Objective To find an effective method for the treatment of malignant cerebral glioma by opening the blood-brain-barrier (BBB).Methods The concentration of methotrexate (MTX) in tumor was measured in 18 patients with cerebral glioma, and 155 patients with malignant glioma were treated by intracarotid infusion of papaverine and Bis-chloronitrosourea (BCNU).Results After intracarotid infusion of papaverine for reversible opening of BBB, the MTX concentration in tumor tissue was 1810±380 ng/g, higher than that in patients without papaverine infusion (997±126 ng/g). Eighty-nine patients with glioblastoma and 66 patients with anaplastic astrocytoma received intracarotid infusion of papaverine and BCNU (250 mg) for an average of 2.14 times. The mean survival time of thesepatients was 114.5 weeks, median survival time was 140 weeks, and five-year survival rate was 22.97%.Conclusion The combined chemotherapy with papaverine and BCNU through intra-arterial infusion is simple, safe and effective in treating malignant cerebral glioma so long as the tumor is sensitive to the drugs.