Preparation, Characterization And In Vitro Evaluation Of Stealth Docetaxel Lipid Nanoemulsions For Efficient Cytotoxicity

syed muzammil afzal, Kishan Veerabrahma

Abstract


Docetaxel is currently used in treatment of breast and ovarian cancers, administered in the form of parenteral IV infusion. Lipid nanoemulsion (LNE) delivery system is biocompatible, biodegradable and easy to prepare. The aim of this study was to develop stable parenteral pegylated docetaxel lipid nanoemulsions (LNEs) for improving cytotoxicity. The O/W LNEs were prepared by homogenization and ultrasonication process. The globule sizes and zeta potentials were measured by using Malvern Zetasizer.  The sizes of oil globules varied from 70.2 to 243.3 nm and zeta potential from −25.5 to −40.2mV. During in vitro drug release studies, the cumulative percentage drug released within 15 h from pegylated lipid nanoemulsions, PLNE-3 and PLNE-6 was 84.02±4.79 and 88.51±4.5 respectively. The total drug content and entrapment efficiencies for the prepared LNEs were determined by HPLC. The in vitro cell line studies were performed on two cell lines (MCF-7 and Hela cell lines). When compared to drug solution, PLNE-6 was found to have 1.55 and 1.6 folds more cytotoxic activity on MCF-7 and Hela cell lines respectively. The IC 50 values of pegylated LNEs on both the cell lines was statistically significant when compared to DS, P<0.05. In conclusion, stealth LNEs were prepared, characterized and  found to be stable and superior in delivery of docetaxel  to cancer cell lines in comparison to plain LNE and drug solution.


Keywords


Docetaxel, DSPE-PEG 5000, DPPE-PEG 5000, Stealth Lipid Nanoemulsions, cytotoxicity.

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