Transferrin-conjugated Docetaxel-PLGA nanoparticles for tumor targeting: Influence on MCF-7 cell cycle

Sajan Jose, Thomas A. Cinu, Rosmy Sebastian, M. H. Shoja, N. A. Aleykutty, Alessandra Durazzo, Massimo Lucarini, Antonello Santini, Eliana B. Souto

Research output: Contribution to journalArticlepeer-review

34 Citations (Scopus)


Targeted drug delivery systems are commonly used to improve the therapeutic index of anti-cancer drugs by increasing their selectivity and reducing systemic distribution and toxicity. Ligand-conjugated nanoparticles (NPs) can be effectively applied for active chemotherapeutic targeting to overexpressed receptors of tumor cells. In this study, transferrin (Tf ) was successfully conjugated with poly-l-lactic-co-glycolic acid (PLGA) using ethylene diamine confirmed by NMR, for the loading of docetaxel trihydrate (DCT) into PLGA nanoparticles (NPs). The DCT-loaded Tf -conjugated PLGA NPs were produced by an emulsion-solvent evaporation technique, and a 32 full factorial design was used to optimize the nanoparticle formulations. The DCT-loaded Tf -conjugated PLGA NPs were characterized by FTIR spectroscopy, differential scanning calorimetry, powder X-ray diffraction (PXRD), TEM, particle size, and zeta potential analysis. In vitro release kinetics confirmed that release of DCT from the designed formulations followed a zero-order kinetics and a diffusion controlled non-Fickian release profile. The DCT-loaded Tf -conjugated PLGA NPs were evaluated in vitro in MCF-7 cells for bioactivity assessment. Cytotoxicity studies confirmed that the Tf -conjugated PLGA NPs were more active than the non-conjugated counterparts. Cell uptake studies re-confirmed the ligand-mediated active targeting of the formulated NPs. From the cell cycle analysis, the anti-cancer activity of DCT-loaded Tf -conjugated PLGA NPs was shown to occur by arresting the G2/M phase.

Original languageEnglish
Article number1905
Issue number11
Publication statusPublished - 01-11-2019
Externally publishedYes

All Science Journal Classification (ASJC) codes

  • Chemistry(all)
  • Polymers and Plastics


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