Bioerodible contraceptive implant and methods of use thereof
Inventors
BAILLIE, John H. • BAILLIE, Ruth • Blouin, George • Farahani, Newsha • MARX, Christopher
Assignees
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Publication Number
US-9980850-B2
Publication Date
2018-05-29
Expiration Date
Abstract
A contraceptive drug delivery system is provided in the form of a controlled release, bioerodible pellet for subdermal implantation. The pellet is bioerodible, and provides for the sustained release of a contraceptive agent over an extended time period. Bioerosion products are water soluble, bioresorbed, or both, obviating the need for surgical removal of the implant. Methods of using the drug delivery system, including in female contraception, are also provided.
Core Innovation
The invention relates to a drug delivery system for use in female contraception. The system includes a subdermally implantable pellet that provides controlled release of a contraceptive agent throughout an extended drug delivery time period and produces a serum level sufficient to achieve contraceptive efficacy during that period while being bioerodible in situ.
The pellet is elongated and includes a first region comprising an inner core and a second region comprising an outer shell. The outer shell encloses the surface of the inner core along its length but not the first end or the second end, so that the inner core has exposed surface area at the first and second ends.
The contraceptive agent is distributed between the core and the shell under quantitative constraints, including at least about 80 wt. % in the core, at least about 80 wt. % in the shell, or at least about 20 wt. % in each of the core and the shell. The document also describes design criteria tying release behavior to exposed surface area and pharmacokinetics such as plasma progestin levels and AUC, and it characterizes a reduced tail period by tuning pellet geometry, drug distribution, and bioresorbable excipients.
The system is directed to sustaining release of progestogen or progestogen plus estrogen to maintain serum levels sufficient for contraceptive efficacy. The document also describes optional radio-opacity and mentions female hormone replacement therapy as an additional use case.
Claims Coverage
The claim set includes one independent claim defining the core structural and functional elements of the subdermally implantable pellet system for female contraception, with additional dependent claims refining the release profile, contraceptive agent composition, and material or processing-related constraints.
Subdermally implantable pellet providing controlled release for female contraception
A drug delivery system for use in female contraception, comprising a subdermally implantable pellet that provides controlled release of a contraceptive agent throughout an extended drug delivery time period and results in a serum level sufficient to achieve contraceptive efficacy during the extended drug delivery time period, wherein the pellet is bioerodible in situ.
Elongated core-and-shell pellet with exposed end surfaces
An elongated pellet having a first region with an inner core and a second region with an outer shell, where the outer shell encloses the surface of the inner core along its length but not the first end or the second end, so that the inner core has exposed surface area at the first and second ends.
Quantitative contraceptive-agent distribution between core and shell
A distribution of the contraceptive agent such that at least about 80 wt. % is present in the core or at least about 80 wt. % is present in the shell, or the core and the shell each contain at least about 20 wt. % of the contraceptive agent.
Overall, the independent claim coverage centers on a bioerodible, subdermal, elongated core-and-shell pellet configured to achieve contraceptive serum efficacy over an extended time period while enforcing end-exposed core geometry and quantitative placement of the contraceptive agent across core and shell.
Stated Advantages
Achieves contraceptive efficacy during an extended drug delivery time period by providing a serum level of the contraceptive agent following subdermal implantation.
Reduces a tail period or sub-effective drug delivery period by tuning pellet geometry, drug distribution, and bioresorbable excipients.
Documented Applications
Female contraception using subdermal implantation in a female individual with the described controlled-release contraceptive pellet system.
Female hormone replacement therapy is mentioned as an additional use.
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