Background <p>Melatonin (MEL) is a neurohormone with recognized antioxidant and antitumor properties. However, its therapeutic efficacy is limited due to low bioavailability and solubility in physiological media. To overcome these barriers, albumin-based nanoparticles have emerged as promising carriers in drug delivery systems.</p> Objective <p>This study aimed to develop and evaluate melatonin-loaded bovine serum albumin nanoparticles (BSA-NPs) produced by ionizing radiation as a chemically clean platform for selective drug delivery in cancer therapy.</p> Methods <p>BSA nanoparticles were synthesized using two distinct approaches: mechanical agitation (NPs–MEL A) and gamma irradiation from a <sup>60</sup>Co source (NPs–MEL I), without chemical crosslinkers. The formulations were characterized by dynamic light scattering, Zeta potential analysis, and scanning electron microscopy. <i>In vitro</i> cytotoxicity was evaluated using NIH3T3 fibroblasts and MCF7 human breast cancer cells through the MTT assay. Melatonin release profiles were also assessed under physiological conditions.</p> Results <p>The irradiated nanoparticles exhibited improved colloidal stability, with a strongly negative Zeta potential (− 57.25 mV) and a controlled melatonin release profile, reaching approximately 68% after 48&#xa0;h. In cytotoxicity assays, NPs–MEL I significantly reduced MCF7 cell viability to approximately 25%, while maintaining cell viability above 90% in NIH3T3 fibroblasts. In contrast, nanoparticles produced by mechanical agitation showed lower selectivity between tumor and nontumor cells.</p> Conclusion <p>Gamma irradiation proved to be an effective strategy for producing stable albumin nanoparticles capable of selectively enhancing melatonin’s antitumor activity while preserving normal cell viability. These findings support the potential of radiation-produced BSA nanoparticles as a promising <i>in vitro</i> model for selective anticancer drug delivery.</p>

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Synthesis, characterization and cytotoxicity of gamma-irradiated albumin nanoparticles conjugated with melatonin

  • Cássia Priscila Cunha da Cruz,
  • Murilo Álison Vigilato Rodrigues,
  • Ademar Benévolo Lugão

摘要

Background

Melatonin (MEL) is a neurohormone with recognized antioxidant and antitumor properties. However, its therapeutic efficacy is limited due to low bioavailability and solubility in physiological media. To overcome these barriers, albumin-based nanoparticles have emerged as promising carriers in drug delivery systems.

Objective

This study aimed to develop and evaluate melatonin-loaded bovine serum albumin nanoparticles (BSA-NPs) produced by ionizing radiation as a chemically clean platform for selective drug delivery in cancer therapy.

Methods

BSA nanoparticles were synthesized using two distinct approaches: mechanical agitation (NPs–MEL A) and gamma irradiation from a 60Co source (NPs–MEL I), without chemical crosslinkers. The formulations were characterized by dynamic light scattering, Zeta potential analysis, and scanning electron microscopy. In vitro cytotoxicity was evaluated using NIH3T3 fibroblasts and MCF7 human breast cancer cells through the MTT assay. Melatonin release profiles were also assessed under physiological conditions.

Results

The irradiated nanoparticles exhibited improved colloidal stability, with a strongly negative Zeta potential (− 57.25 mV) and a controlled melatonin release profile, reaching approximately 68% after 48 h. In cytotoxicity assays, NPs–MEL I significantly reduced MCF7 cell viability to approximately 25%, while maintaining cell viability above 90% in NIH3T3 fibroblasts. In contrast, nanoparticles produced by mechanical agitation showed lower selectivity between tumor and nontumor cells.

Conclusion

Gamma irradiation proved to be an effective strategy for producing stable albumin nanoparticles capable of selectively enhancing melatonin’s antitumor activity while preserving normal cell viability. These findings support the potential of radiation-produced BSA nanoparticles as a promising in vitro model for selective anticancer drug delivery.