Abstract: | Monodispersed bioactive glass nanoparticles (BGNs) have received much attention in various biomedical applications such as tissue regeneration, drug/gene delivery, bioimaging, and cancer therapy. However, the poor dispersion stability of BGNs in a physiological environment has limited their wide biomedical applications. The long‐term in vitro/in vivo toxicity and biodegradation of BGNs are also not clear. Monodispersed glycerolphosphate‐functionalized BGNs (GP‐BGN) are synthesized and their stability under physiological environment in vitro, and long‐term biodegradation behavior in vitro and in vivo are investigated herein. GP‐BGN shows significantly enhanced particles stability in physiological environment, good hemocompatibility and cellular biocompatibility, as well as high cellular uptake ability. GP‐BGN also exhibits long‐term biodegradation behavior in vitro/in vivo and negligible biotoxicity (tissue and blood toxicity). This study demonstrates that monodispersed surface‐functionalized BGNs could be used as biocompatible and biodegradable nanomaterials for long‐term safe bioimaging and disease therapy. |