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Publication Number
US-12605345-B2
Publication Date
2026-04-21
Expiration Date
Abstract
The present invention relates to transdermal delivery systems, methods and kits that include an agent to penetrate the basement membrane, a membrane of the skin previously known to be difficult to penetrate. In particular, the formulation includes a basement membrane disruptor that reversibly denatures the basement membrane of the skin. The formulation of the present invention further includes having at least one penetration agent, at least one vaso-modulator, and at least one active ingredient. In an embodiment, the penetration agent includes a solvent, a lipophilic agent, a hydrophilic agent, wherein the basement membrane disruptor, the vaso-modulator, and the active ingredient pass through the stratum corneum and epidermis. The basement membrane disruptor allows the vaso-modulator and the active ingredient pass through the basement membrane to dermis. The active ingredient, once at the dermis, is delivered locally to the tissue or systemically to the blood stream.
Core Innovation
The invention provides a transdermal delivery formulation for delivering at least one active ingredient to a mammal having a body surface. The formulation comprises at least one penetration agent, at least one basement membrane disruptor, at least one vaso-modulator, and at least one active ingredient, and allows penetration of the active ingredient to a dermis layer of the body surface.
The basement membrane disruptor disrupts skin basement membrane permeability by reversibly denaturing skin basement membrane proteins, thereby permitting passage of the active ingredient. The formulation denatures basement membrane molecules to permit passage and allows basement membrane molecules to renature after delivery of the active ingredient to the dermis.
The vaso-modulator is included to create dermal fluid-dynamic effects intended to move the active ingredient into local tissue or systemic circulation. The formulation can be applied in a topical/transdermal manner, including single-step or sequential/co-administered application, and can include optional occlusive or transpiration barriers; the document also describes kits and systems that create the formulation and embodiments such as patch components.
Claims Coverage
The independent claims include four inventive areas and are built around four component categories: penetration agent, basement membrane disruptor, vaso-modulator, and active ingredient, with an outcome that penetration occurs to a dermis layer.
Transdermal formulation with penetration agent, basement membrane disruptor, vaso-modulator, and active ingredient
A formulation for transdermal delivery of an active ingredient to a mammal having a body surface, comprising at least one penetration agent, at least one basement membrane disruptor, at least one vaso-modulator, and at least one active ingredient.
Applying formulation to enable dermis penetration
A method for transdermal delivery of a formulation having an active ingredient to a mammal having a body surface, comprising applying the formulation to the body surface, wherein the formulation comprises at least one penetration agent, at least one basement membrane disruptor, at least one vaso-modulator, and at least one active ingredient, and allows for penetration of the active ingredient to a dermis layer of the body surface.
Administering penetration agent, basement membrane disruptor, vaso-modulator, and active ingredient to enable dermis penetration
A method for transdermal delivery of a formulation having an active ingredient to a mammal, comprising administering at least one penetration agent, at least one basement membrane disruptor, at least one vaso-modulator, and at least one active ingredient to the body surface, wherein the formulation allows for penetration of the active ingredient to the dermis.
Kit for transdermal delivery that creates a formulation for dermis penetration
A kit for transdermal delivery of an active ingredient to a mammal having a body surface, comprising at least one penetration agent, at least one basement membrane disruptor, at least one vaso-modulator, and at least one active ingredient, wherein the kit creates a formulation that allows for penetration of the active ingredient to a dermis layer of the body surface.
The independent claim set consistently centers on compositions and delivery approaches that combine penetration agent, basement membrane disruptor, and vaso-modulator with an active ingredient, with a claimed outcome of penetration into a dermis layer.
Stated Advantages
Expanded variety of transdermally deliverable agents, including higher molecular weight and lower logP.
Avoidance of oral side effects.
Documented Applications
Transdermal delivery of an active ingredient to a mammal to enable penetration of the active ingredient into the dermis layer of a body surface.
Delivery system embodiments such as patch components, optionally with microneedles, sonophoresis, or iontophoresis [procedural detail omitted for safety].
Use as a kit or system including the components to create the formulation; optionally includes written instructions for use by or on a mammal.
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