Trans-epithelial membrane drug delivery system
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Publication Number
US-12246098-B2
Publication Date
2025-03-11
Expiration Date
Abstract
The present invention relates to trans-epithelial membrane delivery systems, methods and kits that include an agent to penetrate the basement membrane, a membrane of the skin and mucosa previously known to be difficult to penetrate. In particular, the formulation includes a basement membrane disruptor that reversibly denatures or cleaves molecules of the basement membrane of the epithelial membrane. 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 outer layers of the epithelial membrane. The basement membrane disruptor allows the vaso-modulator and the active ingredient pass through the basement membrane to smooth muscle. The active ingredient, once at the smooth muscle, is delivered locally to the tissue or systemically to the blood stream.
Core Innovation
The invention relates to a trans-epithelial membrane delivery formulation and a kit for transdermal delivery of an active ingredient to a mammal. The formulation includes at least one first penetration agent, at least one basement membrane disruptor, and at least one vaso-modulator, together with at least one active ingredient. The formulation has a pH between about 5.0 and about 6.5 and is configured to allow penetration of the active ingredient past the basement membrane.
The formulation uses a combination of penetration agents, including mucolytic agents and specified penetration agent options, together with basement membrane disruptors that act as reversible denaturation and/or cleavage agents for basement membrane molecules. Basement membrane disruptors include specified protease classes and other enzyme-related disruptors, and are used to disrupt the basement membrane to permit passage of the active ingredient past the basement membrane.
To support trans-epithelial delivery, the formulation also includes a vaso-modulator selected from vasodilators or vasoconstrictors, present in a specified amount range, in combination with the penetration agents and basement membrane disruptor. The described delivery outcome includes penetration of the active ingredient past the basement membrane and, in a transdermal kit context, penetration to smooth muscle while maintaining the formulation pH between about 5.0 and about 6.5.
Claims Coverage
The independent claim coverage comprises 2 independent claims, focused on a trans-epithelial formulation and a corresponding transdermal delivery kit. Each independent claim defines inventive features centered on the combination of a specified penetration agent, a specified basement membrane disruptor, and a specified vaso-modulator at defined amount ranges together with a pH range enabling penetration past the basement membrane.
Trans-epithelial formulation with penetration agents, basement membrane disruptor, vaso-modulator and pH 5.0-6.5
A formulation for trans-epithelial membrane delivery of an active ingredient to a mammal comprising: at least one first penetration agent in an amount ranging from 0.01% w/w to 2.0% w/w; at least one basement membrane disruptor in an amount ranging from 0.2% w/w to 10% w/w; at least one vaso-modulator in an amount ranging from 0.001% w/w to 15% w/w; and at least one active ingredient, wherein the formulation has a pH between about 5.0 and about 6.5 and allows penetration of the active ingredient past the basement membrane.
Transdermal delivery kit to smooth muscle using penetration agents, basement membrane disruptor, vaso-modulator and pH 5.0-6.5
A kit for transdermal delivery of an active ingredient to a mammal comprising: at least one first penetration agent in an amount ranging from 0.01% w/w to 2.0% w/w; at least one basement membrane disruptor in an amount ranging from 0.2% w/w to 10% w/w; at least one vaso-modulator in an amount ranging from 0.001% w/w to 15% w/w; and at least one active ingredient, wherein the kit creates a formulation that allows for penetration of the active ingredient to a smooth muscle and wherein the formulation has a pH between about 5.0 and about 6.5 and allows for penetration of the active ingredient past the basement membrane.
Across both independent claims, the core inventive concept is a trans-epithelial/transdermal delivery composition that combines a specified first penetration agent, a specified basement membrane disruptor, and a specified vaso-modulator, together with an active ingredient, while maintaining formulation pH between about 5.0 and about 6.5 to enable penetration past the basement membrane and, in the kit claim, to smooth muscle.
Stated Advantages
Allows penetration of the active ingredient past the basement membrane.
For the transdermal kit, allows penetration of the active ingredient to smooth muscle.
Documented Applications
A Franz cell study showing substantially increased CBD penetration through EpiOral™ buccal tissue when using trypsin or pancreatin versus controls without enzymes or a commercial product.
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