Amino Acid-Modified Polyethylenimines with Enhanced Gene Delivery Efficiency and Biocompatibility

Polymers

Qin-Fang Zhang³  Chao-Ran Luan³  Dong-Xiao Yin³  Ji Zhang³  Yan-Hong Liu³  Qi Peng¹  Yong Xu²  Xiao-Qi Yu³ 

[1] West China School of Medicine, Sichuan University, Chengdu 610041, China;Humanwell Healthcare (Group) Co., LTD., 666 Gaoxin Road, East Lake High-Tech Development Zone, Wuhan 430075, China;Key Laboratory of Green Chemistry and Technology (Ministry of Education), College of Chemistry, Sichuan University, Chengdu 610064, China;

关键词: gene delivery;    polyethylenimine;    non-viral gene vector;    biocompatibility;   

DOI  :  10.3390/polym7111516

来源: mdpi

【 摘 要 】

The development of gene delivery vectors with high efficiency and biocompatibility is one of the key points of gene therapy. A series of polycations were prepared from polyethylenimine (PEI) with several amino acids or their analogs. The target polymers have different charge and hydrophilic/hydrophobic properties, which may affect their performance in the gene transfection process. Gel retardation and DLS assays showed that these polymers may condense DNA into nanoparticles with positive zeta potentials and proper sizes for cellular uptake. Luciferase reporter gene transfection results revealed their higher transfection efficiency than PEI; especially in the presence of serum, in which up to 23 times higher efficiency was achieved by employing glycolic acid-grafted PEI. Moreover, it was found that the degree of substitution on PEI has an apparent influence on the transfection, and the balance between electron-positive/negative groups largely affects the delivery process. The higher serum tolerance was also proven by BSA adsorption, flow cytometry and confocal microscopy assays. Results demonstrate that such type of polycations may serve as promising non-viral gene delivery vectors.

【 授权许可】

CC BY   
© 2015 by the authors; licensee MDPI, Basel, Switzerland.