Transferrin tagged lipid nanoemulsion of docetaxel for enhanced tumor targeting

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• 作者：Syed Muzammil Afzal^a ; Mohammad Zubair Shareef^b ; Veerabrahma Kishan^a ; ^{vbkishan@yahoo.com}
• 关键词：Transferrin tagged docetaxel lipid emulsion ; Non-invasive imaging study ; Fluorescent tissue distribution study ; Enhanced tumor targeting ; Improved antitumor activity ; Solid tumor targeting
• 刊名：Journal of Drug Delivery Science and Technology
• 出版年：2016
• 出版时间：December 2016
• 年：2016
• 卷：36
• 期：Complete
• 页码：175-182
• 全文大小：1174 K
• 卷排序：36

文摘

The objective was to develop transferrin coupled docetaxel lipid nanoemulsion (FT) for improving tumor targeted delivery. The plain lipid nanoemulsion (LNE) was prepared by homogenization and ultrasonication process (FP). Transferrin was tagged to stearylamine containing lipid nanoemulsion (FS) globules using EDC reaction. The prepared LNEs were characterized for size, PDI, zeta potential and in vitro release. The in vitro cytotoxic studies of the delivery systems were performed on MCF-7 and HeLa cells. MDA-MB 231 cells were xenografted in Balb/c mice and the tumor targeting efficiency was tested on it using imaging system. Further, the tumor regression studies were performed in tumor induced C57BL/6 mice. The prepared LNEs were in the size range of 200–393 nm, The IC 50 values of FT on both the cell lines were statistically significant. The % tumor inhibition for the groups treated with FP, FS and FT when compared to untreated control was found to be 55.62 ± 5.41%, 54.27 ± 4.85%, and 84.66 ± 4.29% respectively. During the image guided distribution studies, FT was found to be superior in tumor targeting activity in comparison to FP and FS by 3.54 and 2.62 folds respectively. The developed FT has great future potential to improve cancer treatment efficacy by minimizing side effects.