The objective of this study is to show how therapeutically effective a combination of a drug delivery system (DDS) and ultrasound (US) is by introducing data from two related experiments. Fullerene (C60) was chemically modified by polyethylene glycol (PEG) for water‐solubilization and tumour targeting. When the PEG‐modified C60 was injected intravenously into tumour bearing mice, followed by US irradiation to the tumour site, a synergistic anti‐tumour effect was observed. Following the intravenous injection of interferon (IFN) conjugated with pullulan which has an inherent affinity for the liver, and subsequent US irradiation to the liver, the activity level of an IFN‐specific enzyme was significantly enhanced compared with that of the conjugate injection alone.

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