IP Library Granted Patent US 11,918,686
Granted Patent B2
US 11,918,686 · App. 16/948,498 · Granted Mar 5, 2024

Lipid bilayer coated mesoporous silica nanoparticles with a high loading capacity for one or more anticancer agents

Inventors: Andre E. Nel (Sherman Oaks, CA); Jeffrey I. Zink (Sherman Oaks, CA); Huan Meng (Los Angeles, CA)
Assignee: The Regents of the University of California
A61K9/127A61K9/5115A61K31/337A61K31/4709A61K31/7068A61K31/7105A61K31/713A61K45/06A61K47/02
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Quick Facts
Patent No.
US 11,918,686
App. No.
16/948,498
Granted
Mar 5, 2024
Kind
B2
Abstract

A submicron structure comprising a silica body defining a plurality of pores that are suitable to receive molecules therein, and having a surface, and a phospholipid bilayer coating the surface, wherein said submicron structure has a maximum dimension of less than one micron, and wherein the phospholipid bilayer stably seals the plurality of pores; and wherein the submicron structure is a member of a monodisperse population of submicron structures.

Claims (28)

1. A drug delivery carrier comprising:

a silica body having a plurality of pores suitable to receive a therapeutic agent therein, and having a surface;

an intact lipid bilayer coating the surface and encapsulating the silica body and stably sealing the plurality of pores, wherein the encapsulating is performed without lipid phase exchange and without contacting a preformed liposome with the silica body;

a first therapeutic agent within the pores of the silica body, wherein the first therapeutic agent comprises gemcitabine; and

a second therapeutic agent disposed in the lipid bilayer, wherein the second therapeutic agent comprises paclitaxel.

2. The drug delivery carrier of claim 1 , wherein the drug delivery carrier provides a predetermined dose and ratio of first therapeutic agent to second therapeutic agent.

3. The drug delivery carrier of claim 1 , wherein the first therapeutic agent and the second therapeutic agent act synergistically.

4. The drug delivery carrier of claim 1 , wherein the drug delivery carrier includes about 20% w/w or greater of gemcitabine molecules within the pores of the silica body.

5. The drug delivery carrier of claim 1 , wherein the drug delivery carrier includes about 30% w/w or greater of gemcitabine molecules within the pores of the silica body.

6. The drug delivery carrier of claim 1 , wherein the drug delivery carrier includes about 40% w/w or greater of gemcitabine molecules within the pores of the silica body.

7. The drug delivery carrier of claim 1 , wherein the lipid bilayer is formed from a lipid film containing the second therapeutic agent.

8. The drug delivery carrier of claim 1 , wherein the drug delivery carrier is configured to retain the first therapeutic agent within the silica body without substantial loss for at least 1 week prior to administration to a subject.

9. The drug delivery carrier of claim 1 , wherein the drug delivery carrier is configured to retain the first therapeutic agent within the silica body with 10% or less loss for at least 1 week prior to administration to a subject.

10. The drug delivery carrier of claim 1 , wherein the drug delivery carrier is a member of a monodisperse population of drug delivery carriers.

11. The drug delivery carrier of claim 1 , wherein the drug delivery carrier is a submicron structure with a maximum dimension of between 20 nm and 300 nm.

12. The drug delivery carrier of claim 1 , wherein the drug delivery carrier has a submicron structure with a maximum dimension of between 50 nm and 200 nm.

13. The drug delivery carrier of claim 1 , wherein the lipid bilayer comprises a phospholipid bilayer.

14. The drug delivery carrier of claim 13 , wherein the phospholipid bilayer comprises 2-dioleoyl-3-trimethylammonium-propane (DOTAP), 1,2-dioleoyl-sn-glycero-3-phospho-L-serine (DOPS),1,2-dioleoyl-sn-glycero-3-phosphocholine (DOPC), or any combination thereof.

15. A composition comprising a plurality of drug delivery carriers, each drug delivery carrier comprising:

a silica body having a plurality of pores suitable to receive a therapeutic agent therein, and having a surface;

an intact lipid bilayer coating the surface and encapsulating the silica body and stably sealing the plurality of pores, wherein the encapsulating is performed without lipid phase exchange and without contacting a preformed liposome with the silica body;

a first therapeutic agent within the pores of the silica body, wherein the first therapeutic agent comprises gemcitabine; and

a second therapeutic agent disposed in the lipid bilayer, wherein the second therapeutic agent comprises paclitaxel.

16. The composition of claim 15 , wherein the composition comprises a stable colloidal suspension.

17. The composition of claim 15 , wherein the plurality of drug delivery carriers provides a predetermined dose and ratio of the first therapeutic agent to the second therapeutic agent.

18. The composition of claim 15 , wherein the plurality of drug delivery carriers form a monodisperse population having a deviation in average diameter of 10% or less.

19. The composition of claim 15 , wherein the composition is formulated for systemic administration to a subject for treating cancer.

20. The composition of claim 15 , wherein the composition is formulated for intravenous, intra-arterial, intraperitoneal, intramuscular, or subcutaneous administration.

Continuity (4)
Continuation 14772740
Provisional Application 61858388 · Jul 25, 2013
Provisional Application 61773013 · Mar 5, 2013
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