Biodegradable intranasal system for the sustained-release of an active ingredient in the intranasal cavity

Patent metadata

Field	Value
Publication number	US-2025387407-A1
Application number	US-202318881381-A
Country	US
Kind code	A1
Filing date	Jul 6, 2023
Priority date	Jul 7, 2022
Publication date	Dec 25, 2025
Grant date	—

Abstract

The invention relates to biodegradable intranasal system for the sustained-release of fluticasone propionate in the intranasal cavity, said system comprising a biodegradable polyester matrix that comprises the fluticasone propionate as the active ingredient to be released in the intranasal cavity, wherein the polyester is selected from the list of poly(L,D-lactic acid) (PLA), poly(caprolactone) (PCL), their copolymers such as PLA-PCL, and mixtures thereof; and a method for preparing said system. The invention also relates to a kit comprising the system of the invention and the means of insertion of the system into the nasal cavity. The invention further relates to fluticasone propionate for use for treating chronic rhinitis or chronic sinusitis, wherein the fluticasone propionate is in a form suitable for administration in the nasal cavity by means of the biodegradable intranasal system of the invention.

First claim

1 - 16 . (canceled)

17 . A biodegradable intranasal system for the sustained-release of fluticasone propionate in the intranasal cavity, said system comprising a biodegradable polyester matrix that comprises the fluticasone propionate as the active ingredient to be released in the intranasal cavity, wherein the polyester is selected from the group consisting of poly(D,L-lactic acid) (PDLLA), poly(D-lactic acid) (PDLA), poly(caprolactone) (PCL), copolymers of poly(caprolactone) (PCL) and poly(lactic acid) (PLA), and mixtures thereof.

18 . The biodegradable intranasal system of claim 17 , wherein the polyester is selected from the group consisting of a poly(caprolactone) (PCL), a poly(D,L-lactic acid) (PDLLA) comprising at least 50% L-lactic acid, PLA-PCL copolymers, and mixtures thereof.

19 . The biodegradable intranasal system of claim 17 , wherein the polyester is poly(caprolactone) (PCL) or a mixture of poly(caprolactone) (PCL) and PLA-PCL copolymer.

20 . The biodegradable intranasal system of claim 17 , wherein the polyester is a poly(caprolactone) (PCL).

21 . The biodegradable intranasal system according to claim 17 , wherein the poly(caprolactone) (PCL) has a molar mass between 25,000 g/mol and 250,000 g/mol.

22 . The biodegradable intranasal system according to claim 17 , wherein the content of fluticasone propionate is at most 20% by weight or is between 0.1% and 10% by weight, based on the total weight of the system.

23 . The biodegradable intranasal system according to claim 17 , wherein said system is made of the biodegradable polyester matrix that comprises the fluticasone propionate as the active ingredient to be released in the intranasal cavity.

24 . The biodegradable intranasal system according to claim 17 , wherein said system does not comprise a coating.

25 . The biodegradable intranasal system according to claim 17 , wherein at least 15% by weight of the fluticasone propionate initially present in the system is released after 180 days after introduction of the system in an aqueous or humid medium.

26 . The biodegradable intranasal system according to claim 17 , wherein said system releases the fluticasone propionate in the intranasal cavity for at least 120 days.

27 . The biodegradable intranasal system according to claim 17 , wherein said system releases the fluticasone propionate in the intranasal cavity for at least 240 days.

28 . A kit comprising at least a system as defined in claim 17 and a means of insertion of the system into a nasal cavity.

29 . A method of treating chronic allergic or non-allergic rhinitis comprising administering a biodegradable intranasal system as defined in claim 17 into the nasal cavity of a subject.

30 . A method of treating chronic sinusitis comprising administering a biodegradable intranasal system as defined in claim 17 into the nasal cavity of a subject.

31 . A method for preparing a biodegradable intranasal system comprising a step of forming the system by a treatment selected from extrusion, solvent evaporation, hot pressing, hot injection, freeze drying, electrospinning, molding or 3D printing, said system comprising a biodegradable polyester matrix that comprises fluticasone propionate as an active ingredient to be released in the intranasal cavity, wherein the polyester is selected from the group consisting of poly(D,L-lactic acid) (PDLLA), poly(D-lactic acid) (PDLA), poly(caprolactone) (PCL), copolymers of poly(caprolactone) (PCL) and poly(lactic acid) (PLA), and mixtures thereof.

32 . The method of claim 31 , comprising a preliminary step of mixing together the polyester and the fluticasone propionate, before the treatment step.

Assignees

• Dianosic
• Centre Nat Rech Scient
• Univ Montpellier
• Enscm

Inventors

• Garric Xavier
• Zahouani Sarah
• Moreau Victor

Classifications

• A61K47/34

  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) · CPC title

• A61K9/0043 Primary

  Nose · CPC title

• A61K31/56 Primary

  Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids · CPC title

• A61P11/00

  Drugs for disorders of the respiratory system · CPC title

• A61K9/7007

  Drug-containing films, membranes or sheets (A61K9/0041, A61K9/0043, A61K9/006, A61K9/0063 take precedence) · CPC title