Self-assembled micellar aggregates based monomethoxyl poly(ethylene glycol)-b-poly(ε-caprolactone)-b-poly(aminoethyl methacrylate) ,triblock copolymers as efficient gene delivery vectors

摘要

Amphiphilic triblock copolymers monometh oxyl poly(ethylene glycol) (mPEG)-b-poly(ε-caprolactone) (PCL)-b-poly(aminoethyl methacrylate)s (PAMAs) (mPE- CAs) were synthesized as gene delivery vectors. They exhibited lower cytotoxicity and higher transfection effi ciency in COS-7 cells in presence of serum compared to 25 kDa bPEI. The influence of rnPEG and PCL segments in mPECAs was evaluated by comparing with corre sponding diblock copolymers. The studies showed the incorporation of the hydrophobic PCL segment in triblock copolymers affected the binding capability to pDNA and surface charges of complexes due to the formation of micelles increasing the local charges. The presence of mPEG segment in gene vector decreased the surface charges of the complexes and increased the stability of the complexes in serum because of the steric hindrance effect. It was also found that the combination of PEG and PCL segments into one macromolecule might lead to synergistic effect for better transfection efficiency in serum.