Endosomolytic agents, activation

Fig. 2 Masked endosomolytic agents for pH-triggered endosomal escape. The polymers designed by Meyer et al. [69] (a) and Rozema et al. [71] (b) contain endosomolytic compounds whose lytic potential is activated by endosomal cleavage of masking groups coupled by acid-sensitive linkages. Furthermore, disulfide bonds are embedded which release the nucleic acid after endosomal escape by cleavage in the reducing cytosolic environment...

As PAA exist in the form of a salt, it is important to determine, prior to use as endosomolytic agents, which, if any salt, exhibits the most appropriate pH-membrane perturbation properties. A SANS study was therefore initiated to investigate systematically the effects of pH and counterion on the molecular structure (as assessed by Rg) of the PAA, ISA 23 when dispersed in D2O, and to correlate molecular structure with its hemolytic activity. Fig. 10 shows the normalized... 

---