IP Library Granted Patent US 9,757,337
Granted Patent B2
US 9,757,337 · App. 14/907,249 · Granted Sep 12, 2017

Multicompartmental lipid nanoparticles

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Quick Facts
Patent No.
US 9,757,337
App. No.
14/907,249
Granted
Sep 12, 2017
Kind
B2
Abstract

The present invention relates to novel multicompartmental lipid nanoparticles (or cellisomes) with excellent stability comprising a first lipophilic compartment (lipid matrix) partly anchored to a second hydrophilic compartment delimited by a phospholipid bilayer (bilayer), as well as the method for preparing same and the use thereof as a vector for administering a wide variety of molecules of interest.

Claims (28)

1. Multi-compartment lipid nanoparticles having a mean diameter of 10 to 500 nm, wherein the multi-compartment lipid nanoparticles comprise a first lipophilic compartment comprising lipids partly enclosed by a second hydrophilic compartment delimited by a phospholipid bilayer, said first compartment being partly anchored to said second compartment, and

wherein the multi-component lipid nanoparticles are stabilized by a mixture of surfactants comprising (a) phospholipids and (b) a mixture of non-ionic surfactants comprising a three-sequence surfactant of “hydrophobic-hydrophilic-hydrophobic” type having a Griffin HLB value of greater than 11,

wherein the composition does not include a cationic surfactant.

2. The nanoparticles of claim 1 , where the polydispersity index is 5 to 15%.

3. The nanoparticles of claim 1 , where the mean diameter is 100 to 250 nm.

4. The nanoparticles of claim 1 where the lipids of the lipophilic compartment are in liquid or semi-solid state at 25° C.

5. The nanoparticles of claim 1 , where the lipophilic compartment comprises a fatty acid ester optionally mixed with a glyceride.

6. The nanoparticles of claim 5 , where said fatty acid ester comprises mixtures of polyethylene glycol mono- and diesters, the molar mass of the hydrophilic part of which varies from 100 to 700 g/mol.

7. The nanoparticles of claim 5 , where the glyceride is selected from the group consisting of mixtures of glycerol mono-, di- and triesters that are liquid or solid at 25° C.

8. The nanoparticles of claim 1 , where said phospholipid surfactant (a) comprises mixtures of zwitterionic phospholipids.

9. The nanoparticles of claim 1 , further comprising at least one molecule of interest.

10. The nanoparticles of claim 9 , where the molecule of interest is selected from the group consisting of a nucleic acid, a protein, a polysaccharide and a molecule of 40 to 2000 Da.

11. Pharmaceutical composition comprising a suspension of nanoparticles as defined in claim 1 in a pharmaceutically acceptable excipient.

12. The nanoparticles of claim 1 for use as a carrier for administering a molecule of interest.

13. The nanoparticles of claim 9 for use as medicine.

14. The nanoparticles of claim 13 , wherein said medicine is administered by injection, orally, cutaneously, or nasally.

15. The nanoparticles of claim 1 , wherein the three-sequence surfactant comprises a macrogoglyceride or a polyoxyethylene fatty acid ester.

16. Method for preparing the multicompartment lipid nanoparticles of claim 1 comprising the following steps:

preparation of an oil/water emulsion comprising water, at least one lipid, phospholipids, a mixture of nonionic surfactants comprising a three-sequence surfactant of “hydrophobic-hydrophilic-hydrophobic” type, and optionally at least one molecule of interest;

homogenization of said emulsion under high pressure.

17. Method as claimed in claim 16 , further comprising a step of heating the emulsion to a temperature of 30 to 80° C. before its homogenization.

18. Method as claimed in claim 16 , where said lipid comprises mixtures of polyethylene glycol mono- and diesters, the molar mass of the hydrophilic part of which varies from 100 to 700 g/mol.

19. Method as claimed in claim 16 , where said phospholipid comprises mixtures of zwitterionic phospholipids.

20. Method as claimed in claim 16 , where said mixture of hydrophilic nonionic surfactants comprises macrogolglycerides or polyoxyethylene fatty acid esters.

21. Method as claimed in claim 20 , where the oil/water emulsion comprises:

5-30% by mass lipids;

0.5-5% by mass phospholipids;

0.5-5% by mass of said mixture of hydrophilic nonionic surfactants comprising macrogoglycerides or polyoxyethylene fatty acid esters.

Assignments (2)
MERGER Recorded Aug 22, 2022
From: UNIVERSITE DE PARIS 11 - PARIS SUD (ALSO NAMED UNIVERSITÉ PARIS-SUD)
To: UNIVERSITE PARIS-SACLAY
Reel/Frame 060856/0245 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 15, 2016
From: FAIVRE, VINCENT; LESIEUR, SYLVIANE; OUATTARA, MODIBO; TRUONG CONG, TRI
To: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE - CNRS; UNIVERSITE PARIS-SUD
Reel/Frame 038102/0836 →