisies de sorte qu'il y ait un excès stAEchiométrique d'amphiphile cationique chargé positivement à un premier pH faible, un excès stAEchiométrique d'un amphiphile anionique chargé négativement à un second pH élevé et ledit mélange ayant un point isoélectrique intermédiaire entre lesdits premier et second pH. Le liposome est caractérisé en ce que lesdits amphiphiles cationique chargé positivement et anionique chargé négativement sont adaptés afin de former un sel de lipide l'un avec l'autre audit point isoélectrique. L'invention concerne également des procédés de prédiction de la fusogénicité d'un liposome amphotère à un pH donné, de formulation d'un liposome amphotère et de charge d'un liposome amphotère avec un groupement de chargement.
Lutz Silke
Muller Claudia
Panzner Steffen
Siepi Evgenios
Blake Cassels & Graydon Llp
Marina Biotech Inc.
Novosom Ag
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