Hyper-compressed PLGA Microparticles for Sustained Drug Release

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Solution Overview

Problem

Current ocular and local drug delivery systems face challenges in providing long-acting, localized release of therapeutic agents without systemic side effects, requiring improved formulations and delivery methods that ensure stability, controlled release, and reduced dosing frequency.

Innovation Solution

The development of hyper-compressed micro and nano particles using biocompatible polymers like PLGA, which are compressed to alter drug release profiles, allowing for controlled and consistent release of therapeutic agents over extended periods, suitable for localized treatment of various conditions.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Duration of action of moving object

If conventional ocular inserts are used for localized drug delivery, then localized treatment is achieved, but the duration of action is limited requiring frequent dosing

Engineering Contradiction:
Improveduration of drug releaseVSAvoiddosing frequency
Core Design Contradiction:
Duration of action of moving objectVSEase of operation

Solution Approach 1:

The patent changes the physical and chemical parameters of the drug delivery system by using hyper-compressed microparticles with controlled porosity and polymer composition (PLGA with specific lactide:glycolide ratios). These parameter changes enable sustained release over weeks to months, transforming the dosing paradigm from frequent daily/weekly insert replacement to single-implant long-term therapy.

Inventive Principle:
Principle #35Parameter changes

2Reliability

If systemic administration is used to ensure adequate drug levels, then therapeutic effect is achieved, but toxic side effects occur

Engineering Contradiction:
Improvetherapeutic efficacyVSAvoidsystemic side effects
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent applies local quality by creating a localized reservoir of drug at the implant site with controlled release kinetics. The hyper-compressed microparticle matrix provides high local drug concentration where needed while maintaining low systemic levels, achieving therapeutic efficacy at the target site without systemic toxicity.

Inventive Principle:
Principle #3Local quality

3Reliability

If frequent dosing is required to maintain therapeutic levels, then drug efficacy is maintained, but patient compliance deteriorates

Engineering Contradiction:
Improvetherapeutic level maintenanceVSAvoidpatient compliance
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

The patent employs preliminary action by pre-formulating the drug in a controlled-release matrix that automatically maintains therapeutic levels over extended periods. The single implantation event pre-establishes the drug delivery system, eliminating the need for repeated patient actions (dosing) while maintaining reliable therapeutic levels through the engineered release profile.

Inventive Principle:
Principle #10Preliminary action

4Adaptability or versatility

If localized radiation treatment is used to confine therapy to a specific organ, then localized treatment is achieved, but the approach cannot be applied to pharmacological treatments

Engineering Contradiction:
Improvelocalization capabilityVSAvoidsystemic exposure
Core Design Contradiction:
Adaptability or versatilityVSObject-generated harmful factors

Solution Approach 1:

The patent uses composite materials by combining biocompatible polymers (PLGA) with therapeutic agents in a hyper-compressed microparticle matrix. This composite structure provides both the mechanical integrity needed for implantation and the controlled release properties necessary for localized pharmacological therapy, adapting the localization concept from radiation to pharmacology.

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

This approach enables a controlled, sustained release of drugs with reduced systemic side effects, improved patient compliance, and localized treatment efficacy, as demonstrated by the prolonged release of dexamethasone in ocular tissues and other applications.

Implementation Method 1

The rate of drug diffusion is controlled by the polymer composition, the membrane thickness, and the solubility of the drug

Methodology Applied
Scientific EffectDiffusion: Diffusion

Implementation Method 2

The polymer undergoes resorption by the body through the process of hydrolysis

Methodology Applied
Scientific EffectHydrolysis: Hydrolysis

Data Source

PatentUS8071119B2Controlled release implantable dispensing device and method
Publication Date: 2011.12.06 SUSTAINED NANO SYSTEMS LLC
  • US8071119B2 patent drawing
  • US8071119B2 patent drawing
  • US8071119B2 patent drawing

AI summary

A dispensing device having a polymer which is combined with a therapeutic agent in the form of a microparticle or nanoparticle which is “hyper-compressed” to form a controlled release dispensing device and methods of locally administering a therapeutic agent using said microparticles.