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Using drug-excipient interactions for siRNA delivery |
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| Authors: | Bruno Katharina |
| Institution: | |
| Abstract: | SiRNA is the trigger of RNA interference, a mechanism discovered in the late 1990s. To release the therapeutic potential of this versatile but large and fragile molecule, excipients are used which either interact by electrostatic interaction, passively encapsulate siRNA or are covalently attached to enable specific and safe delivery of the drug substance. Controlling the delicate balance between protective complexation and release of siRNA at the right point and time is done by understanding excipients-siRNA interactions. These can be lipids, polymers such as PEI, PLGA, Chitosans, Cyclodextrins, as well as aptamers and peptides. This review describes the mechanisms of interaction of the most commonly used siRNA delivery vehicles, and looks at the results of their clinical and preclinical studies. |
| Keywords: | AFM atomic force microscopy ApoB Apolipoprotein B AMD age related macular degeneration Bp base-pairs bPEI branched PEI CDP Cyclodextrin-containing polymers CPP cell penetrating peptide D5W 5% (w/v) glucose in water DD deacetylation degree DLS Dynamic light scattering ds double-stranded IL Interleukin ITC Isothermal titration calorimetry i v intravenous mRNA messenger RNA MW molecular weight N/P ratio Nitrogen to Phosphor ratio PAMAM poly(amidoamine) PEG polyethylene glycol PEI Polyethyleneimine R8 octaarginine RES reticuloendothelial system RISC RNA-induced silencing complex RNAi RNA interference SAXS Small angle X-ray scattering shRNA small hairpin RNA siRNA small interfering RNA STR-R8 stearyl octaarginine t½ half-life TEM transmission electron microscopy TLR Toll-like receptor TNF-α Tumor necrosis factor-α VEGF Vascular Endothelial Growth Factor |
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