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Novel, biocompatible polyplexes, based on the combination of cationic pentablock copolymers with folic acid functionalized copolymers, were designed and developed for target-specific siRNA delivery. The resulting micelleplexes spontaneously formed polymeric micelles with a hydrophobic core surrounded directly by a cationic poly-2-(4-aminobutyl)-oxazole (PABOXA) and subsequently shielded by hydrophilic poly-2-methyl-oxazole (PMOXA) layer. The described micelleplexes form highly stable particles even in complete serum after 24 h compared with the highly cationic polymer PEI, which show aggregate formation in serum containing buffer solution. Targeted siRNA delivery and gene knockdown could be shown using green fluorescent protein (GFP) expressing HeLa cells, resulting in ∼31% and ∼8% suppression of the expression of GFP for targeted and nontargeted micelleplexes, respectively. Comparison studies of folic-receptor positive HeLa cells with normal folic-receptor-negative HEK293 cells revealed involvement of re...
| Authors: | Roman Lehner; Kegang Liu; Xueya Wang; Patrick Hunziker | |
| Journal: | Biomacromolecules | |
| Year: | 2017 | |
| DOI: | 10.1021/acs.biomac.7b00851 | |
| Publication date: | 25-Jul-2017 |
Chemokine receptor CXCR4 plays an important role in cancer cell invasion and metastasis. Recent findings suggest that anti-VEGF therapies upregulate CXCR4 expression, which contributes to resistance to antiangiogenic therapies. Here, we report the development of novel derivatives of polyeth ... more
The molecular structures of three parthenolide analogues, (−)-goyazensolide (1), (−)-15-deoxygoyazensolide (2), and (−)-ereglomerulide (3), isolated from the leaves of Piptocoma rufescens in a previous study were determined by X-ray analysis, and the absolute configuration of (−)-goyazensol ... more
Mutual Impact of Phase Separation/Crystallization and Water Sorption in Amorphous Solid Dispersions
The molecular integration of poorly water soluble active pharmaceutical ingredients (APIs) in a suitable polymeric matrix is a possible approach to enhance the dissolution behavior and solubility of these APIs. Like all newly developed pharmaceutical formulations, these formulations (often ... more
Discovery of a biochemical basis for broccoli's cancer-fighting ability
Scientists are reporting discovery of a potential biochemical basis for the apparent cancer-fighting ability of broccoli and its veggie cousins. They found for the first time that certain substances in the vegetables appear to target and block a defective gene associated with cancer. Their ... more
Faster, more cost-effective DNA test for crime scenes, disease diagnosis
Scientists in Japan are reporting development of a faster, less expensive version of the fabled polymerase chain reaction (PCR) a DNA test widely used in criminal investigations, disease diagnosis, biological research and other applications. The new method could lead to expanded use of PCR ... more
'Nanoshells' simultaneously detect and destroy cancerous cells
Researchers at Rice University in Texas have developed a new approach to fighting cancer, based on nanoscale particles that can both detect and destroy cancerous cells. The report appears in the American Chemical Society's journal Nano Letters. Current molecular imaging approaches only dete ... more
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