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