PCL-PEG Acetal Polymer for Solvent-Free Drug Delivery

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Solution Overview

Problem

Current drug delivery systems face challenges with low drug loading efficiency and the use of organic solvents, which can be detrimental to sensitive drugs like proteins and peptides, and there is a need for better controlled release systems for sustained delivery of biologically active agents.

Innovation Solution

A semi-solid polymer composed of polycaprolactone (PCL) and polyethylene glycol (PEG) units, conjugated to form an acetal group, allowing for efficient drug loading and release of a wide range of drugs, including hydrophobic and hydrophilic molecules, with tunable release rates and biocompatible degradation products.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If organic solvents are used to dissolve drugs during dosage preparation, then drug solubility is improved, but safety and drug stability deteriorate due to residual solvent and detrimental effects on delicate drugs

Engineering Contradiction:
Improvedrug solubilityVSAvoidresidual solvent safety concern
Core Design Contradiction:
Quantity of substanceVSObject-affected harmful factors

Solution Approach 1:

The patent uses a semi-solid polymer composition as an intermediary carrier that replaces organic solvents. The polymer matrix absorbs and holds the drug, enabling dissolution and delivery without requiring harmful organic solvents. This intermediary approach allows thermally sensitive and solvent-sensitive drugs to be formulated safely.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent changes the physical state and composition parameters by using a semi-solid polymer matrix instead of liquid organic solvents. The polymer composition's physical properties (viscosity, semi-solid state) enable drug incorporation without organic solvents, altering the formulation parameters to eliminate harmful residual solvents while maintaining drug solubility and stability.

Inventive Principle:
Principle #35Parameter changes

2Ease of operation

If conventional micelles or nanoparticles are used for drug encapsulation, then drug delivery capability is improved, but drug loading efficiency deteriorates to low percentages

Engineering Contradiction:
Improvedrug delivery capabilityVSAvoiddrug loading efficiency
Core Design Contradiction:
Ease of operationVSQuantity of substance

Solution Approach 1:

The patent employs a composite semi-solid polymer composition combining multiple polymer components with specific functional groups. This composite material structure enables high drug loading efficiency while maintaining delivery capability, as the polymer matrix can incorporate large amounts of drug through its amorphous structure and hydrogen bonding capabilities.

Inventive Principle:
Principle #40Composite materials

Solution Approach 2:

The semi-solid polymer composition utilizes an amorphous porous matrix structure that allows high drug loading. The porous nature of the polymer matrix provides extensive space for drug incorporation, achieving high loading percentages compared to conventional dense micelle or nanoparticle structures.

Inventive Principle:
Principle #31Porous materials

3Stability of the object's composition

If thermally sensitive drugs are formulated using conventional methods, then drug stability is maintained, but formulation complexity increases due to need for special processing conditions

Engineering Contradiction:
Improvedrug stabilityVSAvoidformulation processing complexity
Core Design Contradiction:
Stability of the object's compositionVSDevice complexity

Solution Approach 1:

The semi-solid polymer acts as a protective intermediary that shields thermally sensitive drugs from harmful thermal and solvent conditions during formulation. The polymer matrix provides a stable environment that maintains drug stability while simplifying the formulation process, as no special temperature-controlled processing is required.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent uses a biodegradable polymer matrix that can be easily synthesized and discarded after delivering the drug. This approach simplifies formulation processing by using readily available polymer materials that don't require complex processing, and the polymer naturally degrades in the body after serving its purpose.

Inventive Principle:
Principle #27Cheap short-living objects (Disposable)

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 polymer enables high drug loading efficiency, biocompatible, and cost-effective delivery of various drugs, including proteins and peptides, through minimally invasive injection or topical application, with controlled release profiles and stability across different pH environments.

Implementation Method 1

The polymer is capable of loading and releasing a wide range of drugs... the degradation products are biocompatible

Methodology Applied
Scientific EffectHydrolysis: Hydrolysis

Data Source

PatentUS10226534B2Semi-solid delivery systems
Publication Date: 2019.03.12 REGENTS OF THE UNIVERSITY OF MINNESOTA
  • US10226534B2 patent drawing
  • US10226534B2 patent drawing
  • US10226534B2 patent drawing

AI summary

The invention provides semi-solid systems for delivering biologically active materials that include a polymer comprising 1) one or more polycaprolactone (PCL) units and 2) at least one or more polyethylene glycol (PEG) units; wherein at least one of said polycaprolactone units is conjugated to a PEG forming an acetal group.