Nanostructured active ingredient carrier system

Patent metadata

Field	Value
Publication number	US-11376336-B2
Application number	US-201816476752-A
Country	US
Kind code	B2
Filing date	Jan 10, 2018
Priority date	Jan 10, 2017
Publication date	Jul 5, 2022
Grant date	Jul 5, 2022

Abstract

The invention relates to a nanostructured active ingredient carrier system, in particular for reducing cytotoxic properties owing to the use of sheath polymer and the transport resulting therefrom, for interactions with cell membranes during the transport of hydrophilic constituents and, in connection therewith, the generation of an early endosomal release of the interaction complex from the carrier system. The problem addressed by the present invention is that of specifying a nanostructured active ingredient carrier system which avoids the disadvantages of the prior art and in particular permits a reduction in cytotoxic properties owing to the use of a sheath polymer and the transport resulting therefrom. This problem is solved in that a nanostructured active ingredient carrier system is provided in the form of a particle consisting of a carrier sheath, wherein the carrier sheath comprises at least one or more hydrophobic sheath polymers, one or more charged complexing polymers and one or more hydrophilic active ingredients, wherein the complexing polymer interacts with the active ingredient.

First claim

The invention claimed is:

1. A nanostructured active ingredient carrier system comprising
at least one hydrophobic shell polymer, the shell polymer including poly(lactic-co-glycolic acid (PLGA);
a complexing polymer, the complexing polymer including a polymethacrylate; and
a genetic material,
wherein the complexing polymer comprises primary amino groups, secondary amino groups, or a combination of primary and secondary amino groups.

2. The nanostructured active ingredient carrier system according to claim 1 , characterized in that the complexing polymer includes poly-N,N-dimethyl-(2-aminoethyl)-methacrylate (PDMAEMA), poly-(2-aminoethyl)-methacrylate (PAEMA), poly-N-methyl-(2-amioethyl)-methacrylate (PMAEMA), or a copolymer thereof, or any combination thereof, and the genetic material includes a siRNA.

3. The nanostructured active ingredient carrier system of claim 1 , wherein the genetic material includes siRNA, mRNA, ncRNA, saRNA, short hairpin-RNA, micro-RNA, or plasmid-DNA.

4. The nanostructured active ingredient carrier system of claim 1 , wherein the nanostructured active ingredient carrier system is free of polyethyleneimine.

5. The nanostructured active ingredient carrier system of claim 1 , wherein the at least one hydrophobic shell polymer has a layered structure in the carrier system.

6. The nanostructured active ingredient carrier system of claim 1 , wherein the active ingredient carrier system is a nanoparticle having a size not greater than 1 micron.

7. The nanostructured active ingredient carrier system according to claim 1 , wherein the at least one hydrophobic shell polymer is a biodegradable polymer.

8. The nanostructured active ingredient carrier system of claim 1 , wherein the complexing polymer comprises is a copolymer.

9. The nanostructured active ingredient carrier system of claim 1 , wherein the complexing polymer comprises at least two types of amino groups, the types of amino groups being selected from primary amino groups, secondary amino groups and tertiary amino groups.

10. The nanostructured active ingredient carrier system of claim 1 , wherein the complexing polymer comprises primary amino groups and secondary amino groups.

11. The nanostructured active ingredient carrier system of claim 1 , wherein the complexing polymer comprises primary amino groups, secondary amino groups, and tertiary amino groups.

12. The nanostructured active ingredient carrier system of claim 3 , wherein the genetic material includes siRNA.

13. The nanostructured active ingredient carrier system according to claim 1 , wherein the complexing polymer includes at least one of a polypeptide, a poly(methacrylate), a polystyrene, a polyamide, a polyacrylamide, a polyurethane, a polyacrylonitrile, a polyethylene glycol, a polyethylene oxide, a polyoxazoline, or any copolymer thereof.

14. The nanostructured active ingredient carrier system according to claim 1 , wherein the shell polymer is a biocompatible polymer.

15. The nanostructured active ingredient carrier system according to claim 1 , further comprising sucrose, trehalose, or glucose.

16. A method of transporting nucleic acids into a cell, the method comprising transfecting the cell with the nucleic acids using a nanostructured active ingredient carrier system, wherein the nanostructure active ingredient carrier system comprises at least one hydrophobic shell polymer, the shell polymer including poly(lactic-co-glycolic acid (PLGA); at least one complexing polymer; and the nucleic acids, wherein the complexing polymer comprises primary amino groups, secondary amino groups, or a combination of primary and secondary amino groups.

17. The method of claim 16 , wherein the nucleic acids include siRNA.

Assignees

• Univ Jena Friedrich Schiller

Inventors

• Traeger Anja
• Truetzschler Anne-Kristin
• Bus Tanja
• Schubert Ulrich Sigmar

Classifications

• A61K47/6933 Primary

  the polymer being obtained by reactions only involving carbon to carbon, e.g. poly(meth)acrylate, polystyrene, polyvinylpyrrolidone or polyvinylalcohol · CPC title

• A61K9/5153 Primary

  Polyesters, e.g. poly(lactide-co-glycolide) · CPC title

• A61K47/58

  obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. poly[meth]acrylate, polyacrylamide, polystyrene, polyvinylpyrrolidone, polyvinylalcohol or polystyrene sulfonic acid resin · CPC title

• A61K9/5146

  obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyamines, polyanhydrides · CPC title