2017
DOI: 10.1002/adma.201705436
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Dimeric Drug Polymeric Micelles with Acid‐Active Tumor Targeting and FRET‐Traceable Drug Release

Abstract: Trans-activating transcriptional activator (TAT), a cell-penetrating peptide, is extensively used for facilitating cellular uptake and nuclear targeting of drug delivery systems. However, the positively charged TAT peptide strongly interacts with serum components and undergoes substantial phagocytosis by the reticuloendothelial system, causing a short blood circulation in vivo. In this work, an acid-active tumor targeting nanoplatform DA-TAT-PECL is developed to inhibit the nonspecific interactions of TAT in t… Show more

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Cited by 127 publications
(76 citation statements)
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“…Their results demonstrate that the targeting molecule significantly increased tumor‐specific cellular uptake and enhanced the treatment efficacy compared with unmodified nanocapsules. Another similar nanosystem has been developed with TAT as a tumor‐targeting reagent to promote nanoparticles penetrating into the tumor cells . Similarly, ligand‐modified nanoplatforms targeting for brain disease therapy are found to selectively permeate through the blood–brain barrier (BBB) compared to pristine nanoparticles .…”
Section: Key Features Of Nanoparticles Required For Efficient Cancer mentioning
confidence: 99%
“…Their results demonstrate that the targeting molecule significantly increased tumor‐specific cellular uptake and enhanced the treatment efficacy compared with unmodified nanocapsules. Another similar nanosystem has been developed with TAT as a tumor‐targeting reagent to promote nanoparticles penetrating into the tumor cells . Similarly, ligand‐modified nanoplatforms targeting for brain disease therapy are found to selectively permeate through the blood–brain barrier (BBB) compared to pristine nanoparticles .…”
Section: Key Features Of Nanoparticles Required For Efficient Cancer mentioning
confidence: 99%
“…The amino group on the surface of PAMAM reacted with the succinimide of MAL-PEG-NHS, while the disappearance of the characteristic peak of MAL in the 1 H NMR spectrum of PAMAM-PEG-EpDT3 further suggested that EpDT3 was linked to PEG. The introduction of PEG not only partially blocks the positive electricity of PAMAM and reduces toxicity but also makes PAMAM-PEG as the gene carrier with prolonged circulatory effect [30]. Consequently, PAMAM-PEG-EpDT3 was formed due to the reaction between the sulfhydryl of EpDT3 and MAL on one end of the PEG chain ( Figure 2C).…”
Section: Resultsmentioning
confidence: 99%
“…Some tumor‐targeting ligands have indeed proved their value in enhancing the tumor‐targeting efficiency of nanomedicines . Activated tumor‐targeting has recently been proven to be a more effective method for tumor‐targeting . In order to improve the therapeutic outcome of dye‐based nanomedicines and to provide activated targeting and drug release properties, peptides can be introduced.…”
Section: Introductionmentioning
confidence: 99%