Bioerodible implant for long-term drug delivery and associated methods of manufacture and use
Inventors
BAILLIE, John H. • BAILLIE, Ruth • Blouin, George • Farahani, Newsha • MARX, Christopher
Assignees
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Publication Number
US-11185496-B2
Publication Date
2021-11-30
Expiration Date
Abstract
A 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 pharmacologically active agent over an extended time period. As such, the drug delivery system finds significant utility in chronic drug administration. Bioerosion products are water soluble, bioresorbed, or both, obviating the need for surgical removal of the implant. Methods for manufacturing and using the drug delivery system are also provided.
Core Innovation
The invention is a controlled release drug delivery system that includes a subdermally implantable pellet providing controlled release of a pharmacologically active agent throughout an extended drug delivery time period. The pellet is configured so that, following subdermal implantation of at least one pellet into a subject, the resulting serum level of the active agent is sufficient to achieve therapeutic efficacy during the extended drug delivery time period. The pellet is bioerodible in situ, including bioerosion products that are water soluble and/or bioresorbable, such that surgical removal is avoided.
The pellet has an elongated form with a first region comprising a non-polymeric inner core having a length, a surface along the length, a first end, and an opposing second end, and a second region comprising a non-polymeric outer shell enclosing the surface of the inner core along its length while not enclosing the first end or the second end. This structure leaves the inner core with exposed surface area at the first and second ends.
The inner core and the outer shell are comprised of a lipidic excipient composition including a first lipidic excipient and a second lipidic excipient having aqueous solubilities that differ by at least 10%. The amount and distribution of the pharmacologically active agent are arranged so that at least about 80 wt. % of the active agent is present in the core, or alternatively the core and the shell each contain at least about 20 wt. % of the active agent.
The patent also describes an extended release time period characterized by an effective drug delivery time period followed by a reduced sub-effective tail period, and explains that pellet dimensions, excipient aqueous solubility, and exposed surface area tune release rate and duration.
Claims Coverage
The partial content provides one independent claim (clm-00001). It contains a system-level pellet structure and material constraints defining how a subdermally implantable, bioerodible elongated pellet achieves serum therapeutic efficacy over an extended drug delivery time period using a lipidic excipient composition and specified active agent distribution.
Subdermally implantable, bioerodible controlled-release pellet for extended therapeutic serum levels
A controlled release drug delivery system that comprises a subdermally implantable pellet providing controlled release of a pharmacologically active agent throughout an extended drug delivery time period, where the pellet is bioerodible in situ and following subdermal implantation results in a serum level sufficient to achieve therapeutic efficacy during the extended drug delivery time period.
Elongated non-polymeric inner core with non-polymeric outer shell leaving end exposure
A pellet having an elongated form with a first region comprising a non-polymeric inner core (having a length, a surface along the length, a first end, and an opposing second end) and a second region comprising a non-polymeric outer shell enclosing the surface of the inner core along its length but not the first end or the second end such that the inner core has exposed surface area at the first and second ends.
Lipidic excipient composition with differing aqueous solubilities between first and second lipidic excipients
The inner core and outer shell are comprised of a lipidic excipient composition including a first lipidic excipient and a second lipidic excipient having aqueous solubilities that differ by at least 10%.
Active agent distribution in core or in both core and shell
At least about 80 wt. % of the active agent is present in the core, or alternatively the core and the shell each contain at least about 20 wt. % of the active agent.
Overall, the claim coverage is anchored on an elongated, subdermally implantable and bioerodible pellet that delivers a pharmacologically active agent to achieve therapeutic serum levels over an extended drug delivery time period. The inventive structure combines a non-polymeric inner core with an outer non-polymeric shell that leaves the ends exposed, lipidic excipient compositions having lipid aqueous solubility difference of at least 10%, and specified active agent distribution between core and shell.
Stated Advantages
Avoids surgical removal because the pellet is bioerodible in situ and bioerosion products are water soluble and/or bioresorbable.
Documented Applications
Chronic psychiatric delivery.
Antiviral and HIV delivery.
Anti-inflammatory delivery.
Contraception, including male and female hormones.
Oncology delivery.
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