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-10493254-B2
Publication Date
2019-12-03
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 provides a method for delivering a permeant through a biological membrane of a subject by forming one or more micropores in the biological membrane and placing a patch in physical contact with the micropores to define a formed pathway for delivery. The patch comprises a matrix containing at least one hydrophilic permeant disposed within the matrix, where at least a portion of the hydrophilic permeant can dissolve in biological moisture received from the subject through the micropores, and at least one permeability enhancer disposed within the matrix.
A further aspect of the invention is the inclusion of at least one solubility control agent disposed within the matrix to control the dissolution of the hydrophilic permeant in the biological moisture received by the matrix, thereby controlling delivery into the subject via the formed pathway. The solubility control agent comprises at least one selected from an agent that selectively controls pH of the biological moisture relative to the isoelectric point of the hydrophilic permeant, an agent that selectively controls the ionic strength of the biological moisture, and a salting-out agent.
The invention addresses delivery of hydrophilic permeants through biological membranes using micropores while controlling dissolution-driven delivery behavior through the formed pathways. By using a patch that maintains the hydrophilic permeant in an undissolved or partially undissolved state within an anhydrous matrix and by tailoring dissolution using solubility control agents, the delivery is described as being modulated to reduce burst/bolus delivery and to extend delivery over a period ranging from minutes to days.
Claims Coverage
The identified independent claim is clm-00001. It contains four core inventive elements that define the method: micropore formation, patch contact with micropores, a matrix with hydrophilic permeant and permeability enhancer, and a solubility control agent system to control permeant dissolution and thereby delivery through the formed pathway.
Forming micropores and contacting with a patch in physical contact
Forming one or more micropores in the biological membrane, and placing a patch in physical contact with said one or more micropores.
Matrix with hydrophilic permeant that can dissolve in biological moisture
Providing the 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.
Permeability enhancer disposed within the matrix
Providing at least one permeability enhancer disposed within the matrix.
Solubility control agent for controlling dissolution and delivery
Providing at least one solubility control agent disposed within the matrix for controlling the dissolution of the hydrophilic permeant in the biological moisture received by the matrix to control delivery of the hydrophilic permeant into the subject via the at least one formed pathway, wherein the at least one solubility control agent comprises at least one selected from an agent that selectively controls pH of the biological moisture relative to the isoelectric point of the hydrophilic permeant, an agent that selectively controls the ionic strength of the biological moisture, and a salting-out agent.
Across the independent claim, claim coverage centers on micropore-mediated transport through a formed pathway using a patch containing a hydrophilic permeant, permeability enhancer, and a solubility control agent that controls dissolution via pH relative to the isoelectric point, ionic strength, and/or salting-out.
Stated Advantages
Improved permeant utilization and/or controlled permeant delivery behavior is described through managing permeant dissolution in the matrix.
Reduction or elimination of burst/bolus delivery effects is described through controlling dissolution of the hydrophilic permeant using the solubility control agent in an anhydrous matrix.
Delivery is described as being extendable or modulated over an administration period ranging from minutes to days.
Potential reduced cold-chain need for protein/vaccine payloads is stated.
Documented Applications
Transdermal or through-skin delivery of a hydrophilic permeant through a biological membrane using micropores and a patch in physical contact.
Delivery of hydrophilic permeants including fentanyl citrate and hydromorphone HCl is described.
Delivery of hydrophilic permeants including insulin and exenatide is described.
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