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The nanoparticle composition was optimized for high serum stability and low protein binding.
However, for the elimination of free malignant cells in circulating blood, high serum stability and specificity to tumor cells are of great importance.
Our results indicate that the NMeGly for Gly substitution and the Sta-Leu substitution at the C-terminus confer high serum stability while maintaining high receptor affinity, resulting in biodistribution properties that outperform those of the other peptides.
Fluorescence quenching assays and molecular dynamics (MD) simulations revealed that the high serum stability of the dendron micelles can be attributed to reduced micelle-serum protein interactions, owing to their dendritic, dense PEG outer shell.
HAI-NGs were obtained with a small size of ca. 90 nm, bright green fluoresence and high serum stability from hyaluronic acid-cystamine-tetrazole and reductively degradable polyiodixanol-methacrylate via nanoprecipitation and a photo-click crosslinking reaction.
What's more, the drug loading nanocarriers owns high serum stability, which can contribute to long-time circulation in the blood vessels, resulting in long-lasting antitumor activities, especially for the killing of free malignant cells in circulating blood [12, 17, 18].
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The newly developed delivery vector was designed to impart bioreducibility for greater intracellular pDNA release, higher serum stability and efficient complexing ability by incorporating disulfide linkage, PEG and low molecular weight polyethylenimine, respectively.
In the case of Lfc5 however, its higher serum stability compensated for the lower activity so that its activity in serum is close to that of Lfc6.
Indeed, MPI-1 is more efficient in suppresssing tumor growth of sarcoma xenograft in mice than MPI, which was attributed to its higher serum stability.
While both G2 and G3 bolaamphiphiles are highly efficient for siRNA transfection, G2 vectors exhibit much higher serum stability than G3 analogues.
Furthermore, peptoids have high serum-stability [ 13], are non-immunogenic [ 34], and are cell permeable [ 35], thus making them good candidates for use in drug discovery.
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