Tuning the morphology of supramolecular aggregates for nanocarrier‐based drug delivery

Abstract Due to the unique drug delivery mode and specific therapy, nano‐formulations are of interest for biomedical applications and treating many diseases. However, traditional method of nano‐formulation construction via additional carriers or structural modifications of therapeutic drugs might be cumbersome or low loading‐efficient. Herein, the kinetics, accessible pathways, and final outcomes of supramolecular assembly processes of therapeutic drugs are investigated in detail. It was found that the supramolecular aggregates of cephradine (CEP) undergoes a morphological transformation from anisotropic nanofiber (EtOH) to isotropic spherical nanoparticle (H 2 O), similar to “plants took root, sprouted, blossomed and bore fruit.” Moreover, the assembly kinetics results reveal the assembly pathways of nucleation elongation in H 2 O and surface‐catalyzed secondary nucleation in EtOH. The method presented in this work has the potential to be used for efficiently designing specific nano‐formulations.