Polyamidoamine Dendrimer Grafted with an Acid-Responsive Charge-Reversal Layer for Improved Gene Delivery.

ABSTRACT: We report on a heterogeneous dendrimer (G3-acetal-NH₂) derivative possessing an acid-responsive charge-reversal layer. The synthesis of G3-acetal-NH₂ starts with a polyamidoamine (PAMAM) dendrimer G3 core and follows the aza-Michael addition with N-(2-(1-(allyloxy)ethoxy)ethyl)acrylamide synthesized by us and the thiol-ene click chemistry with cysteamine hydrochloride in sequence. In a weakly acidic environment, the surface of this newly formed dendrimer can turn from amine-terminated to hydroxyl-terminated due to the cleavage of the acetal groups. This charge conversion from 34.3 ± 2.7 to 18.0 ± 0.3 mV in 24 h at pH 5.3 enables its capacity as a gene delivery vehicle. G3-acetal-NH₂ with a positively charged surface can condense

SUBMITTER: Wang J 

PROVIDER: S-EPMC7583228 | biostudies-literature | 2020 Oct

REPOSITORIES: biostudies-literature