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Pure Appl. Chem., 2011, Vol. 83, No. 11, pp. 2027-2040

Published online 2011-08-27

Chitosan nanoparticles for tamoxifen delivery and cytotoxicity to MCF-7 and Vero cells

Neralakere Ramanna Ravikumara1,2 and Basavaraj Madhusudhan2*

1 Department of Biochemistry, P.G. Centre, Kuvempu University, Shivagangothri, Davanagere 577 002, Karnataka, India
2 Research Center for Nanoscience and Technology, Department of Biochemistry and Food Technology, Davanagere University, Shivagangothri, Davanagere 577 002, Karnataka, India

Abstract: In this study, tamoxifen citrate-loaded chitosan nanoparticles (tamoxcL-ChtNPs) and tamoxifen citrate-free chitosan nanoparticles (tamoxcF-ChtNPs) were prepared by an ionic gelation (IG) method. The physicochemical properties of the nanoparticles were analyzed for particle size, zeta (ζ) potential, and other characteristics using photon correlation spectroscopy (PCS), zeta phase analysis light scattering (PALS), scanning electron microscopy (SEM), Fourier transform infrared (FTIR), and differential scanning calorimetry (DSC). The variation in particle size was assessed by changing the concentration of chitosan, pentasodium tripolyphosphate (TPP), and the pH of the solution. The optimized tamoxcL‑ChtNPs showed mean diameter of 187 nm, polydispersity of 0.125, and ζ-potential of +19.1 mV. The encapsulation efficiency (EE) of tamoxifen citrate (tamoxc) increased at higher concentrations, and release of tamoxc from the chitosan matrix displayed controlled biphasic behavior. Those tamoxcL-ChtNPs tested for chemosensitivity showed dose- and time-dependent antiproliferative activity of tamoxc. Further, tamoxcL-ChtNPs were found to be hemocompatible with human red blood cells (RBCs) and safe by in vitro cytotoxicity tests, suggesting that they offer promise as drug delivery systems in therapy.