Pharmaceutical applications of hydrotropic polymer micelles

摘要

Hydrotropic polymer micelles effective for increasing the water solubility of poorly soluble drugs are described. Such hydrotropic polymer micelles have the combined properties of polymer micelles and hydrotropic agents, which display a synergistic effect for increasing the solubility of such drugs. Hydrotropic polymer micelles are formed in solution from amphiphilic copolymers that comprise a hydrophilic polymer and a hydrophobic polymer having pendant hydrotropic agents. A preferred copolymer is a di-, tri- or multi-block copolymer composed of hydrophilic and hydrophobic polymer chains. A particularly preferred hydrophilic chain comprises polyethyleneoxide (PEG) and a preferred hydrophobic chain comprises hydrotropic monomer units derived from nicotinamide. The micelles are found to be much more effective in solubilizing poorly soluble drugs and exhibit an excellent long-term stability even at high loading of drugs. A hydrotropic polymer micelle has nanometer scale size, by which they can deliver poorly soluble drugs to the body through diverse routes of administration.