Theranostics, a new medical term that combines therapeutics and diagnostics is considered an ideal system for medical care. Ultrasound is considered one of the most reasonable energies for the development of theranostics. Additionally, microbubbles, which are ultrasound contrast agents, have received considerable attention for their effectiveness in diagnosis and therapy. Microbubbles are composed of an inner gas and an outer shell composed of proteins or phospholipids. Under ultrasound exposure, the oscillation or collapse of microbubbles is induced depending on the intensity of the ultrasound. These mechanical effects are important for imaging, drug delivery, and ablation therapies. Therefore, it is essential that microbubbles reach the targeted site and induce mechanical effects to achieve effective and efficient diagnosis and therapy. We have previously developed novel microbubbles with high stability by optimizing the outer shell composition. Recently, microbubbles containing distearoylphosphatidyl glycerol showed high stability and prolonged circulation in the blood. These novel microbubbles may be useful for diagnosis and therapy. The combination of microbubbles and ultrasound has received considerable attention for brain-targeted drug delivery applications. We examined whether microbubbles can be used for brain-targeted drug delivery and evaluated the effect of the encapsulated gas on drug delivery. Thus, novel microbubbles combined with ultrasound can deliver molecules to the brain. Microbubbles containing perfluoropropane or perfluorobutane could efficiently deliver molecules to the brain. The novel microbubbles have long-circulating properties in the blood and could deliver molecules to the brain. The combination of novel microbubbles and ultrasound would contribute to the development of efficient thranostic systems.