Morpholino-terminated dendrimer shows enhanced tumor pH-triggered cellular uptake, prolonged circulation time, and low cytotoxicity

Morpholino-terminated dendrimer shows enhanced tumor pH-triggered cellular uptake, prolonged... Short circulation is a disadvantage of dendrimers as drug delivery carriers due to their small size. In this work, pH-sensitive morpholino-terminated generation 5 poly(amido amine) (PAMAM) is prepared. At neutral pH, the dendrimer has a hydrophilic neutral surface and thereby stealth property. Under tumor acidic environments, the dendrimer develops positive charges due to protonation of the morpholino groups, and cellular uptake of the dendrimer is subsequently enhanced. The dendrimer is predicted to penetrate deeper within the tumor due to its small size (∼9 nm), and thereby the pH-sensitive function can be efficiently achieved because the microenvironment in the deeper sites is more acidic. Moreover, the morpholino-terminated PAMAM exhibited longer in vivo circulation time compared to PAMAM and hydroxyl-terminated PAMAM, partly compensating for the disadvantage of short circulation of dendrimers. Furthermore, the morpholino-terminated PAMAM also showed lower cytotoxicity than PAMAM and hydroxyl-terminated PAMAM. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Polymer Elsevier

Morpholino-terminated dendrimer shows enhanced tumor pH-triggered cellular uptake, prolonged circulation time, and low cytotoxicity

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Publisher
Elsevier
Copyright
Copyright © 2016 Elsevier Ltd
ISSN
0032-3861
D.O.I.
10.1016/j.polymer.2015.12.056
Publisher site
See Article on Publisher Site

Abstract

Short circulation is a disadvantage of dendrimers as drug delivery carriers due to their small size. In this work, pH-sensitive morpholino-terminated generation 5 poly(amido amine) (PAMAM) is prepared. At neutral pH, the dendrimer has a hydrophilic neutral surface and thereby stealth property. Under tumor acidic environments, the dendrimer develops positive charges due to protonation of the morpholino groups, and cellular uptake of the dendrimer is subsequently enhanced. The dendrimer is predicted to penetrate deeper within the tumor due to its small size (∼9 nm), and thereby the pH-sensitive function can be efficiently achieved because the microenvironment in the deeper sites is more acidic. Moreover, the morpholino-terminated PAMAM exhibited longer in vivo circulation time compared to PAMAM and hydroxyl-terminated PAMAM, partly compensating for the disadvantage of short circulation of dendrimers. Furthermore, the morpholino-terminated PAMAM also showed lower cytotoxicity than PAMAM and hydroxyl-terminated PAMAM.

Journal

PolymerElsevier

Published: Feb 10, 2016

References

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