Comparative study on preparative methods of DC-Chol/DOPE liposomes and formulation optimization by determining encapsulation efficiency.
Three most commonly used preparative methods, dry-film, reverse phase evaporation and ethanol injection were employed to prepare cationic liposomes composed of DC-Chol and DOPE, respectively. The resulting samples were contrasted through morphology observation, particle size and zeta potential analysis. Sephadex filtration method with high selectivity was developed to determine the encapsulation efficiency of plasmid DNA-loaded cationic vectors, on this basis, cationic liposomes formulation was further optimized by applying Box Behnken design with encapsulation efficiency as evaluation index. The results showed that liposomes prepared by dry-film method were of best quality and stability, moreover, the optimum formulation of cationic liposomes and optimal value of each influencing factors were quantitatively obtained, measured value was highly consistent with predicted results. These findings preliminarily clarified the effect of preparative methods on performance of cationic liposome, as well as formulation factors on encapsulation efficiency, and will provide important methodological reference for further study of liposomes carriers for gene delivery.
Center of Drug Metabolism and Pharmacokinetics, College of Pharmacy, China Pharmaceutical University, Nanjing, PR China.
Shuoye
S
Yang
Jiayin
J
Chen
Di
D
Zhao
Deen
D
Han
Xijing
X
Chen
D002412:Cations; D002626:Chemistry, Pharmaceutical / Q000379:methods; D002784:Cholesterol / Q000031:analogs & derivatives* / Q000737:chemistry; D004247:DNA / Q000008:administration & dosage*; D003911:Dextrans; D000431:Ethanol / Q000737:chemistry; D005374:Filtration; D018014:Gene Transfer Techniques; D008081:Liposomes; D010316:Particle Size; D010714:Phosphatidylethanolamines / Q000737:chemistry*; D010957:Plasmids
C410262:1,2-dioleoyl-glycero-3-phosphatidyl ethanolamine; D002412:Cations; D003911:Dextrans; D008081:Liposomes; D010714:Phosphatidylethanolamines; C070648:3-(N-(N',N'-dimethylaminoethane)carbamoyl)cholesterol; D000431:Ethanol; D004247:DNA; C025614:sephadex; D002784:Cholesterol