PLGA Anti-Inflammatory Microspheres for Sustained Joint Pain Relief

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Solution Overview

Problem

Current treatments for joint pain and inflammation, such as rheumatoid arthritis and osteoarthritis, often cause systemic side effects and fail to provide sustained relief, necessitating a localized, sustained-release formulation that minimizes these side effects.

Innovation Solution

A formulation of microspheres containing a steroidal and non-steroidal anti-inflammatory drugs encapsulated in poly(lactic-co-glycolic acid) copolymers (PLGA), with a high initial release rate followed by controlled release over several months, suspended in a diluent solution, preferably with hyaluronic acid.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If oral anti-inflammatory medications are administered, then systemic anti-inflammatory effect is achieved, but systemic side effects occur including stomach irritation and HPA axis suppression

Engineering Contradiction:

Improvesystemic anti-inflammatory effectVSAvoidsystemic side effects

Core Design Contradiction:

Quantity of substanceVSObject-affected harmful factors

Solution Approach 1:

The patent extracts the anti-inflammatory action from systemic circulation and localizes it to the joint space through intra-articular injection of microspheres. This delivers the therapeutic effect directly to the target site while eliminating exposure of the stomach and other systemic organs to the medication, thereby resolving the contradiction between achieving anti-inflammatory effect and avoiding systemic side effects.

Inventive Principle:

Principle #2Taking out (Extraction)

Solution Approach 2:

The patent uses microspheres as an intermediary carrier that releases anti-inflammatory medication locally within the joint space. This intermediary system allows the drug to act where needed without entering systemic circulation in significant amounts, thus achieving therapeutic effect while minimizing systemic side effects like stomach irritation and HPA axis suppression.

Inventive Principle:

Principle #24Intermediary (Mediator)

2Object-affected harmful factors

If localized intra-articular injection is administered, then systemic side effects are reduced, but duration of action is insufficient requiring repeated injections

Engineering Contradiction:

Improvesystemic side effectsVSAvoidduration of relief

Core Design Contradiction:

Object-affected harmful factorsVSDuration of action of moving object

Solution Approach 1:

The patent incorporates anti-inflammatory medication into microspheres during manufacturing, preparing the drug in a controlled-release format before administration. This preliminary action ensures that when injected into the joint, the medication is already configured to release over an extended period, providing sustained relief for months without requiring repeated injections.

Inventive Principle:

Principle #10Preliminary action

Solution Approach 2:

The patent changes the physical and chemical parameters of the medication delivery system by using microspheres with controlled porosity and degradation rates. These parameter changes enable the drug to be released slowly over time from the microsphere matrix, extending the duration of action from days to months while maintaining localized action and minimizing systemic side effects.

Inventive Principle:

Principle #35Parameter changes

3Speed

If high dose corticosteroids are injected locally, then immediate anti-inflammatory effect is achieved, but rapid depletion occurs requiring frequent re-injection

Engineering Contradiction:

Improveonset of anti-inflammatory effectVSAvoidduration of relief

Core Design Contradiction:

SpeedVSDuration of action of moving object

Solution Approach 1:

The patent implements periodic action through controlled-release microspheres that release corticosteroid medication in a sustained manner over time. The microsphere matrix provides an initial burst release for immediate effect, followed by gradual release over months, creating a periodic delivery pattern that maintains therapeutic levels without rapid depletion and eliminates the need for frequent re-injection.

Inventive Principle:

Principle #19Periodic action

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

Provides immediate pain relief with sustained anti-inflammatory effects for up to three months, reducing systemic side effects and acting as a joint lubricant, while minimizing stomach irritation and HPA axis suppression.

Implementation Method 1

both the steroidal and the non-steroidal drugs are controlled released over several months for sustained pain relief

Methodology Applied

Scientific EffectDiffusion: Diffusion

Implementation Method 2

microspheres of poly(lactic-co-glycolic acid) copolymers (PLGA), wherein the steroidal drug can be initially released from the microspheres in the first week

Methodology Applied

Scientific EffectPolymer degradation: Decomposition (biological)

Implementation Method 3

a diluent solution in which the drug microspheres are suspended, preferably in the presence of hyaluronic acid

Methodology Applied

Scientific EffectLubrication: Lubrication

Data Source

PatentUS12589102B2Injectable sustained-release formulations for treatment of joint pain and inflammation

Publication Date: 2026.03.31 FORDOZ PHARMA CORP

AI summary

Drug-loaded microspheres containing both a steroidal anti-inflammatory drug and a non-steroidal anti-inflammatory drug and injectable formulations containing the microspheres for sustained release of both drugs are disclosed. Methods of making such drug-loaded microspheres, formulations, and use of them for treating pains and inflammations, especially those caused by rheumatoid arthritis or osteoarthritis using such microspheres and formulations are also described.