Permeant delivery system and methods for use thereof
Inventors
Tagliaferri, Frank • Smith, Alan • Enscore, David • Tolia, Gaurav • Baudys, Mirek
Assignees
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Publication Number
US-9498609-B2
Publication Date
2016-11-22
Expiration Date
Abstract
Disclosed are a patch, system, and method for delivery of a permeant composition into a subject via at least one formed pathway through a biological membrane of the subject. The patch comprises a matrix, at least one hydrophilic permeant disposed within the matrix, wherein at least a portion of the permeant can dissolve in biological moisture received from the subject, and at least one permeability enhancer disposed within the matrix. Also disclosed are systems and methods for delivery of a permeant composition into a subject via at least one formed pathway through a skin layer of the subject.
Core Innovation
The invention describes a transdermal patch that delivers a permeant through at least one formed pathway in a biological membrane of a subject. The patch includes a matrix containing at least one hydrophilic permeant that dissolves in biological moisture received from the subject, and the permeant is delivered through micropores or other formed pathways that allow the biological moisture to contact the matrix.
The patch further includes at least one permeability enhancer disposed within the matrix. The permeability enhancer is at least one pH control agent that adjusts the pH of the contacted biological moisture in a selected range comprising an acidic pH range of from 2 to 4 and a basic pH range of from about 8 to 10.
In system embodiments, a porator forms a micropore in the biological membrane and a patch is placed in physical contact with the micropore such that biological moisture received through the micropore dissolves at least a portion of the hydrophilic permeant in the matrix. In method embodiments, one or more micropores are formed in the biological membrane and a patch is placed in physical contact with the micropores, where the patch matrix contains the hydrophilic permeant and the pH control agent permeability enhancer to adjust the contacted biological moisture pH within the acidic or basic ranges.
Claims Coverage
The independent claims are clm-00001, clm-00025, and clm-00052, each centered on delivering a hydrophilic permeant through a formed pathway or micropore in a biological membrane and using a matrix-contained permeability enhancer that is a pH control agent to adjust the contacted biological moisture to either an acidic pH range of 2 to 4 or a basic pH range of about 8 to 10. Across the independent claims, the inventive features focus on the patch formulation and its coupling to the formed pathway or micropore.
Matrix with hydrophilic permeant dissolvable in biological moisture
A patch for delivering a permeant via at least one formed pathway through a biological membrane comprising a matrix and at least one hydrophilic permeant disposed within the matrix, wherein at least a portion of the hydrophilic permeant can dissolve in biological moisture received from the subject.
pH control agent permeability enhancer adjusting contacted biological moisture pH (acidic 2–4 or basic 8–10)
A patch having at least one permeability enhancer disposed within the matrix, wherein the permeability enhancer is at least one pH control agent that adjusts the pH of the contacted biological moisture in a range selected from an acidic pH range of from 2 to 4 and a basic pH range of from 8 to 10.
Porator plus patch where micropore enables dissolution of hydrophilic permeant in contacted biological moisture
A system comprising a porator and a patch wherein the patch comprises a matrix; at least one hydrophilic permeant disposed within the matrix, wherein at least a portion of the hydrophilic permeant can dissolve in biological moisture received from the subject through a micropore formed by the porator.
System permeability enhancer as pH control agent (acidic 2–4 or basic 8–10)
In the system, at least one permeability enhancer disposed within the matrix, wherein the permeability enhancer is at least one pH control agent that adjusts the pH of the contacted biological moisture in a range selected from the acidic pH range of from 2 to 4 and the basic pH range of from about 8 to 10.
Form one or more micropores and contact with patch matrix containing hydrophilic permeant dissolvable in micropore-received moisture
A method comprising forming one or more micropores in the biological membrane; and placing a patch in physical contact with said one or more micropores, wherein said patch comprises a matrix and at least one hydrophilic permeant disposed within the matrix, wherein at least a portion of the hydrophilic permeant can dissolve in biological moisture received from the subject through said one or more micropores.
Method permeability enhancer as pH control agent adjusting contacted biological moisture pH (acidic 2–4 or basic 8–10)
In the method, at least one permeability enhancer disposed within the matrix, wherein the permeability enhancer is at least one pH control agent that adjusts the pH of the contacted biological moisture in a range selected from the acidic pH range of 2 to 4 and the basic pH range of from about 8 to 10.
Across clm-00001, clm-00025, and clm-00052, the claim coverage is focused on a matrix-based patch that contains a hydrophilic permeant dissolvable in contacted biological moisture through formed pathways or micropores, and on a permeability enhancer that is a pH control agent to adjust the contacted biological moisture pH to either an acidic pH range of 2–4 or a basic pH range of about 8–10.
Stated Advantages
Improved permeant utilization.
Elimination of burst effect.
Extended administration over hours-to-days.
Shelf stability due to anhydrous reservoir design.
Documented Applications
Transdermal permeant delivery using a patch through micropores/form pathways in skin layers/stratum corneum.
Pharmacokinetic (PK) evaluation in hairless rat studies for hydromorphone, fentanyl citrate, insulin, and exenatide using patch/permeability-enhancer compositions with pH control agents.
In vitro release studies evaluating permeant release kinetics with different pH control agents and permeability enhancer/polymer compositions.
Pore permeability maintenance screening using EVA films with and without permeability enhancers.
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