Review Article

Design and Development of Degradable Polyethylenimines for Delivery of DNA and Small Interfering RNA: An Updated Review

Table 1

Representative examples of degradable PEIs having ester linkage (modified from [103]).

TypeMw of starting PEI (Da)CrosslinkersCells CharactersReference

8001,3-Butanediol diacrylateMDA-MB-2314 h half-life, 9-fold higher gene expression[21]
Linear423PEG diacrylateHepG2
MG63
Importance of MW of PEG, 4 h of half-life, aerosol route is more effective than I.V. one[24]
423Sorbitol dimethacrylateA549, HeLa, H322Accelerated gene transfer by hyperosmotic activity
No aggregation of polyplexes after lyophilization
[37]

8001,3-Butanediol diacrylate, 1,6-hexane diacrylateMDA-MB-231Reaction with primary and secondary amines of PEI[21]
8001,6-Hexane diacrylateNeuro2a, BI6F10Reaction temperature controls half-life[22, 23]
600, 1200, 1800Poloxamer diacrylateA549, 293T, HepG2Little serum dependency of transfection[34]
Branched600, 1200, 1800Polycaprolactone diacrylate293T, HepG2, HeLa25-fold higher gene expression, 5 h of half-life[35]
1200Glycerol dimethacrylateHeLa, HepG2, 293TSynergistic effect of hyper osmotic glycerol and buffering capacity of PEI[36]
600, 1200, 1800PEG dimethacrylate293T, HeLa, HepG2Longer half-life than PEG diacrylate[54]
1200Sorbitol diacrylateA549, HeLa, 293TSelective caveolae endocytosis pathway by osmotic polysorbitol[55]
1200Mannitol diacrylateA549, HeLa, N2aAvoidance of delivered gene from lysosomal fusion by shifting to caveolae endocytosis pathway[56]

Grafted800PEG dithiothreitolHeLa, MCF-7, COS-71,1′-Carbonyldiimidazole was used as a linker. A slight serum dependency in transfection activity[50]