# US 11,992,560 B2 · Electrospun fibers for a local release of an anti-inflammatory drug and a promyelinating drug

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- Number: US 11,992,560 B2
- Document ID: US11992560B2
- Status: Granted
- Kind: B2
- Application number: 17/251,601
- Filed: 2018-06-14
- Published: 2021-08-12
- Granted: 2024-05-28
- Earliest claimed: 2018-06-14
- Assignees: Alma Mater Studiorum - Università di Bologna
- Applicants: Alma Mater Studiorum—Università Di Bologna
- Inventors: Laura Calza; Luciana Giardino; Maria Letizia Focarete; Chiara Gualandi; Maria-Laura Bolognesi; Nadia Passerini; Giampiero Pagliuca; Teresa Gazzotti; Elisa Zironi
- Web page: https://patentgrep.com/patent/US11992560B2

## CPC

- A61K 9/70: Web, sheet or filament bases {; Films; Fibres of the matrix type containing drug (hollow drug-filled fibres A61K9/0092)}
- A61K 9/0024: {Solid, semi-solid or solidifying implants, which are implanted or injected in body tissue (compositions for intravenous administration, normal injectable solutions or dispersions for, e.g. subcutaneous administration A61K9/0019; brain implants A61K9/0085; (coated) prostheses, catheters or stents A61L)}
- A61K 31/12: Ketones
- A61K 31/19: Carboxylic acids, e.g. valproic acid (salicylic acid A61K31/60)
- A61K 31/192: having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid {(cannabinoids A61K31/658)}
- A61K 31/196: the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
- A61K 31/197: the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid (carnitine A61K31/205)
- A61K 31/198: Alpha-amino acids, e.g. alanine or edetic acid [EDTA] (betaine A61K31/205; proline A61K31/401; tryptophan A61K31/405; histidine A61K31/4172; peptides not degraded to individual amino acids A61K38/00)
- A61K 31/40: having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K 31/405: Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
- A61K 31/407: condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
- A61K 31/42: Oxazoles
- A61K 31/421: 1,3-Oxazoles, e.g. pemoline, trimethadione
- A61K 31/4418: having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
- A61K 31/5415: ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
- A61K 31/5575: having a cyclopentane, e.g. prostaglandin E2, prostaglandin F2-alpha
- A61K 31/603: having further aromatic rings, e.g. diflunisal
- A61K 31/704: attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin {(digitoxin A61K31/7048)}
- A61P 25/28: for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The present invention relates to electro spun fibers for a local release in the central nervous system of an anti-inflammatory and a promyelinating agent over a defined time-window, in order to limit secondary neurodegeneration triggered by the glutamate release and supported by on-going inflammation. The combined treatment aimed to reduce inflammation and improve remyelination in the very early stage of the pathology improving the chronic clinical outcome of the lesion. In particular the present invention relates to electrospun polymeric fibers, wherein said fibers are loaded with 3,3,5-Triiodo-L-thyronine (T3) and Ibuprofen.

## Claims

### Claim 1

Electrospun polymeric fibers in the form of scaffold, wherein part or all of said fibers are loaded with the promyelinating agent 3,3,5-Triiodo-L-thyronine (T3) and another part or all of said fibers are loaded with an anti-inflammatory agent, for a local release of said promyelinating agent and said anti-inflammatory agent in a method of treating a spinal cord injury, wherein said electrospun polymeric fibers are suitable to be implanted directly on top of a lesion, wherein the local release of said promyelinating agent and said anti-inflammatory agent in a method of treating a spinal cord injury occurs over an estimated time of 8 to 14 days.

### Claim 2 (depends on 1)

The electrospun fibers according to claim 1 wherein said anti-inflammatory agent is selected from a non-steroidal anti-inflammatory drug (NSAID), a salicylate, an anti-inflammatory glucocorticoid, and pirfenidone.

### Claim 3 (depends on 2)

The electrospun fibers according to claim 2 wherein said anti-inflammatory agent is a non-steroidal anti-inflammatory drug (NSAID) selected from ibuprofen, flurbiprofen, diclofenac, and diclofenac with misoprostol, indomethacin, ketoprofen, fenbrufen, naproxen, sulindac, celecoxib, nabumetone, mefenamic acid, oxyphenbutazone, diflunisal, etodolac, fenoprofen, flurbiprofen, meclofenamate, meloxicam, nabumetone, oxaprozin, piroxicam, tolmetin, valdecoxib and propionic acid derivatives or their mixture.

### Claim 4 (depends on 1)

The electrospun fibers according to claim 1 wherein said promyelinating agent is T3 and said anti-inflammatory agent is ibuprofen.

### Claim 5 (depends on 1)

The electrospun fibers according to claim 1 wherein said polymeric fibers are biopolymeric fibers.

### Claim 6 (depends on 1)

The electrospun fibers according to claim 1 wherein said polymer is selected from synthetic polyesters, polylactic acid (PLLA), polyglycolic acid (PGA), polycaprolactone (PCL) and/or their copolymers and/or their mixtures, polyurethanes, polyamides, fluorinate polymers, or their copolymers and/or mixture, or natural polymers selected from proteins, polysaccharides, polyesters, polypeptides and their copolymers and/or their mixtures.

### Claim 7 (depends on 1)

The electrospun fibers according to claim 1 wherein said polymeric fibers are biocompatible fibers.

### Claim 8 (depends on 1)

The electrospun fibers according to claim 1 wherein between 10 and 90% of said fibers are loaded with the promyelinating agent 3,3,5-Triiodo-L-thyronine (T3).

### Claim 9 (depends on 1)

The electrospun fibers according to claim 1 wherein between 10 and 90% of said fibers are loaded with the anti-inflammatory agent.

### Claim 10 (depends on 1)

The electrospun fibers according to claim 1 wherein all of said fibers are loaded with the promyelinating agent 3,3,5-Triiodo-L-thyronine (T3) and the anti-inflammatory agent.

### Claim 11 (depends on 1)

The electrospun fibers according to claim 1 wherein the promyelinating agent and/or the anti-inflammatory agent is encapsulated within said fibers by non-covalent binding.