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US 2016/0081930 A1Published application
Small Interfering RNA Delivery
AssigneeLipoxen Technologies Limited
InventorsAndrew David Bacon, Peter Laing, Gregory Gregoriadis
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Abstract
A liposomal siRNA composition is described. The liposomes are formed of neutral liposome forming components, and the composition comprising additionally sugar. The composition provides reduced expression of target gene, without causing systemic toxicity. The composition is produced by a dehydration-rehydration technique to provide high yields and good control of liposome size.
Claims16
A method of preparing a liposomal siRNA composition comprising:
- a) mixing into an aqueous suspension of empty liposomes having an average diameter in the range of 20 nm to 200 nm and formed of neutral liposome-forming components
- i) double-stranded siRNA and
- ii) sugar to form a mixed suspension that entraps the siRNA and the sugar in the intravesicular space of the empty liposomes, in which the mass ratio of the siRNA to the neutral liposome-forming components is in the range 0.001:1 w/w to 0.1:1 w/w and the mass ratio of the sugar to the neutral liposome-forming components is in the range 0.7 w/w to 7:1 w/w, and wherein the amount of the sugar in the mixed suspension is less than 10% w/v of the composition;
- and
- b) dehydrating the mixed suspension formed in step i) to form a dehydrated composition,
- wherein liposomes formed by rehydrating the dehydrated composition formed in step ii) have an average diameter in the range 100 nm to 500 nm and wherein the siRNA and sugar are each entrapped in the intravesicular space of the liposomes.
3 more elements
Dependencies are inferred from the claim text.