FORMULATIONS AND CARRIER SYSTEMS INCLUDING FARNESYLTHIOSALYCYLIC MOITIES

摘要

A method of forming or creating a formulation for a compound to be delivered includes creating a carrier agent by conjugating at least one hydrophobic domain or hydrophobic compound with at least one hydrophilic domain or hydrophilic compound and associating the compound to be delivered with the carrier agent to create the formulation. The at least one hydrophobic compound has the formula:;;wherein R1 is a farnesyl group, a geranyl group or geranyl-geranyl group, X is O, S, SO, SO2, NH or Se, Z is C—R2 or N, R2 is H, CN, CO2R7, SO3R7, CONR7R8 or SO2NR7R8, wherein R7 and R8 are each independently H, an alkyl group, an alkenyl group, CO2M or SO3M, wherein M is a cation and R3, R4, and R5 are independently H, a carboxyl group, an alkyl group, an alkenyl group, an aminoalkyl group, a nitroalkyl group, a nitro group, a halo atom, an amino group, a mono-alkylamino group, a di-alkylamino group, mercapto group, a mercaptoalkyl group, an azido group or a thiocyanato group. A plurality of the carrier agents are adapted to assemble into a structure. The hydrophobic compound is cleavably conjugated to the at least one hydrophilic compound via a linkage which is labile in vivo.

主权项

1. A formulation, comprising:
a carrier agent formed by conjugating at least one biologically active hydrophobic compound with at least one hydrophilic compound, the at least one biologically active hydrophobic compound having the formula:wherein R1 is a farnesyl group, a geranyl group or geranyl-geranyl group, X is O, S, SO, SO2, NH or Se, Z is C—R2 or N, R2 is H, CN, CO2R7, SO3R7, CONR7R8 or SO2NR7R8, wherein R7 and R8 are each independently H, an alkyl group, an alkenyl group, CO2M or SO3M, wherein M is a cation and R3, R4, and R5 are independently H, a carboxyl group, an alkyl group, an alkenyl group, an aminoalkyl group, a nitroalkyl group, a nitro group, a halo atom, an amino group, a mono-alkylamino group, a di-alkylamino group, mercapto group, a mercaptoalkyl group, an azido group or a thiocyanato group, wherein a plurality of the carrier agents are adapted to assemble into a structure and the at least one biologically active hydrophobic compound is conjugated with the at least one hydrophilic compound via a linkage which is labile in vivo, and
a biologically active compound associated with the carrier agent.