Multifunctional nanotherapeutics for intracellular trafficking of doxorubicin against breast cancer - supplementary materials

<b>Aims: </b>To develop an estrone-targeted D-alpha-tocopherol polyethylene glycol 1000 succinate (TPGS)-based liposomal system for enhanced intracellular delivery of doxorubicin (DOX). <b>Materials &amp;methods: </b>Zetasizer, transmission electron microscopy, energy dispersive x-ray, Fourier-transform infrared spectroscopy, differential scanning calorimetry, x-ray diffraction, confocal laser scanning microscopy and FACS analysis were used for formulation characterization and evaluation. <b>Results: </b>The DOX-LIPO-TPGS and DOX-LIPOTPGS- estrone formulations had vesicle sizes (117.6 <b>± </b>3.51; 144 <b>± </b>5.00 nm), zeta potential (-36.4 <b>± </b>0.75; -35.8 <b>± </b>0.76), polydispersity index (0.123 <b>± </b>0.005; 0.169 <b>± </b>0.005) and percent entrapment efficiency (73.56 <b>± </b>3.55; 77.16 <b>± </b>3.83%) with improved cytotoxicity and cellular uptake, confirming the targeted potential of the developed formulations. <b>Conclusion: </b>The results suggest that the developed liposomal formulation with desired characteristics is potentially capable of nonimmunogenic, site-specific drug delivery to targeted cancer sites and reduced DOX-associated cardiac toxicity.