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KMID : 0606320020180010069
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Journal of Phamacetical Sciences Sookmyung Women s University
2002 Volume.18 No. 1 p.69 ~ p.78
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Development of Liposomal Formulations of bel-2 Antisense 0ligodeoxynucleotide
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Shim Jin-Young
Jeon Eun-Jung
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Abstract
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Llposomal formulations of bcl-2 antisense oligodeoxynucleotide (ODN) were developed and tested for its apoptotic effect on SK-OV-3 cells in vifyo. The SGTAI 19-20090(S), a synthetic conjugate of 20-mer bcl-2 oligodeoxy-nucleotide (2009) with a Genechem’s proprietary mitomycin derivative by covalent bond, was used throughout the experiment. Negatively charged SGTAI 19- 2009(S) was Incorporated by the Lev method into various liposomal formulations; either neutral one using DPPC: Chol. 1,2-dioleoyl-sn-glycero-3-phosphoethanolamine (DOPE) (6:3:1) or cationic one using stearylamine (SA) : DPPC Chol : DOPE (6:3:1). Formed liposomes were characterized in terms of morphology, size and encapsulation efficiency, Average size of liposomes is 400∼500nm in diameter. Structure of liposomes observed by scanning electron microscope (SEM) was globular shape and had multi lamellars. SGTAI 19-2009(S) had 12% encapsulation efclency on neutral liposome and 34% encapsulation efficiency on cationic liposome. IC50 of SGTAI 19-2009(S) in DPPC liposomes was about 1000nM in SK-OV-3 cells, whereas flee antisense ODN did not show cytotoxic effect at this range. Westers blotting was also carried out to confirm the Bcl-2 protein down- regulation, though it was not semi-quantitatively matched with the growth inhibition results. More vigorous studies are under going to evaluate this and other basic matters.
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