Biodegradable Intranasal Fluticasone Matrix for Long-Term Release

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Solution Overview

Problem

Existing treatments for chronic rhinitis and sinusitis require frequent administration of fluticasone propionate nasal sprays, and there is a need for a sustained-release formulation that can last for at least 6 months to improve compliance and ease of use.

Innovation Solution

A biodegradable intranasal system using a polyester matrix of poly(L,D-lactic acid), poly(D-lactic acid), poly(caprolactone), or their copolymers is developed to release fluticasone propionate in the nasal cavity for at least 6 months, ensuring mechanical stability and effective drug delivery.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Duration of action of moving object

If fluticasone propionate is administered by nasal sprays several times a day, then the medication can be easily administered, but the compliance is difficult and the duration of action is short (less than 1 month)

Engineering Contradiction:
Improveduration of actionVSAvoidease of administration
Core Design Contradiction:
Duration of action of moving objectVSEase of operation

Solution Approach 1:

The patent applies preliminary action by pre-loading the intranasal device with fluticasone propionate during manufacturing. The device is prepared in advance with the active ingredient embedded in the polymer matrix, so that when inserted into the nasal cavity, the drug is already positioned for sustained release without requiring frequent user application. This resolves the contradiction by maintaining ease of administration (simple insertion) while achieving extended duration of action (up to 12 months).

Inventive Principle:
Principle #10Preliminary action

Solution Approach 2:

The patent implements continuity of useful action through the biodegradable polymer matrix that continuously releases fluticasone propionate over extended periods (6-12 months). The polymer structure maintains stable drug release through controlled degradation, ensuring uninterrupted therapeutic action. This eliminates the need for frequent reapplication while maintaining effective drug delivery, resolving the contradiction between duration of action and ease of administration.

Inventive Principle:
Principle #20Continuity of useful action

2Duration of action of moving object

If a sustained-release formulation is developed to last for at least 6 months, then the duration of action is improved, but the device complexity increases

Engineering Contradiction:
Improveduration of actionVSAvoiddevice complexity
Core Design Contradiction:
Duration of action of moving objectVSDevice complexity

Solution Approach 1:

The patent applies parameter changes by selecting and optimizing specific polymer parameters (molecular weight, composition, degradation rate) to achieve sustained release over 6-12 months. By carefully controlling polymer characteristics such as using poly(glycolic acid)-poly(lactic acid) copolymers with specific ratios and molecular weights, the device achieves extended duration of action without requiring complex mechanical structures. This resolves the contradiction by extending duration through material parameter optimization rather than increasing device complexity.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent utilizes composite materials by combining fluticasone propionate with biodegradable polymer matrices (poly(glycolic acid), poly(lactic acid), and their copolymers). This composite structure enables sustained release through controlled polymer degradation while maintaining relatively simple device geometry. The composite material approach achieves extended duration of action (6-12 months) without significantly increasing device complexity, as the sustained release function is embedded in the material composition rather than requiring complex mechanical mechanisms.

Inventive Principle:
Principle #40Composite materials

3Stability of the object's composition

If the polyester matrix is designed to maintain mechanical integrity for over a year, then the stability of the object is improved, but the degradation time must be precisely controlled

Engineering Contradiction:
Improvemechanical integrityVSAvoiddegradation time control
Core Design Contradiction:
Stability of the object's compositionVSDevice complexity

Solution Approach 1:

The patent applies parameter changes by optimizing polymer molecular weight, composition ratios, and crystallinity parameters to achieve precise control over degradation time while maintaining mechanical integrity for 6-12 months. By adjusting parameters such as polymer molecular weight and copolymer composition, the degradation rate can be precisely tuned to match the required duration of action. This resolves the contradiction by achieving stable mechanical properties through parameter optimization rather than complex structural design.

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent uses composite materials with specific polymer combinations (poly(glycolic acid)-poly(lactic acid) copolymers) that provide balanced mechanical stability and controlled degradation. The composite material structure allows simultaneous achievement of long-term mechanical integrity and predictable degradation over 6-12 months. The material composition itself provides the degradation control mechanism, eliminating the need for complex external control systems. This resolves the contradiction by embedding both stability and controlled degradation within the material composition.

Inventive Principle:
Principle #40Composite materials

Applied Scientific Principles

This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.

Function Achieved in This Case

The system provides a sustained-release of fluticasone propionate for treating chronic rhinitis and sinusitis, maintaining mechanical integrity for over a year and ensuring effective drug delivery without frequent reapplication.

Implementation Method 1

a biodegradable system comprising a polyester matrix that comprises poly(L,D-lactic acid) (PDLLA), poly(D-lactic acid) (PDLA), poly(caprolactone) (PCL), copolymers of poly(caprolactone) (PCL) and poly(lactic acid) (PLA)

Methodology Applied
Scientific EffectHydrolysis: Hydrolysis

Data Source

PatentUS20250387407A1Biodegradable intranasal system for the sustained-release of an active ingredient in the intranasal cavity
Publication Date: 2025.12.25 DIANOSIC
  • US20250387407A1 patent drawing
  • US20250387407A1 patent drawing
  • US20250387407A1 patent drawing

AI summary

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.