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US 12,521,447 B2Granted
Cationic lipid compositions for tissue-specific delivery
AssigneeLife Technologies Corporation
InventorsShikha Mishra, Xavier de Mollerat du Jeu
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Abstract
Provided herein are, inter alia, compositions and methods useful for the in vivo delivery of bioactive agents (e.g., therapeutic or diagnostic agents). The compositions provided herein include cationic lipids, helper lipids and a biostability enhancing agent, which together form a lipid aggregate with the bioactive agent and allow for the systemic delivery of the bioactive agent to, for example, lung tissue without the requirement for biomolecular targeting.
Claims11
A method of delivering a bioactive agent to a lung tissue in a subject, said method comprising:
- intravenously administering a bioactive agent-lipid complex to the subject, thereby delivering said bioactive agent-lipid complex to the lung tissue,
- wherein the bioactive agent-lipid complex comprises a bioactive agent and a composition comprising
- (i) a first cationic lipid at a compositional molar ratio from about 0.18 to about 0.32 and of formula:
- wherein
- R1 and R2 are independently substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
- R3 and R4 are independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
- m is an integer from 1 to 6;
- Xa− is an anion;
- (ii) a second cationic lipid at a compositional molar ratio from about 0.24 to about 0.51 and of formula:
- wherein
- R5 and R8 are independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
- R6 and R7 are independently substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;
- n is an integer from 1 to 6;
- and
- Xb− is an anion;
- (iii) a first helper lipid at a compositional molar ratio from about 0.20 to about 0.32;
- (iv) a second helper lipid at a compositional molar ratio from about 0.01 to about 0.14;
- and
- (v) a biostability enhancing agent at a compositional molar ratio from about 0.01 to about 0.02.
16 more elements
Dependencies are inferred from the claim text.