Transdermal drug delivery system
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Publication Number
US-11446257-B2
Publication Date
2022-09-20
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 relates to transdermal delivery of an active ingredient to a mammal in which the body surface comprises a stratum corneum, an epidermis, a basement membrane, and a dermis. Penetration of the active ingredient to the dermis is enabled by using at least one penetration agent, at least one basement membrane disruptor, and at least one vaso-modulator in the formulation.
The penetration agent comprises a solvent, a lipophilic agent, a hydrophilic agent, or a combination thereof, and the basement membrane disruptor reversibly denatures basement membrane molecules to allow passage of the active ingredient. The one or more molecules renature once the active ingredient is delivered to the dermis.
The vaso-modulator comprises a vasodilator or vasoconstrictor to drive delivery so that the active ingredient is delivered either systemically or to local tissue with the vasodilator, or to the dermis with the vasoconstrictor. The invention also encompasses method and kit embodiments for transdermal delivery that include the same coordinated functional components.
Claims Coverage
The independent claims are clm-00001, clm-00016, clm-00017, and clm-00021. Across these independent claims, the document identifies four main inventive feature groups.
Penetration agent for transdermal penetration
The formulation comprises at least one penetration agent comprising a solvent, a lipophilic agent, a hydrophilic agent, or a combination thereof.
Reversibly denaturing basement membrane disruptor
The formulation comprises at least one basement membrane disruptor that reversibly denatures the basement membrane, wherein the basement membrane disruptor is present in an amount ranging from about 0.2% w/w to about 10% w/w.
Vaso-modulator enabling delivery to dermis or systemic/local tissue
The formulation comprises at least one vaso-modulator, wherein the vaso-modulator comprises a vasodilator or vasoconstrictor; wherein the vasodilator allows for the active ingredient to be delivered systemically or to local tissue; and wherein the vasoconstrictor allows for the active ingredient to be delivered to the dermis.
Formulation enables dermal penetration via denature-then-renature basement membrane
The formulation allows for penetration of the active ingredient to the dermis, wherein the basement membrane disruptor denatures one or more molecules of the basement membrane to allow for passage of the active ingredient, and wherein the one or more molecules of the basement membrane renature once the active ingredient is delivered to the dermis.
Transdermal method using penetration agent, reversibly denaturing basement membrane disruptor, and vaso-modulator
The method comprises applying or administering the formulation to the body surface, wherein the formulation comprises at least one penetration agent, at least one basement membrane disruptor that reversibly denatures the basement membrane, at least one vaso-modulator comprising a vasodilator or vasoconstrictor, and at least one active ingredient.
Kit for transdermal delivery with penetration agent, reversibly denaturing basement membrane disruptor, and vaso-modulator
The kit comprises at least one penetration agent, at least one basement membrane disruptor that reversibly denatures the basement membrane, and at least one vaso-modulator comprising a vasodilator or vasoconstrictor, and at least one active ingredient.
Written instructions component in the kit
The kit further comprises a set of written instructions for use, by or on said mammal.
Across the independent claims, the core claim coverage is directed to transdermal delivery in which a formulation or kit combines a penetration agent with a basement membrane disruptor that reversibly denatures basement membrane molecules and later renatures them after delivery to the dermis, together with a vaso-modulator that is either a vasodilator or a vasoconstrictor. The independent method claims cover applying or administering these components, and the kit claim covers providing the components as a kit, with a dependent refinement adding a set of written instructions.
Stated Advantages
Allows penetration of the active ingredient to the dermis.
Enables the basement membrane disruptor to denature basement membrane molecules to allow passage of the active ingredient, followed by renature once the active ingredient is delivered to the dermis.
With a vasodilator, allows the active ingredient to be delivered systemically or to local tissue.
With a vasoconstrictor, allows the active ingredient to be delivered to the dermis.
Documented Applications
Transdermal delivery of an active ingredient to a mammal via a body surface comprising stratum corneum, epidermis, basement membrane, and dermis.
A method for transdermal delivery by applying or administering a formulation to a mammal’s body surface to deliver an active ingredient to the dermis.
A kit for transdermal delivery of an active ingredient to a mammal, including components that create a formulation enabling dermal penetration.
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