Composition
AssigneesBioNTech Delivery Technologies GmbH, BioNTech SE
InventorsSteffen Panzner, Mario Saucedo-Espinosa, Roy Pattipeiluhu, Martin Kirchberg, Kaushik Thanki
Life of this patent
Estimating the term…
Abstract
A composition comprising: (a) an active ingredient; and (b) a lipid mixture comprising: (i) a cationically ionisable lipid capable of forming a lipid nanoparticle; (ii) a steroid; and (iii) a negatively charged amphiphile having a hydrophilic portion and a lipophilic portion; wherein the composition is a lipid nanoparticle composition and is substantially free of a polyethylene glycol-conjugated lipid, wherein the polyethylene glycol (PEG) moiety of the PEG-conjugated lipid has at least 5 consecutive ethylene glycol repeating units, is provided.
Claims43
A composition comprising:
- (a) an active ingredient;
- and
- (b) a lipid mixture comprising:
- (i) a cationically ionisable lipid capable of forming a lipid nanoparticle;
- (ii) a steroid;
- and
- (iii) a negatively charged amphiphile having a hydrophilic portion and a lipophilic portion;
- wherein the composition is a lipid nanoparticle composition and is substantially free of a polyethylene glycol-conjugated lipid, wherein the polyethylene glycol (PEG) moiety of the PEG-conjugated lipid has at least 5 consecutive ethylene glycol repeating units.
The composition of any preceding claim, wherein the negatively charged amphiphile is present in the composition in an amount of up to 20 mol % of the total lipid present in the composition.
The composition of any preceding claim, wherein the cationically ionisable lipid is selected from the group consisting of:
- [(4-hydroxybutyl) azanediyl]di(hexane-6,1-diyl)bis(2-hexyldecanoate)) (ALC-315);
- 2,2-dilinoleyl-4-dimethylaminoethyl-[1,3]-dioxolane (DLin-KC2-DMA);
- heptatriaconta-6,9,28,31-tetraen-19-yl-4-(dimethylamino)butanoate (D-Lin-MC3-DMA);
- 1,2-dilinoleyloxy-N,N-dimethylaminopropane (DLin-DMA);
- N,N-dimethyl-2,3-dioleyloxypropylamine (DODMA);
- di((Z)-non-2-en-1-yl)-9-((4-(dimethylaminobutanoyl)oxy) heptadecanedioate (L319);
- bis-(2-butyloctyl) 10-(N-(3-(dimethylamino) propyl) nonanamido)-nonadecanedioate (A9);
- (heptadecan-9-yl 8-{(2-hydroxyethyl) [6-oxo-6-(undecyloxy) octyl]amino}-octanoate) (L5);
- heptadecan-9-yl 8-{(2-hydroxyethyl) [6-oxo-6-(undecyloxy) hexyl]amino}-octanoate) (SM-102);
- O—[N-{(9Z,12Z)-octadeca-9,12-dien-1-yl)}-N-{7-pentadecylcarbonyloxyoctyl}-amino]4-(dimethylamino)butanoate (HY501);
- di(heptadecan-9-yl) 3,3′-((2-(4-methylpiperazin-1-yl)ethyl) azanediyl)dipropionate (BHD-C2C2-PipZ);
- bis(2-octyldodecyl) 3,3′-((2-(1-methylpyrrolidin-2-yl)ethyl) azanediyl)dipropionate (BODD-C2C2-1Me-Pyr);
- bis(2-octyldodecyl) 3,3′-((2-(pyrrolidin-1-yl)ethyl) azanediyl)dipropionate (BODD-C2C2-Pyr);
- bis(2-octyldodecyl) 3,3′-((2-(1-methylpyrrolidin-2-yl)ethyl) azanediyl)dipropionate (BODD-C2C2-1MePyr);
- bis(2-octyldodecyl) 3,3′-(((1-methylpiperidin-3-yl)methyl) azanediyl)dipropionate (BODD-C2C2-1Me-3PipD);
- bis(2-octyldodecyl) 3,3′-((2-(dimethylamino)ethyl) azanediyl)dipropionate (BODD-C2C2-DMA);
- bis(2-octyldodecyl) 3,3′-((4-(4-methylpiperazin-1-yl)butyl) azanediyl)dipropionate (BODD-C2C4-PipZ);
- bis(2-octyldodecyl) 3,3′-((4-(pyrrolidin-1-yl)butyl) azanediyl)dipropionate (BODD-C2C4-Pyr);
- bis(2-hexyldecyl) 3,3′-((4-(4-methylpiperazin-1-yl)butyl) azanediyl)dipropionate (BHD-C2C4-PipZ);
- di(nonadecan-9-yl) 3,3′-((4-(4-methylpiperazin-1-yl)butyl) azanediyl)dipropionate (DND-C2-C4-PipZ);
- or a mixture of any thereof.
The composition of any preceding claim, wherein the cationically ionisable lipid is present in the composition in an amount of 20 to 80 mol % of the total lipid present in the composition.
The composition of any preceding claim, wherein the lipid mixture comprises one or more additional lipids.
The composition of any preceding claim, wherein the one or more additional lipids comprise a steroid.
The composition of any preceding claim, wherein the active ingredient is a nucleic acid.
The composition of any preceding claim, which is substantially free of a stealth lipid.
A pharmaceutical composition comprising the composition of any preceding claim, together with a pharmaceutically acceptable carrier.
Dependencies are inferred from the claim text.