Microprojection Array for Intradermal Peptide Delivery

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Solution Overview

Problem

PTHrP analogues face challenges in transdermal delivery due to the stratum corneum barrier, particularly for large molecules like peptides, which hinder effective penetration into systemic circulation, and existing delivery methods like subcutaneous injection are inconvenient and may lead to bone loss.

Innovation Solution

A microprojection array with microprojections coated with [Glu22,25, Leu23,28,31, Aib29, Lys26,30]PTHrP(1-34)NH2 and histidine, facilitating intradermal delivery through the skin, allowing for controlled pharmacokinetics and improved bone anabolic effects without bone loss.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If transdermal delivery is attempted for PTHrP analogues, then patient compliance and convenience are improved, but the stratum corneum barrier prevents effective drug penetration into systemic circulation

Engineering Contradiction:

Improvepatient complianceVSAvoiddrug penetration efficiency

Core Design Contradiction:

Ease of operationVSReliability

Solution Approach 1:

The patent uses microprojections as an intermediary device to bridge the stratum corneum barrier. These microprojections physically penetrate the outer skin layer and deliver the PTHrP analogue directly into the intradermal space, bypassing the diffusion barrier while maintaining transdermal application convenience.

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent changes the physical state and delivery parameters by using a coating formulation on microprojections that allows the peptide drug to be deposited and then released upon skin penetration. This transforms the delivery mechanism from passive diffusion to active mechanical penetration with controlled release.

Inventive Principle:

Principle #35Parameter changes

2Ease of operation

If microprojection patches are used for PTHrP delivery, then transdermal delivery is achieved, but complicated therapies result if effective and reproducible coating is not achieved

Engineering Contradiction:

Improvetransdermal delivery capabilityVSAvoidcoating process complexity

Core Design Contradiction:

Ease of operationVSDevice complexity

Solution Approach 1:

The patent applies the coating formulation to the microprojections in advance during manufacturing, creating pre-coated microprojection arrays. This preliminary action ensures that the coating is uniformly distributed and properly adhered before use, eliminating the need for complex coating procedures at the point of administration and ensuring reproducible dosing.

Inventive Principle:

Principle #10Preliminary action

3Reliability

If subcutaneous injection is used for PTHrP delivery, then effective drug delivery is achieved, but patient convenience is reduced and bone loss may occur

Engineering Contradiction:

Improvedrug delivery effectivenessVSAvoidpatient convenience

Core Design Contradiction:

ReliabilityVSEase of operation

Solution Approach 1:

The patent replaces the invasive mechanical system of subcutaneous injection with a non-invasive transdermal microprojection system. The microprojections mechanically penetrate only the epidermis and deliver the drug to the intradermal space, avoiding the need for needle insertion into subcutaneous tissue while maintaining effective drug delivery.

Inventive Principle:

Principle #28Mechanics substitution (Replace mechanical system)

Data Source

PatentEP2699252B1Method of drug delivery for PTH, pthrp and related peptides

Publication Date: 2017.10.25 RADIUS HEALTH INC

AI summary

The present invention provides compositions, devices, methods and processes related to the intradermal delivery of PTHrP and PTHrP analogues, particularly [Glu22,25, Leu23,28,31, Aib29, Lys26,30]hPTHrP(l-34)NH2.