Microneedle array comprising a heat-producing element
Inventors
RONNANDER, James Paul • Koch, Andreas
Assignees
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Publication Number
US-12208228-B2
Publication Date
2025-01-28
Expiration Date
Abstract
The invention relates to a microneedle array having a heat-generating element and its use for the intradermal application of active ingredients, particularly active pharmaceutical ingredients (API) and drugs, wherein this microneedle array is suitable for skin penetration on humans or animals and the microneedles consist of a water-soluble formulation, which contains at least one active ingredient.
Core Innovation
The invention relates to a microneedle array for intradermal application comprising a plurality of microneedles on a carrier, where the microneedle array has at least one heat-generating element. The microneedles contain a substantially water-soluble formulation and at least one water-soluble polymer, and the water-soluble polymer contains at least one active ingredient. The at least one heat-generating element is a latent heat store, and the heat of the at least one heat-generating element can be held for up to 6 hours.
The background problem addressed is that insufficient dwell time and skin-type dependent dissolution lead to a lag time between administration and dissolution of the water-soluble microneedle formulation, which in turn limits the release rate of the active ingredient. The objective described is to reduce lag time and increase release rate of active pharmaceutical ingredients by accelerating microneedle dissolution.
The heat-generating element is described as a latent heat store, with heat generation options that include latent heat stores based on chemical oxidation or crystallization heat, and implementations in which heat can be generated via recrystallization from a supersaturated solution. Example implementations also include heat generation in which latent heat is released, and the resulting heating is associated with in situ dissolution and resorption of penetrated microneedles, thereby shortening lag time and increasing release of the active ingredient.
Claims Coverage
The document provides one independent claim (microneedle array) that recites a latent heat store heat-generating element capable of holding heat for up to 6 hours, together with microneedles containing a substantially water-soluble formulation and a water-soluble polymer with an active ingredient for intradermal use. Additional dependent claims further specify main inventive refinements such as placement of the formulation (tip and/or coating), latent heat generation mechanism via recrystallization and chemical or physicochemical processes, heating temperature range, and heat-driven in situ dissolution/resorption.
Latent heat-store microneedle array for intradermal application
A microneedle array for use in intradermal application comprising a plurality of microneedles on a carrier, wherein the microneedle array has at least one heat-generating element; the microneedles contain a substantially water-soluble formulation and at least one water-soluble polymer which contain at least one active ingredient; the at least one heat generating element is a latent heat store; and the heat of the at least one heat-generating element can be held for up to 6 hours.
Water-soluble formulation in microneedle tip and/or coating
A microneedle array for intradermal application in which a water-soluble formulation containing at least one active ingredient is located in the microneedle tip and/or included as part of a coating.
Heat generation after recrystallization from a supersaturated solution
A microneedle array for intradermal application in which the microneedle array is configured to generate heat after recrystallization from a supersaturated solution via either a chemical oxidation reaction or physicochemical processes.
Latent-heat generation via chemical oxidation or crystallization heat
A microneedle array for intradermal application in which heat is generated after recrystallization from a supersaturated solution by either chemical oxidation using atmospheric oxygen with pyrophoric iron on activated carbon in the presence of water, or by physicochemical processes releasing crystallization heat.
Heat-holding temperature range for the heat-generating element
A microneedle array for intradermal use where the heat of a heat-generating element is 42–50 degrees Celsius.
Heat-driven in situ dissolution and resorption
A microneedle array for intradermal application in which the penetrated microneedles are at least partially dissolved and resorbed in situ due to heat.
Overall, the claim coverage centers on intradermal microneedles carrying a substantially water-soluble formulation with a water-soluble polymer containing an active ingredient, combined with a latent heat store heat-generating element that can hold heat for up to 6 hours. Dependent claims then specify formulation placement (tip/coating), latent heat generation pathways (recrystallization from a supersaturated solution via chemical oxidation or physicochemical crystallization heat), a specified heat temperature range, and heat-associated in situ dissolution and resorption of penetrated microneedles.
Stated Advantages
Reduce lag time between administration and dissolution.
Increase release rate of the active ingredient.
Documented Applications
Intradermal application for delivery of active pharmaceutical ingredients using microneedle arrays having water-soluble formulations and latent heat generation to accelerate dissolution.
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