Microneedle Array PVP Formulation for Glucagon-like Peptide Release

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Solution Overview

Problem

The natural impermeability of the skin's Stratum Corneum barrier prevents effective intradermal delivery of pharmaceutical agents, including glucagon-like peptide analogues, and existing microneedle systems have limitations in achieving controlled release for more than 12 hours, particularly with polyvinylpyrrolidone (PVP) formulations.

Innovation Solution

A microneedle system (MNS) incorporating a microneedle array (MNA) with a formulation of polyvinylpyrrolidone (PVP) and glucagon-like peptide analogues, allowing for intradermal application and controlled release of the active substance over an extended period, preferably more than 12 hours, by forming a unit with PVP that penetrates the skin and releases the peptide continuously.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Object-affected harmful factors

If the Stratum Corneum barrier is used to prevent infiltration of foreign substances, then protection of the body is improved, but administration of pharmaceutical agents through the skin is prevented

Engineering Contradiction:

Improveprotection of the bodyVSAvoidadministration of pharmaceutical agents

Core Design Contradiction:

Object-affected harmful factorsVSEase of manufacture

Solution Approach 1:

The microneedle array divides the skin penetration task into multiple small needles that collectively penetrate the Stratum Corneum barrier, allowing pharmaceutical agents to be delivered intradermally while maintaining the barrier's protective function in non-penetrated areas

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

The microneedles act as intermediary elements that bridge the gap between the pharmaceutical agent and the skin barrier, enabling controlled penetration through the Stratum Corneum without compromising the overall protective function of the skin

Inventive Principle:

Principle #24Intermediary (Mediator)

2Ease of manufacture

If microneedle systems are used for intradermal application, then delivery of pharmaceutical agents is improved, but controlled release for more than 12 hours is not achieved

Engineering Contradiction:

Improvedelivery of pharmaceutical agentsVSAvoidcontrolled release duration

Core Design Contradiction:

Ease of manufactureVSDuration of action of moving object

Solution Approach 1:

The patent changes the formulation parameters by using polyvinylpyrrolidone (PVP) with specific molecular weights and concentrations, adjusting the microneedle composition to enable controlled release of glucagon-like peptide analogues for more than 12 hours, extending the duration of action

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The microneedle array uses composite materials combining PVP polymer with glucagon-like peptide analogues, creating a formulation that provides both delivery capability and extended controlled release, achieving therapeutic effect for more than 12 hours

Inventive Principle:

Principle #40Composite materials

3Duration of action of moving object

If polyvinylpyrrolidone (PVP) is used in microneedle formulation, then controlled release is improved, but formulation stability and skin penetration are compromised

Engineering Contradiction:

Improvecontrolled releaseVSAvoidformulation stability and skin penetration

Core Design Contradiction:

Duration of action of moving objectVSReliability

Solution Approach 1:

The patent optimizes PVP parameters including molecular weight, concentration, and formulation composition to achieve the right balance between controlled release capability and formulation stability, ensuring reliable skin penetration while maintaining extended release

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The PVP formulation is designed with local quality variations, creating zones within the microneedle structure that favor different functions: some areas optimized for skin penetration while others provide controlled release, ensuring both reliability and extended duration

Inventive Principle:

Principle #3Local quality

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

Enables a prolonged controlled release of glucagon-like peptide analogues, such as exenatide, for up to 24 hours, facilitating a one-time daily dose application for conditions like diabetes, insulin resistance, and metabolic syndrome, with improved bioavailability and skin penetration.

Implementation Method 1

Microneedle systems (MNS), which consist of a microneedle array (MNA) and optionally further components, may press the microneedles (also referred to as the main penetration elements) of the array (MNA) against the application point on the skin by means of a compressive force so as to penetrate the Stratum Corneum

Methodology Applied

Scientific EffectMechanical penetration: Mechanical Force

Implementation Method 2

The GLP-1 analogues developed until now act, in part, more strongly than the endogenous GLP-1 and are used as antidiabetics... The half-life period is usually more than 12 hours

Methodology Applied

Scientific EffectDiffusion: Diffusion

Implementation Method 3

U.S. Pat. No. 9,320,878 B2 describes a controlled release of exenatide (claim 4) by means of an MNS based on polyvinyl alcohols (PVA)... PVP, however, is preferred over PVA for influencing the release of active substances

Methodology Applied

Scientific EffectPolymer degradation: Decomposition (biological)

Data Source

PatentUS20240139098A1Microneedle system for applying glucagon-like peptide analogues

Publication Date: 2024.05.02 LTS LOHMANN THERAPIE SYST AG

AI summary

The present invention relates to a microneedle system (MNS) for intradermal application in a controlled release of glucagon-like peptide analogues.