The present application belongs to the field of biopharmaceutical technology and particularly relates to a drug-loaded ganglioside micelle and a method for preparing and use thereof. The present application provides a use of GM1 or a derivative thereof as a carrier material of nano drug delivery system. The blood brain barrier is a key barrier to intracranial drug delivery. The nano drug delivery system provides a powerful tool for non-invasive intracranial combined administration and has important clinical significance. Without introducing other carrier materials, long-circulating modifying materials and nerve repair drugs, the drug-loaded ganglioside micelle prepared by using GM1 or a derivative thereof as a carrier material of nano drug delivery system can achieve nerve injury repair and intracranial combined administration by penetrating the blood-brain barrier. The drug-loading ganglioside micelle in the present application is expected to provide a new perspective and method for improving clinical treatment.