Improvements in or relating to amphoteric liposomes

Details Improvements in or relating to amphoteric liposomes Improvements in or relating to amphoteric liposomes

A - Human Necessities

61

K

A61K 9/127 (2006.01) A61P 1/00 (2006.01) A61P 1/04 (2006.01) A61P 3/10 (2006.01) A61P 5/16 (2006.01) A61P 11/06 (2006.01) A61P 17/06 (2006.01) A61P 19/02 (2006.01) A61P 25/00 (2006.01) A61P 37/06 (2006.01)

Patent

CA 2622584

A serum-stable mixture of lipids capable of encapsulating an active agent to form a liposome, said mixture comprising phosphatidylcholine and phosphatidylethanolamine in a ratio in the range of about 0.5 to about 8. The mixture may also include pH sensitive anionic and cationic amphiphiles, such that the mixture is amphoteric, being negatively charged or neutral at pH 7.4 and positively charged at pH 4. Amphoteric liposomes comprising such a mixture may be used for encapsulating nucleic acid therapeutics, such as oligonucleotides and DNA plasmids. The drug/lipid ratio may be adjusted to target the liposomes to particular organs or other sites in the body.

La présente invention se rapporte à un mélange de lipides stable dans le sérum, qui permet d'encapsuler un agent actif afin de former un liposome, ledit mélange contenant de la phosphatidylcholine et de la phosphatidyléthanolamine, présentes selon un rapport compris entre 0,5 environ et 8 environ. Le mélange selon l'invention peut également renfermer des molécules amphiphiles anioniques et cationiques sensibles au pH, de façon que le mélange soit amphotère, à savoir chargé négativement ou neutre à un pH de 7,4 et chargé positivement à un pH de 4. Il est possible d'utiliser des liposomes amphotères contenant un tel mélange pour encapsuler des substances thérapeutiques à base d'acides nucléiques, telles que des oligonucléotides et des plasmides ADN. Le rapport médicament/lipide peut être ajusté afin que les liposomes puissent être ciblés vers des organes particuliers ou d'autres sites de l'organisme.

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