Nano/microscale biomaterials with therapeutic actions can play a pivotal role in restoring regenerative process of tissues. Among others, some of the particulate forms are discussed here that can action either at the extra or intracellular space of damaged or diseased tissues. Particle actions including the release of therapeutic ions or scavenging of molecules significantly alter the initial/intermediate events (e.g., angiogenesis or inflammation), which ultimately can help restoring regenerative functions.