# US 11,998,638 B2 · Microparticles comprising PCL and uses thereof

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- Number: US 11,998,638 B2
- Document ID: US11998638B2
- Status: Granted
- Kind: B2
- Application number: 17/549,894
- Filed: 2021-12-14
- Published: 2022-04-07
- Granted: 2024-06-04
- Earliest claimed: 2007-07-26
- Assignees: Aqtis IP BV
- Applicants: Aqtis I.P. B.V.
- Inventors: Henderikus Super; Paul Willem Mijnen; Pieter Gerard Zijlstra; Dirk Wybe Grijpma
- Web page: https://patentgrep.com/patent/US11998638B2

## CPC

- A61K 9/14: Particulate form, e.g. powders, {Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles (microspheres A61K9/16; microcapsules A61K9/50; nanocapsules, nanoparticles of the matrix type A61K9/51)}
- A61K 8/025: {Explicitly spheroidal or spherical shape}
- A61K 8/042: {Gels}
- A61K 8/85: Polyesters
- 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 9/06: Ointments; Bases therefor; {Other semi-solid forms, e.g. creams, sticks, gels (composition of ointments, creams or gels A61K47/00)}
- A61K 9/1647: {Polyesters, e.g. poly(lactide-co-glycolide)}
- A61K 9/5031: {obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poly(lactide-co-glycolide)}
- A61K 31/167: having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
- A61K 31/245: Amino benzoic acid types, e.g. procaine, novocaine (salicylic acid esters A61K31/60)
- A61K 31/445: Non condensed piperidines, e.g. piperocaine
- A61K 31/765: Polymers containing oxygen
- A61L 27/18: obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds
- A61L 27/52: Hydrogels or hydrocolloids
- A61P 1/00: Drugs for disorders of the alimentary tract or the digestive system
- A61P 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
- A61P 11/00: Drugs for disorders of the respiratory system
- A61P 11/04: for throat disorders
- A61P 13/10: of the bladder
- A61P 15/10: for impotence
- A61P 17/00: Drugs for dermatological disorders
- A61P 17/02: for treating wounds, ulcers, burns, scars, keloids, or the like
- A61P 23/00: Anaesthetics
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- A61Q 19/00: Preparations for care of the skin
- A61Q 19/08: Anti-ageing preparations
- A61K 9/0019: {Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner (non-active ingredients are additionally classified in A61K47/00)}
- A61K 2800/412: Microsized, i.e. having sizes between 0.1 and 100 microns
- A61K 2800/54: Polymers characterized by specific structures/properties
- A61K 2800/654: The particulate/core comprising macromolecular material
- A61K 2800/91: Injection
- 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)
- A61L: METHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES (preservation of bodies or disinfecting characterised by the agents employed A01N; preserving, e.g. sterilising, food or foodstuffs A23; preparations for medical, dental or toiletry purposes A61K)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61Q: SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS

## Abstract

The invention relates to a process for preparing PCL-comprising microparticles, to microparticles obtainable by said process, to gel hence obtained and to several uses of the gel such as for the preparation of a medicament for treating a skin abnormality or disfigurement, and/or for controlling bladder function and/or controlling gastric reflux and/or for treating erectile dysfunction and/or for treating vocal cords. The gel may also be used for cosmetic applications.

## Claims

### Claim 1

An implant or filler composition comprising a biodegradable, injectable gel and further comprising microparticles, each microparticle comprising polycaprolactone (PCL) and having:
i) homogenous density and form,
ii) homogenous PCL content throughout the microparticle, and
iii) essentially spherical and smooth surface,
wherein at least 80 weight percent of the microparticles has a diameter distribution range between 25 and 75 μm.

### Claim 2 (depends on 1)

The implant or filler composition according to claim 1, wherein each microparticle comprises a PCL homopolymer.

### Claim 3 (depends on 1)

The implant or filler composition according to claim 1, further comprising an anesthetic.

### Claim 4 (depends on 1)

The implant or filler composition according to claim 1, further comprising an active ingredient.

### Claim 5 (depends on 1)

The implant or filler composition to claim 1, wherein the microparticles are formed from a PCL polymer solution and a liquid comprising methylcellulose as a single surfactant.

### Claim 6 (depends on 5)

The implant or filler composition to claim 5, wherein the liquid comprises at least 0.8% w/w % methylcellulose.

### Claim 7 (depends on 1)

The implant or filler composition to claim 1, wherein the composition is a cosmetic composition.

### Claim 8 (depends on 1)

A method to augment soft tissue in a subject in need thereof, comprising administering to the subject in need thereof the implant or filler composition according to claim 1.

### Claim 9 (depends on 8)

The method according to claim 8, wherein the method is for treating a skin abnormality or disfigurement, for controlling bladder function, for controlling gastric reflux, for treating erectile dysfunction, for treating congenital abnormalities, for filling up gums for dental treatment and/or for treating vocal cords.

### Claim 10 (depends on 8)

The method according to claim 8, wherein the administration is repeated periodically.