Delivery of small hydrophilic molecules packaged into lipid vesicles
OwnerRobert H.E. Friesen, Berend Poolman +2inventors
InventorsRobert H.E. Friesen, Berend Poolman, Bernard L. Feringa, Jan B.F.N. Engberts
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Abstract
Methods and compositions for the generation of vehicles for delivering small molecules are disclosed. In one aspect, lipid vesicles having a proteinaceous channel and small molecules are generated. The proteinaceous channel and/or the lipid vesicle are formulated such that the small molecule is released in the vicinity of or near a target cell. The target cell may be located in vitro or in vivo.
Claims30
A method for delivering a small hydrophilic molecule to a cell, said method comprising:
- providing a lipid vesicle comprising a proteinaceous channel, wherein said proteinaceous channel, in an open state, allows passage of small hydrophilic molecules therethrough to said lipid vesicle's exterior, said lipid vesicle formulated such that, upon activation, said proteinaceous channel opens;
- loading said lipid vesicle with a small hydrophilic molecule;
- administering said lipid vesicle to a fluid in contact with the cell;
- allowing said lipid vesicle to migrate to said cell's vicinity;
- activating said lipid vesicle;
- and
- thus opening said proteinaceous channel and delivering said small hydrophobic molecule to the cell.
A composition for delivering a small hydrophilic molecule to a target cell, said composition comprising:
- a lipid vesicle comprising the small hydrophilic molecule and a proteinaceous channel having open and closed states;
- and
- wherein said composition is formulated such that said proteinaceous channel is normally in the closed state thus retaining the small hydrophilic molecule therein.
A method of delivering a small hydrophilic molecule to a target tissue in a subject, said method comprising:
- providing a lipid vesicle comprising a mechanosensitive channel of large conductance (MscL) and small hydrophilic molecule;
- and
- parenterally administering said lipid vesicle to the target tissue.
A lipid vesicle for modulating the bio-availability of a small hydrophilic molecule upon administration of said lipid vesicle to a subject, said lipid vesicle comprising:
- a small hydrophilic molecule;
- a proteinaceous channel incorporated into said lipid vesicle wherein an open state of said proteinaceous channel allows passage of said small hydrophilic molecule therethrough to said lipid vesicle's exterior.
Dependencies are inferred from the claim text.