Efficient delivery of antisense oligodeoxyribonucleotide g3139 by human serum albumin-coated liposomes.
Human serum albumin (HSA)-coated liposomal formulations were synthesized and evaluated for the delivery of antisense oligodeoxyribonucleotide (ODN) G3139 in KB human oral carcinoma cells. Liposomes composed of dimethyldioctadecyl ammonium bromide/egg phosphatidylcholine/alpha-tocopheryl polyethylene glycol 1000 succinate (58:40:2 molar ratio) complexed with G3139 and coated with HSA were investigated for Bcl-2 downregulating activity. Cellular uptake of HSA-coated liposome-ODN complexes was more efficient than the uncoated liposome-ODN complexes. Treatment of the cells with HSA-coated liposome-ODN complexes resulted in efficient Bcl-2 mRNA downregulation that was approximately 3-fold greater than with uncoated liposomes (p < 0.05) and 6-fold greater than with free ODN. The transfection efficiency of liposome-ODN complexes coated with HSA was dependent on the concentration of HSA used and on the contents of alpha-helix and beta-strand in HSA. HSA-coated liposomes are effective delivery vehicles for antisense ODN.
Weecharangsan
Wanlop
W
Division of Pharmaceutics, College of Pharmacy, The Ohio State University, Columbus, Ohio 43210, USA. wanlop@swu.ac.th
Yu
Bo
B
Zheng
Yu
Y
Liu
Shujun
S
Pang
Jiu Xia
JX
Lee
L James
LJ
Marcucci
Guido
G
Lee
Robert J
RJ
D015153:Blotting, Western; D045744:Cell Line, Tumor; D002942:Circular Dichroism; D004587:Electrophoresis, Agar Gel; D006801:Humans; D008081:Liposomes / Q000008:administration & dosage / Q000737:chemistry*; D019253:Proto-Oncogene Proteins c-bcl-2 / Q000037:antagonists & inhibitors / Q000235:genetics / Q000378:metabolism; D020133:Reverse Transcriptase Polymerase Chain Reaction; D012709:Serum Albumin / Q000737:chemistry*; D013873:Thionucleotides / Q000008:administration & dosage*
D008081:Liposomes; D019253:Proto-Oncogene Proteins c-bcl-2; D012709:Serum Albumin; D013873:Thionucleotides; C408162:oblimersen