Nanostructured active ingredient carrier system

Patent metadata

Field	Value
Publication number	US-2020061206-A1
Application number	US-201816476752-A
Country	US
Kind code	A1
Filing date	Jan 10, 2018
Priority date	Jan 10, 2017
Publication date	Feb 27, 2020
Grant date	—

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

1 . A nanostructured active ingredient carrier system in the form of a particle containing a carrier shell, characterized in that the carrier shell comprises at least one or more hydrophobic shell polymers, one or more charged complexing polymers, and one or more hydrophilic active ingredients, wherein the complexing polymer interacts with the active ingredient.

2 . The nanostructured active ingredient carrier system according to claim 1 , characterized in that the interaction between the complexing polymer and the active ingredient is caused by one or more non-covalent interactions in the form of electrostatic bonds, ionic bonds, hydrogen bonds, or van der Waals forces.

3 . The nanostructured active ingredient carrier system according to claim 1 , characterized in that the active ingredients belong to the following substance classes:
nucleic acids in the form of siRNA, mRNA, ncRNA, saRNA, short hairpin-RNA, micro-RNA, or plasmid-DNA, peptides and proteins in the form of antibodies, interferons, and cytokines and or pharmaceutical active ingredients.

4 . The nanostructured active ingredient carrier system according to claim 1 , characterized in that the complexing polymer consists of linear, water-soluble, cationic polymers having 0-70% secondary amine functionalities in the polymer backbone.

5 . The nanostructured active ingredient carrier system according to claim 1 , characterized in that the complexing polymer is selected from the group of polypeptides, poly(meth)acrylates, polystyrene derivatives, polyamides, polyurethanes, polyacrylonitriles, polyethylene glycols, polyethylene oxides, and polyoxazolines and copolymers thereof in a variety of compositions, excluding polyethylenimine.

6 . The nanostructured active ingredient carrier system according to claim 1 , characterized in that the carrier shell comprises the interaction complex of active ingredient and complexing polymer and thereby forms a nanostructuring of the carrier system.

7 . The nanostructured active ingredient carrier system according to claim 1 , characterized in that the hydrophobic shell polymer is designed as a blend and/or in layers of hydrophobic polymers which enclose an active ingredient complex.

8 . The nanostructured active ingredient carrier system according to claim 6 , characterized in that the shell polymer is selected from the group of polyesters, poly(meth)acrylates, polystyrene derivatives, polyamides, polyurethanes, polyacrylonitriles, polytetrafluoroethylenes, silicones, polyethylene glycols, polyethylene oxides, and polyoxazolines and copolymers thereof in various compositions.

9 . The nanostructured active ingredient carrier system according to claim 1 , characterized in that the shell polymer is a biocompatible polymer.

10 . The nanostructured active ingredient carrier system according to claim 1 , characterized in that the shell polymer includes auxiliaries and additives in form of polyvinyl alcohol, Pluronic for the preparation of a nanoemulsion or in form of sucrose, trehalose, or glucose for freeze-drying.

11 . A use of the nanostructured active ingredient carrier system according to claim 1 for the transport of siRNA.

12 . A nanostructured active ingredient carrier system comprising a shell polymer PLGA, a complexing polymer based on polymethacrylates, and genetic material.

13 . The nanostructured active ingredient carrier system according to claim 12 , characterized in that the complexing polymer is PDMAEMA, PAEMA, PMAEMA, or a copolymer thereof, and the genetic material is an 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

• 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

• A61K9/5153 Primary

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