IP Library › Granted Patent US 11,684,578
Granted Patent B2
US 11,684,578 · App. 16/485,855 · Granted Jun 27, 2023

Liposomic drug-delivery vehicles

Inventors: Jacob Klein (Rehovot, IL); Ronit Goldberg (Rehovot, IL); Weifeng Lin (Rehovot, IL)
Assignee: Yeda Research and Development Co. Ltd.
A61K9/1273A61K9/0019A61P19/02
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Quick Facts
Patent No.
US 11,684,578
App. No.
16/485,855
Granted
Jun 27, 2023
Kind
B2
Abstract

A liposome for use in delivering a therapeutically active agent to a subject in need thereof is disclosed herein. The liposome comprises: a) at least one bilayer-forming lipid; b) a polymeric compound having the general formula I: wherein m, n, L, X, Y, and Z are as defined herein; and c) a therapeutically active agent, incorporated in the liposome and/or on a surface of the liposome.

Claims (42)

1. A method of delivering a therapeutically active agent to a subject in need thereof, the method comprising administering to the subject a liposome comprising:

a) at least one bilayer-forming lipid;

b) a polymeric compound having the general formula I:

wherein:

m is zero or a positive integer;

n is an integer which is at least 3;

Y is a backbone unit which forms a polymeric backbone;

L is absent or is a linking moiety;

Z has the general formula II:

wherein:

A is a substituted or unsubstituted hydrocarbon;

B is an oxygen atom or is absent; and

R 1 -R 3 are each independently selected from the group consisting of hydrogen, alkyl, cycloalkyl, heteroalicyclic, aryl and heteroaryl; and

X is a lipid moiety having the general formula III:

wherein:

W 1 and W 2 are each independently selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl and acyl, wherein at least one of W 1 and W 2 is not hydrogen;

J is —P(═O)(OH)—O— or absent;

K is a substituted or unsubstituted hydrocarbon from 1 to 10 carbon atoms in length, or absent;

M is a linking group selected from the group consisting of —O—, —S—, amino, sulfinyl, sulfonyl, phosphate, phosphonyl, phosphinyl, carbonyl, thiocarbonyl, urea, thiourea, carbamyl, thiocarbamyl, amido, carboxy, and sulfonamide, or absent; and

Q is a substituted or unsubstituted hydrocarbon from 1 to 10 carbon atoms in length,

wherein when M is absent, K is also absent; and

c) a therapeutically active agent, incorporated in the liposome or on a surface of the liposome,

thereby delivering said therapeutically active agent to said subject in need thereof

wherein said administering comprises sustained release of said therapeutically active agent.

2. The method of claim 1 , being for use in treating a medical condition treatable by said therapeutically active agent in said subject.

3. The method of claim 1 , wherein said therapeutically effective agent is selected from the group consisting of an analgesic, an anti-inflammatory agent, an anti-proliferative agent, an anti-microbial agent, and a vaccine antigen.

4. The method of claim 1 , wherein said administering is effected by parenteral systemic administration.

5. The method of claim 1 , wherein said administering is effected by intra-articular administration.

6. The method of claim 1 , being for treating a synovial joint disorder.

7. The method of claim 6 , wherein said synovial joint disorder is selected from the group consisting of arthritis, bursitis, carpal tunnel syndrome, fibromyositis, gout, locked joint, tendinitis, traumatic joint injury, and joint injury inflicted by surgery.

8. The method of claim 1 , wherein said therapeutically active agent is an analgesic or anti-inflammatory agent.

9. The method of claim 1 , wherein a molar ratio of said bilayer-forming lipid and said polymeric compound is in a range of from 5:1 to 5,000:1.

10. The method of claim 1 , wherein Y is a substituted or unsubstituted alkylene unit.

11. The method of claim 1 , wherein B is an oxygen atom.

12. The method of claim 1 , wherein A is a substituted or unsubstituted hydrocarbon from 1 to 4 carbon atoms in length.

13. The method of claim 1 , wherein R 1 -R 3 are each independently hydrogen or C 1-4 -alkyl.

14. The method of claim 1 , wherein n is at least 5.

15. The method of claim 1 , wherein at least a portion of said Y, said L or said Z comprises at least one targeting moiety.

16. The method of claim 1 , wherein said lipid is selected from the group consisting of a fatty acid, a monoglyceride, a diglyceride, a triglyceride, a glycerophospholipid, a sphingolipid, and a sterol.

17. The method of claim 1 , wherein said lipid moiety comprises at least one fatty acid moiety selected from the group consisting of lauroyl, myristoyl, palmitoyl, stearoyl, palmitoleoyl, oleoyl, and linoleoyl.

18. The method of claim 1 , wherein said liposome is formulated as part of a pharmaceutical composition, which further comprises a pharmaceutically acceptable carrier.

19. The method of claim 1 , wherein n is in a range of from 5 to 50, and m is in a range of from 0 to 50.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 23, 2019
From: KLEIN, JACOB; GOLDBERG, RONIT; LIN, WEIFENG
To: YEDA RESEARCH AND DEVELOPMENT CO. LTD.
Reel/Frame 050141/0703 →
Continuity (2)
Provisional Application 62459624 · Feb 16, 2017
Related Publication 20190374466A1 · Dec 12, 2019