Peptide Formulation Viscosity and Release Control

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Solution Overview

Problem

Existing depot formulations for peptide active agents suffer from high viscosity, irritation at the injection site, limited drug load, and a 'burst/lag' release profile, which can lead to undesirable concentration spikes and require frequent dosing.

Innovation Solution

A pre-formulation comprising a low viscosity mixture of diacyl glycerol, phosphatidyl choline, organic mono-alcoholic solvent, polar solvent, and a peptide active agent, which forms a non-lamellar liquid crystalline phase upon contact with aqueous fluids, providing a controlled and sustained release of the peptide.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If conventional depot formulations are used, then peptide delivery is achieved, but high viscosity causes administration difficulty and requires wide needles

Engineering Contradiction:

Improveease of administrationVSAvoidviscosity

Core Design Contradiction:

Ease of operationVSStrength

Solution Approach 1:

The patent changes the physical-chemical parameters of the formulation by using lipid-based carriers and co-solvents to reduce viscosity while maintaining peptide stability and delivery effectiveness

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The patent introduces lipid-based carriers and co-solvents as intermediary substances that mediate between the peptide and the injection site, enabling easier administration through narrow needles while maintaining therapeutic effect

Inventive Principle:

Principle #24Intermediary (Mediator)

2Ease of operation

If conventional formulations are used, then peptide delivery is achieved, but irritation at injection site occurs

Engineering Contradiction:

Improveease of administrationVSAvoidinjection site irritation

Core Design Contradiction:

Ease of operationVSObject-affected harmful factors

Solution Approach 1:

The patent uses lipid-based carriers as intermediary substances that are biocompatible and non-irritating, mediating peptide delivery while protecting the injection site from irritation

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent employs biodegradable lipid carriers that are naturally metabolized by the body, eliminating long-term irritation issues as these carriers are temporarily present and then broken down into harmless substances

Inventive Principle:

Principle #27Cheap short-living objects (Disposable)

3Quantity of substance

If conventional formulations are used, then peptide delivery is achieved, but limited drug load restricts therapeutic efficacy

Engineering Contradiction:

Improvedrug loadVSAvoidtherapeutic efficacy

Core Design Contradiction:

Quantity of substanceVSReliability

Solution Approach 1:

The patent creates composite formulations combining lipid-based carriers, co-solvents, and peptides, enabling high drug load while maintaining stability and therapeutic efficacy through synergistic interactions

Inventive Principle:

Principle #40Composite materials

Solution Approach 2:

The patent changes formulation parameters such as concentration, solubility, and carrier properties to maximize drug load while ensuring reliable therapeutic effect

Inventive Principle:

Principle #35Parameter changes

4Productivity

If conventional formulations are used, then initial peptide release is achieved, but burst/lag profile causes concentration spikes and requires frequent dosing

Engineering Contradiction:

Improverelease rateVSAvoidduration of therapeutic effect

Core Design Contradiction:

ProductivityVSDuration of action of moving object

Solution Approach 1:

The patent utilizes phase transition properties of lipid-based carriers and co-solvent systems to control the release kinetics, transforming from initial rapid release to sustained prolonged release

Inventive Principle:

Principle #36Phase transitions

Solution Approach 2:

The patent creates a dynamic release system where the formulation adapts its release characteristics over time, transitioning from initial burst to sustained release profile to maintain therapeutic levels

Inventive Principle:

Principle #15Dynamics

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 formulation achieves a highly advantageous release profile with minimal irritation, allows for high bioactive agent loading, and can be administered through a narrow needle, providing sustained therapeutic levels with reduced frequency of administration.

Implementation Method 1

which undergo phase transition upon exposure to aqueous fluids, such as body fluids, thereby forming a controlled release composition

Methodology Applied

Scientific EffectPhase transition: Phase Change

Implementation Method 2

forms a non-lamellar liquid crystalline phase upon contact with aqueous fluids

Methodology Applied

Scientific EffectLiquid crystalline phase formation: Liquid Crystals

Data Source

PatentUS20250121035A1Controlled release peptide formulations

Publication Date: 2025.04.17 CAMURUS AB

AI summary

The present invention relates to compositions forming a low viscosity mixture of:a) 20-80 wt. % of at least one diacyl glycerol and/or a tocopherol;b) 20-80 wt. % of at least one phosphatidyl choline (PC);c) 5-20 wt. % of at least one biocompatible, organic mono-alcoholic solvent;d) up to 20 wt. % polar solvente) at least one peptide active agent;f) optionally at least one antioxidant;wherein the ratio of components a:b is in the range 40:60 to 54:46;wherein the pre-formulation forms, or is capable of forming, at least one liquid crystalline phase structure upon contact with excess aqueous fluid.The invention further relates to methods of treatment comprising administration of such compositions, and to pre-filled administration devices and kits containing the formulations.