# US 12,214,105 B2 · Long lasting biodegradable polymer based in-situ forming implant for treatment of bone injuries

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- Number: US 12,214,105 B2
- Document ID: US12214105B2
- Status: Granted
- Kind: B2
- Application number: 17/436,862
- Filed: 2019-03-05
- Published: 2022-05-19
- Granted: 2025-02-04
- Earliest claimed: 2019-03-05
- Assignees: Future University In Egypt
- Applicants: Future University In Egypt
- Inventors: Fatma Samir Abd El-Salam El-Sebaie; Seham Abd Elkhalek Elkheshen; Azza Ahmed Mohamed Mahmoud; Nermeen Adel Ahmed Elkasabgy; Emad Basalious Bashir Basalious; Amany Abdel Monem Mostafa Abdel Rahman; Mohammed Said Mostafa Amer
- Web page: https://patentgrep.com/patent/US12214105B2

## CPC

- A61L 27/18: obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds
- A61P 19/00: Drugs for skeletal disorders
- 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 31/4535: containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
- A61K 47/14: Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
- A61K 47/20: containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
- A61K 47/34: Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers (A61K47/10 takes precedence)
- A61L 27/54: Biologically active materials, e.g. therapeutic substances {(A61L27/227 takes precedence)}
- A61L 27/58: Materials at least partially resorbable by the body
- A61L 2300/412: Tissue-regenerating or healing or proliferative agents
- A61L 2400/06: Flowable or injectable implant compositions
- A61L 2430/02: for reconstruction of bones; weight-bearing implants
- 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
- 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)

## Abstract

A pharmaceutical composition capable of forming free burst release effect in-situ forming implant useful for injection inside bone injuries without surgery is provided. This pharmaceutical composition includes; biodegradable polymer, selective estrogen receptor modulator, organic solvent and liquid lipid, solidifies upon contacting with the surrounding medium and form solid implant with compact framework by in-situ phase separation method to deliver the selective estrogen receptor modulator. This compact framework restores the porous structure of the implant by time which is essential in promoting bone healing.

## Claims

### Claim 1

An In-situ forming implant formulation comprising: poly (lactide-co-glycolide) (PLGA) copolymer in concentration range from 5% to 20% w/v, a selective estrogen receptor modulator, 1-monolinolein in concentration range from 5% to 10% w/v, and an organic solvent.

### Claim 2 (depends on 1)

The In-situ forming implant formulation according to claim 1, wherein the concentration of PLGA copolymer is in concentration of 10% w/v.

### Claim 3 (depends on 1)

The In-situ forming implant formulation according to claim 1, wherein the PLGA copolymer is ester terminated comprising lactide to glycolide ratio of 50:50.

### Claim 4 (depends on 1)

The In-situ forming implant formulation according to claim 1, wherein the PLGA copolymer is ester terminated comprising lactide to glycolide ratio of 75:25.

### Claim 5 (depends on 1)

The In-situ forming implant formulation according to claim 1, wherein the selective estrogen receptor modulator is selected from tamoxifene, tormifene, raloxifene and bazedoxifene, and pharmaceutically acceptable salts thereof.

### Claim 6 (depends on 5)

The In-situ forming implant formulation according to claim 5, wherein the selective estrogen receptor modulator is raloxifene hydrochloride.

### Claim 7 (depends on 1)

The In-situ forming implant formulation according to claim 1, wherein the concentration of 1-monolinolein is 10% w/v.

### Claim 8 (depends on 1)

The In-situ forming implant formulation according to claim 1, wherein the organic solvent is selected from N-methyl-2 pyrrolidone, tetrahydrofuran, methyl acetate, ethyl acetate, dimethyl formamide, dimethyl sulfoxide, dimethylsulfone, triacitin, and propylene glycol.

### Claim 9 (depends on 1)

The In-situ forming implant formulation according to claim 1, wherein the organic solvent is dimethyl sulfoxide.

### Claim 10 (depends on 1)

The In-situ forming implant formulation according to claim 1 comprising 10% w/v 75:25 PLGA ester terminated, 1% w/v raloxifene hydrochloride, 10% w/v 1-monolinolein, and dimethyl sulfoxide.