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A series of 1,2-dihydroquinoline derivatives were synthesized and evaluated for cytotoxicity in HeLa, Hep G2 and 6HEK-293T cell lines. EEDQ2 was identified as a promising anti-cancer agent with low IC50 in HeLa (18.55μg/ml) and Hep G2 (14.53μg/ml) cells. For improving the antitumor activity and tumor selectivity of EEDQ2, we prepared transferrin (Tf)-modified liposomes (LPs) to deliver EEDQ2. When HeLa and Hep G2 cells were treated with LP-delivered EEDQ2, the ROS level was significantly enhanced, and mitochondrial membrane potential was reversed. Tf-LPs improved cell uptake of EEDQ2 by about 3.7 times compared with non-targeted LPs. These data suggest that Tf-LPs delivering EEDQ2 is a promising strategy to treat cancer. [ABSTRACT FROM AUTHOR]

The aim of this review is to summarize advances that have been made in the delivery of phytochemicals for cancer therapy by the use of nanotechnology. Over recent decades, much research effort has been invested in developing phytochemicals as cancer therapeutic agents. However, several impediments to their wide spread use as drugs still have to be overcome. Among these are low solubility, poor penetration into cells, high hepatic disposition, and narrow therapeutic index. Rapid clearance or uptake by normal tissues and wide tissue distribution result in low drug accumulation in the target tumor sites can result in undesired drug exposure in normal tissues. Association with or encapsulation in nanoscale drug carriers is a potential strategy to address these problems. This review discussed lessons learned on the use of nanotechnology for delivery of phytochemicals that been tested in clinical trials or are moving towards the clinic. [ABSTRACT FROM AUTHOR]

Docetaxel (DTX) is commonly used for breast cancer treatment. Tween 80 used for DTX dissolution in its clinical formulation causes severe hypersensitivity and other adverse reactions. In this study, trastuzumab (Tmab)-coated lipid-polymer hybrid nanoparticles (PLNs) were prepared, composed of poly (d, l -lactide- co -glycolide), PLGA; polyethylenimine (PEI); and lipids. The PLGA/PEI/lipid formed a hydrophobic core, while Tmab was electrostatically adsorbed on the surface of the PLNs as a ligand that targets human epidermal growth factor receptor 2 (HER2)-positive breast cancer cells. The resulting PLNs, electrostatically adsorbed Tmab-bearing PLGA/PEI/lipid nanoparticles (eTmab-PPLNs), had a mean particle size of 217.4 ± 13.36 nm, a ζ potential of 0.056 ± 0.315 mV, and good stability. In vitro, the eTmab-PPLNs showed increased cytotoxicity in HER2-postive BT474 cells but not in HER2-negative MCF7 cells. Studies of the ability of eTmab-PPLNs to target HER2 were performed. The uptake of eTmab-PPLNs was shown to be dependent on HER2 expression level. Therefore, eTmab-PPLNs provide a promising therapeutic for the treatment of breast cancer. [ABSTRACT FROM AUTHOR]