Betulinic acid-loaded polymeric nanoparticles: synthesis, characterization and tumor-targeting potential

Cancer remains one of the major global public health challenges, with current treatments often limited by tumor resistance and severe side effects. In this context, natural compounds such as betulinic acid (BA) combined with nanotechnology represent promising alternatives, particularly when tumor-targeting strategies are employed. Therefore, this study aims to develop polymeric nanoparticles (NP) functionalized with a transferrin receptor (TfR1)-targeting peptide to optimize drug delivery and enhance the antitumor activity of BA. This study demonstrated that the NP exhibited favorable physicochemical properties, including colloidal stability and extended circulation time due to PEG. Peptide functionalization influenced the release kinetics of BA and significantly enhanced interaction with MCF-7 cells, evidencing tumor selectivity. Moreover, the nanosystems exhibited hemocompatibility, supporting their potential for intravenous administration and the development of safer, more targeted antitumor therapies. The combination of selectivity, safety, and controlled release makes these NPs promising candidates in oncology. This work advances knowledge of polymeric nanoformulations and supports the development of more targeted antitumor therapies, with future perspectives including formulation optimization, improved functionalization, in vivo studies, and validation across diverse cell models.