DC-Chol/DOPE cationic liposomes: a comparative study of the influence factors on plasmid pDNA and siRNA gene delivery.
Cationic liposomes (CLs) composed of 3beta-[N-(N',N'-dimethylaminoethane) carbamoyl] cholesterol (DC-Chol) and dioleoylphosphatidylethanolamine (DOPE) (DC-Chol/DOPE liposomes) have been classified as one of the most efficient gene delivery systems. Our study aims to examine the effect of the molar ratio of DC-Chol/DOPE, PEGylation and serum on the pDNA (plasmid pDNA) and siRNA (small interfering RNA) transfection of DC-Chol/DOPE liposomes. The results showed that the most efficient DC-Chol/DOPE liposomes for pDNA or siRNA delivery were at a 1:2 or 1:1 molar ratio of DC-Chol/DOPE, respectively. The transfection efficiency of DC-Chol/DOPE liposomes increased along with increased weight ratio of DC-Chol/siRNA. However, the pDNA transfection efficiency decreased along with increased weight ratio of DC-Chol/pDNA from 3/1. As expected, PEGylation decreased siRNA and pDNA transfection efficiency of DC-Chol/DOPE liposomes. In PEGylated DC-Chol/DOPE liposomes, increased weight ratio of DC-Chol/pDNA from 3/1 did not lead to higher pDNA transfection efficiency, whereas increased weight ratio of DC-Chol/siRNA resulted in increased siRNA transfection efficiency. Furthermore, the serum did not significantly inhibit the pDNA and siRNA transfection efficiency of DC-Chol/DOPE liposomes. In conclusion, our results elucidated the influence factors of DC-Chol/DOPE liposome transfection and would reveal that siRNA and pDNA transfection mechanisms were different in DC-Chol/DOPE liposomes.
Zhang
Yang
Y
Department of Pharmaceutical Science, School of Pharmacy, The Second Military Medical University, 800 Xiang Yin Road, Shanghai 200433, People's Republic of China.
Li
Huimei
H
Sun
Jing
J
Gao
Jie
J
Liu
Wei
W
Li
Bohua
B
Guo
Yajun
Y
Chen
Jianming
J
D002412:Cations; D045744:Cell Line, Tumor; D002784:Cholesterol / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000737:chemistry; D004337:Drug Carriers / Q000008:administration & dosage / Q000138:chemical synthesis; D018014:Gene Transfer Techniques; D006801:Humans; D008081:Liposomes / Q000008:administration & dosage* / Q000138:chemical synthesis; D010316:Particle Size; D010714:Phosphatidylethanolamines / Q000008:administration & dosage / Q000737:chemistry*; D010957:Plasmids / Q000008:administration & dosage*; D034741:RNA, Small Interfering / Q000008:administration & dosage*; D018719:Erb-b2 Receptor Tyrosine Kinases / Q000187:drug effects; D055672:Static Electricity; D014162:Transfection / Q000379:methods*
D002412:Cations; D002784:Cholesterol; D004337:Drug Carriers; D008081:Liposomes; D010714:Phosphatidylethanolamines; D034741:RNA, Small Interfering; D018719:Erb-b2 Receptor Tyrosine Kinases; C410262:1,2-dioleoyl-glycero-3-phosphatidyl ethanolamine; C070648:3-(N-(N',N'-dimethylaminoethane)carbamoyl)cholesterol; C508053:ERBB2 protein, human