Nanoaggregates sensitive to pH and reduction, a process for the preparation thereof, and a pharmaceutical composition for treating malignant tumor comprising the same

摘要

PURPOSE: A nanoaggregate is provided to deliver a hydrophilic anticancer gene and a hydrophobic chemotherapeutic agent into a cell using one drug delivery system and to deliver an anticancer agent with high efficiency. CONSTITUTION: A nanoaggregate contains 1 micelle unit containing a hydrophobic chemotherapeutic agent conjugated to one end of a biocompatible non-ionic polymer and a hydrophilic anticancer gene conjugated to the other end of the biocompatible non-ionic polymer. The hydrophobic chemotherapeutic agent is conjugated to the biocompatible non-ionic polymer through a reduction-sensitive linker which is isolated under the presence of a reducing agent. The hydrophilic anticancer gene is conjugated to the biocompatible non-ionic polymer through a pH-sensitive linker which is isolated at pH 4-6. The 1 micelle unit has a structure of chemical formula 1. A method for preparing the nanoaggregate comprises: conjugating the hydrophobic chemotherapeutic agent at one end of the biocompatible non-ionic polymer through the reduction-sensitive linker; conjugating the hydrophilic anticancer gene to the other end through the pH-sensitive linker; and dispersing the complex containing the hydrophilic anticancer gene and the hydrophobic chemotherapeutic agent for self-assembling.