Biobased Hyperbranched Polyesters for Sustained Drug Delivery

Resolve Bottlenecks,
Find Innovative Solutions
Generate Solutions

Solution Overview

Problem

Current drug delivery systems face challenges such as limited drug potency due to degradation before reaching the target site, difficulty in targeting specific areas of the body, and the need for complex synthetic polymers that are not readily bioresorbable or biodegradable, making it hard to achieve controlled and sustained release of medications.

Innovation Solution

Development of biobased, biodegradable hyperbranched polyesters using bimolecular non-linear polymerization (BMNLP) to create a composition where active ingredients can be covalently bonded or encapsulated, allowing for controlled release through hydrolysis or enzymatic action, with monomers like glycerol and adipic or succinic acid, enabling targeted and sustained delivery.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If synthetic polymers are used for sustained release delivery systems, then controlled release and targeting capability are improved, but biodegradability and bioresorbability deteriorate causing adverse effects

Engineering Contradiction:
Improvecontrolled release capabilityVSAvoidadverse effects from non-biodegradability
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent changes the chemical composition parameters of the polymer from conventional synthetic materials to hyperbranched polyesters with specific functional groups (carboxyl, hydroxyl, amino) that enable both controlled release through hydrolysis/enzymatic degradation and complete biodegradability into benign products

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates a composite structure where the hyperbranched polyester serves as both the delivery vehicle and the degradation product, combining controlled release functionality with biodegradability in a single material system rather than requiring separate components

Inventive Principle:
Principle #40Composite materials

2Quantity of substance

If covalent bonding of high concentrations of actives to polymers is attempted, then drug loading capacity is improved, but synthetic complexity and cost increase

Engineering Contradiction:
Improvedrug loading capacityVSAvoidsynthetic complexity
Core Design Contradiction:
Quantity of substanceVSDevice complexity

Solution Approach 1:

The patent extracts the complex multi-step covalent bonding synthesis from the formulation process and replaces it with a simpler physical encapsulation method where drugs are loaded into the hyperbranched polyester structure during polymerization or by dissolution, eliminating the need for separate conjugation steps

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The patent performs preliminary encapsulation of the drug within the hyperbranched polyester structure during the polymerization process itself, rather than requiring post-polymerization modification or complex conjugation chemistry, thereby simplifying the overall synthetic pathway

Inventive Principle:
Principle #10Preliminary action

3Ease of operation

If medications are administered orally for sustained release, then patient compliance and ease of administration are improved, but drug degradation in the stomach and tissue barrier penetration deteriorate

Engineering Contradiction:
Improveease of administrationVSAvoiddrug integrity and delivery efficiency
Core Design Contradiction:
Ease of operationVSReliability

Solution Approach 1:

The patent imparts local protective quality to the drug by encapsulating it within the hydrophobic interior of the hyperbranched polyester structure, creating a protective microenvironment that shields the drug from gastric acid degradation while allowing controlled release at the target site

Inventive Principle:
Principle #3Local quality

Solution Approach 2:

The patent introduces the hyperbranched polyester as an intermediary carrier between the oral administration route and the target tissue, which protects the drug during gastrointestinal transit and facilitates controlled delivery to the target site through its degradation and release mechanisms

Inventive Principle:
Principle #24Intermediary (Mediator)

4Stability of the object's composition

If poly-condensation reactions or ring opening polymerization are used to synthesize polyesters from renewable feedstocks, then biobased and biodegradable properties are improved, but molecular weight control and polymer uniformity deteriorate

Engineering Contradiction:
Improvebiobased and biodegradable propertiesVSAvoidmolecular weight control
Core Design Contradiction:
Stability of the object's compositionVSManufacturing precision

Solution Approach 1:

The patent segments the polymerization process into controlled stages using stepwise addition of monomers and controlled hydrolysis conditions, allowing precise control over molecular weight and polydispersity while maintaining the biobased and biodegradable characteristics of the polyester structure

Inventive Principle:
Principle #1Segmentation

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 solution achieves controlled release of active ingredients with high loading capacity, biocompatibility, and biodegradability, providing effective and targeted delivery while minimizing systemic toxicity and biochemical degradation, and allowing for recycling of residual materials.

Implementation Method 1

The active ingredient can be released at the point of delivery, usually by hydrolysis or enzymatic action

Methodology Applied
Scientific EffectHydrolysis: Hydrolysis

Implementation Method 2

The active ingredient can be released at the point of delivery, usually by hydrolysis or enzymatic action

Methodology Applied
Scientific EffectEnzymatic action: Enzyme

Data Source

PatentUS12030986B2Sustained release composition using biobased biodegradable hyperbranched polyesters
Publication Date: 2024.07.09 MICHIGAN STATE UNIV
  • US12030986B2 patent drawing
  • US12030986B2 patent drawing
  • US12030986B2 patent drawing

AI summary

The present invention provides a sustained release composition having hyperbranched polymers that are polyesters that are biobased and biodegradable, and that have at least one active ingredient, which composition delivers the active ingredient over time. These active ingredients can be a wide variety of compounds so long as they can covalently bind to the polymer or be encapsulated in the polymer in a manner that is released at the point of delivery, usually by acid hydrolysis or enzymatic bond scission.