Liposomal antisense methyl phosphonate oligonucleotides and meth

Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Liposomes

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514 44, 536 241, A61K 3722

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054179785

ABSTRACT:
A liposomal methyl phosphonate oligonucleotide composition useful in treatment of chronic myeloid leukemia comprises (a) a liposome which comprises at least one phospholipid, and (b) an antisense methyl phosphonate oligonucleotide which is entrapped in the liposome. The molar ratio of phospholipid in the liposome to the methyl phosphonate entrapped in the liposome is between about 100:1 and about 10,000:1. A process for making the composition includes the steps of (a) mixing an antisense methyl phosphonate oligonucleotide in a first organic solvent with at least one phospholipid in a second organic solvent, where the molar ratio of phospholipid to methyl phosphonate is between about 100:1 and about 10,000:1, (b) lyophilizing the mixture formed in step (a), producing a lyophilized powder, (c) hydrating the lyophilized powder, and (d) sonicating the hydrated material.

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