Bile acid oligomer conjugate for novel vesicular transport and use thereof

A composition for oral administration, comprising:

• an end site-specific macromolecule-bile acid oligomer conjugate in which the macromolecule is a heparin;
• and
• a solubilizer, wherein:
• the bile acid oligomer is of Formula 2:
• wherein:
• n=2 to 3;
• each of R1 and R2 is a bile acid residue, and R1 and R2 are the same bile acid residue;
• L is a linker having a functional group comprising an amine group;
• the linker is conjugated to the terminal site of the heparin;
• and
• the linker is ethylenediamine (EDA).

A formulation for oral administration, comprising:

• an end site-specific macromolecule-bile acid oligomer conjugate, wherein the macromolecule is a heparin;
• a solubilizer;
• an excipient;
• a disintegrant;
• a binder;
• and
• a lubricant,
• wherein:
• the bile acid oligomer is of Formula 2:
• wherein:
• n=2 to 3;
• each of R1 and R2 is a bile acid residue, and R1 and R2 are the same bile acid residue;
• L is a linker having a functional group comprising an amine group;
• the linker is conjugated to the terminal site of the heparin via a carbonyl group at the end site of the heparin;
• and
• the linker is ethylenediamine (EDA).

A pharmaceutical composition, comprising a heparin-bile acid oligomer conjugate, wherein:

• the bile acid oligomer is of Formula 2:
• wherein:
• n=2 to 3;
• each of R1 and R2 is a bile acid residue, and R1 and R2 are the same bile acid residue;
• L is a linker having a functional group comprising an amine group;
• the linker is conjugated to the terminal site of the heparin via a carbonyl group of a reducing unit at the end site of the heparin;
• and
• the linker is ethylenediamine (EDA).