Liposomal composition for convection-enhanced delivery to...

A - Human Necessities – 61 – K

Patent

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A61K 9/127 (2006.01) A61K 31/4745 (2006.01) A61K 38/16 (2006.01) A61K 49/18 (2006.01) A61P 25/00 (2006.01)

Patent

CA 2743959

Convection-enhanced delivery (CED) is used as a method to deliver a direct infusion of therapeutic agents to the central nervous centre thus circumventing the blood-blood barrier. A non-PEGylated liposomal composition comprising at least one saturated neutral phospholipid and at least one saturated anionic phospholipid and a therapeutic or diagnostic agent encapsulated therein is used to overcome toxicity associated with high peak drug concentration delivered locally CED as well as to increase tissue distribution volume for an improved sustained drug release. In one embodiment, the liposome composition comprises a molar ratio of DSPC:DSPG:CHOL of 7:2:1 and the therapeutic or diagnostic agent is selected from topotecan, conotoxin, gadodiamide or rhodamine, and is used in the treatment of epilepsy

L'invention porte sur une administration améliorée par convection (CED) qui est utilisée en tant que procédé d'administration d'une infusion directe d'agents thérapeutiques au système nerveux central, contournant ainsi la barrière hémato-encéphalique. On utilise une composition liposomale non PEGylée comprenant au moins un phospholipide neutre saturé et au moins un phospholipide anionique saturé et un agent thérapeutique ou de diagnostic encapsulé dans celui-ci pour surmonter la toxicité associée à une concentration de médicament à pic élevé administrée localement (CED) ainsi que pour augmenter le volume d'administration au tissu pour une libération de médicament entretenue améliorée. Dans un mode de réalisation, la composition du liposome comprend un rapport molaire de DSPC:DSPG:CHOL de 7:2:1 et l'agent thérapeutique ou de diagnostic est choisi parmi le topotécane, la conotoxine, le gadodiamide ou la rhodamine, et on l'utilise dans le traitement de l'épilepsie.

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