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KMID : 0848120130380040155
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International Journal of Oral Biology
2013 Volume.38 No. 4 p.155 ~ p.160
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Cholesterol conjugated spermine as a delivery modality of antisense oligonucleotide
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Yoo Hoon
Im Yoon-Kyung
Kim Myung-Su
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Abstract
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therapeutics is the inefficient delivery of these agents intocells. We prepared cholesterol conjugated spermine andevaluated its usefulness as a delivery modality for antisenseoligonucleotides in HeLa-Luc cells. A 2’-O-methylantisense oligonucleotide sequence, designed to correctsplicing at an aberrant intron inserted into a normalluciferase reporter gene, was used for complex formationwith cholesterol conjugated spermine. Effective delivery ofthis antisense agent into nucleus would results in theexpression of a luciferasereporter gene product. Thecholesterol-spermine formed stable complexes with theantisense oligonucleotide and showed modest deliveryactivity. Furthermore, this delivery activity was maintainedeven in the presence of serum proteins, mimicking in vivoconditions. Cholesterol-spermine thus has potential as adelivery system for antisense oligonucleotides into cells.
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KEYWORD
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cholesterol conjugated spermine, antisense oligonucleotide, delivery
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