# US 11,298,319 B2 · Cell penetrating peptide (CPP)-mediated EV loading

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- Number: US 11,298,319 B2
- Document ID: US11298319B2
- Status: Granted
- Kind: B2
- Application number: 16/317,455
- Filed: 2017-07-10
- Published: 2019-12-26
- Granted: 2022-04-12
- Earliest claimed: 2016-07-11
- Assignees: Evox Therapeutics Ltd
- Applicants: Evox Therapeutics Ltd
- Inventors: Oscar Wiklander; Per Lundin; Dhanu Gupta
- Web page: https://patentgrep.com/patent/US11298319B2

## CPC

- A61K 9/1271: Non-conventional liposomes, e.g. PEGylated liposomes or liposomes coated or grafted with polymers (liposomes as conjugates {A61K47/6911})
- A61K 47/64: Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent (peptidic linkers A61K47/65)
- A61K 9/00: Medicinal preparations characterised by special physical form {(nuclear magnetic resonance contrast preparations or magnetic resonance imaging contrast preparations A61K49/18; preparations containing radioactive substances A61K51/12)}
- A61K 9/5068: {Cell membranes or bacterial membranes enclosing drugs (liposomes with additional exogenous lipids A61K9/127)}
- A61K 47/54: the modifying agent being an organic compound
- A61K 47/61: the organic macromolecular compound being a polysaccharide or a derivative thereof
- A61K 47/645: {Polycationic or polyanionic oligopeptides, polypeptides or polyamino acids, e.g. polylysine, polyarginine, polyglutamic acid or peptide TAT}
- A61K 47/6901: {Conjugates being cells, cell fragments, viruses, ghosts, red blood cells or viral vectors}
- A61K 47/6911: {the form being a liposome}
- A61K 47/6951: {using cyclodextrin (cyclodextrins used as simple excipients A61K47/40)}
- A61K 47/6957: {the form being a device or a kit, e.g. stents or microdevices}
- C12N 15/113: Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides; {Antisense DNA or RNA; Triplex- forming oligonucleotides; Catalytic nucleic acids, e.g. ribozymes; Nucleic acids used in co-suppression or gene silencing (when used in plants C12N15/8218)}
- C12N 15/88: using microencapsulation, e.g. using {amphiphile} liposome vesicle
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- C12N: MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA (microbiological testing media C12Q1/00)

## Abstract

The present invention relates to methods for loading extracellular vesicles (EVs) with a pharmacological agent. The invention discloses the use of cell-penetrating peptides as carriers into EVs, using either a non-covalent or covalent loading approach. Furthermore, the present invention pertains to medical uses and compositions comprising such pharmacological agent-loaded EVs.

## Claims

### Claim 1

A method for loading exosomes with at least one pharmacological agent, comprising exposing a population of exosomes to at least one pharmacological agent and at least one cell-penetrating peptide (CPP), wherein the at least one pharmacological agent and the at least one CPP are present in the form of a non-covalent complex.

### Claim 2 (depends on 1)

The method according to claim 1, further comprising an electroporation step or the use of a lipid-based transfection reagent.

### Claim 3

A method for loading an exosome with at least one pharmacological agent, comprising the steps of:
i. exposing a population of exosome source cells to the at least one pharmacological agent and at least one cell-penetrating peptide (CPP), wherein the at least one pharmacological agent and the at least one CPP are present in the form of a non-covalent complex; and,
ii. harvesting exosomes produced by the exosome source cells, wherein the exosomes comprise said pharmacological agent.

### Claim 4 (depends on 3)

The method according to claim 3, further comprising combining step (i) with electroporation of the exosome source cells.

### Claim 5 (depends on 1)

The method according to claim 1, wherein the non-covalent complex between the at least one CCP and the at least one pharmacological agent are present in the form of nanoparticles with positive or negative zeta potential.

### Claim 6 (depends on 3)

The method according to claim 3, wherein the non-covalent complex between the at least one CCP and the at least one pharmacological agent are present in the form of nanoparticles with positive or negative zeta potential.