Acta Phys. -Chim. Sin. ›› 2014, Vol. 30 ›› Issue (2): 345-350.doi: 10.3866/PKU.WHXB201311282

• SOFT MATTER • Previous Articles     Next Articles

Negatively Charged Lipopolyplex for Gene Delivery Based on Low-Molecular-Weight Polyethylenimine and Oleic Acid

YANG Yang1, GUO Xia2   

  1. 1 State Key Laboratory of Biotherapy, West China Hospital, Sichuan University, Chengdu 610041, P. R. China;
    2 School of Chemistry and Chemical Engineering, Yangzhou University, Yangzhou 225002, Jiangsu Province, P. R. China
  • Received:2013-09-16 Revised:2013-11-28 Published:2014-01-23
  • Contact: GUO Xia E-mail:guoxia@yzu.edu.cn
  • Supported by:

    The project was supported by the National Natural Science Foundation of China (21073155, 21373179) and NIH grants, USA (CA129835, CA149363, CA151652, CA129421).

Abstract:

The development of synthetic vectors based on low-molecular-weight polyethylenimine (PEI) and the construction of negatively charged vectors with high nucleic acid encapsulation are two of the current research trends in gene delivery. In the present study, we developed a stable and negatively charged lipopolyplex based on oleic acid and a low-molecular-weight PEI (2 kDa); it was formed by simultaneously mixing oleic acid micelles and a polyplex produced from PEI (2 kDa) and oligo dsDNA. This lipopolyplex is stable in serum, and because of the low molecular weight of the PEI, the lipopolyplex exhibits very low toxicity. The encapsulation efficiencies of nucleic acids by traditional anionic vectors are low, but very high (more than 80%) by this lipopolyplex. Suitable surface modification with 1,2-distearoryl-sn-glycero-3-phosphoethanolamine-N-methoxy(polyethyleneglycol-2000) ammonium salt enabled the lipopolyplex to bind to cells, and a high cellular uptake efficiency (ca 90%) was observed in vitro.

Key words: Polyethylenimine, Oleic acid, Gene delivery