Enteric coating for targeting the duodenum
Inventors
Kam, Kimberly • Sheridan, Martin • DiCiccio, Angela
Assignees
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Publication Number
US-12350380-B1
Publication Date
2025-07-08
Expiration Date
Abstract
A system for targeted delivery of a medicament to the gastrointestinal tract (e.g., selectively to the duodenum) of a subject. The system includes a medicament, a mucoadhesive layer at least partially surrounding the medicament, and an enteric coating encasing the medicament and mucoadhesive layer. The enteric coating comprises a material degradable by a pH of the GI tract and a material digestible by a lipase. Also provided are method of making and using the system for targeted delivery of a medicament to the gastrointestinal tract. Also provided are a system for deploying a medicament-containing needle system using an expanding element. The system includes a medicament-containing needle system and an expanding element within a capsule. The capsule is initially coated with an enteric coating. As the enteric coating degrades the expanding element absorbs fluid that enters the capsule and expands to deploy the medicament-containing needle system from the capsule.
Core Innovation
The disclosed invention provides a system for targeted delivery of a medicament to a gastrointestinal (GI) tract of a subject, in which the medicament comprises biotherapeutics and/or nucleic acids. The medicament is surrounded by a mucoadhesive layer coated onto the medicament and comprising one of pectin, sodium caboxymethyl cellulose, or carbopol, and the system further includes an enteric coating encasing the medicament and the mucoadhesive layer.
The enteric coating comprises a first layer comprising a polymer degradable by a pH of the GI tract and a second layer comprising a wax material digestible by a lipase. The polymer of the first layer is selected from polylactic acid, nylon, polyester, and polyvinyl alcohol, and the wax of the second layer comprises one of coconut oil or bees wax.
A second disclosed aspect includes a duodenum-targeted capsule system in which the capsule at least partially encases a medicament needle system and includes a mucoadhesive layer surrounding the medicament needle system. The capsule enteric coating encases the mucoadhesive layer and includes the pH-degradable first layer adjacent the mucoadhesive layer and the lipase-digestible wax outer layer.
The system also includes an expanding element expandable in response to absorbing fluid for driving the medicament and the medicament needle system out of the capsule. Capsule openings are at least partially sealed by the enteric coating, where fluid entry degrades or activates the enteric coating and enables expansion-driven deployment.
Claims Coverage
The provided independent claims are clm-00001 and clm-00011. Across these independent claims, the inventive features cover four main features: a mucoadhesive layer formulation around a medicament, an enteric coating defined by a pH-degradable polymer first layer and a lipase-digestible wax second outer layer, a rapid duodenum dissolution behavior, and a duodenum-targeted capsule implementation with a medicament needle system and an expanding element responsive to absorbed fluid.
Duodenum-targeted mucoadhesive medicament system with rapid enteric dissolution
A system for targeted delivery of a medicament to a gastrointestinal (GI) tract, comprising a medicament comprising biotherapeutics and/or nucleic acids; a mucoadhesive layer surrounding the medicament and comprising one of pectin, sodium caboxymethyl cellulose, or carbopol; and an enteric coating encasing the medicament and mucoadhesive layer.
pH-degradable first layer adjacent mucoadhesive layer plus lipase-digestible wax outer layer
The enteric coating comprises a first layer comprising a polymer degradable by a pH of the GI tract, adjacent the mucoadhesive layer, with the polymer selected from polylactic acid, nylon, polyester, and polyvinyl alcohol, and a second layer comprising a wax material digestible by a lipase as an outer layer, wherein the wax material comprises one of coconut oil or bees wax.
Enteric coating dissolves in less than one minute in human duodenum at defined dissolution rate
The enteric coating dissolves in less than one minute in a human duodenum at a dissolution rate from 5 (mg/cm3)/min to 26 (mg/cm3)/min.
Medicament needle system in capsule with expanding element to drive medicament out
A system for targeted delivery of a medicament to a GI tract comprising a medicament comprising biotherapeutics and/or nucleic acids; a medicament needle system for delivering the medicament to the GI tract; a capsule at least partially encasing the medicament needle system and comprising a mucoadhesive layer surrounding the medicament needle system and an enteric coating encasing the mucoadhesive layer; and an expanding element expandable in response to absorbing fluid for driving the medicament and medicament needle system out of the capsule.
Capsule enteric coating with pH-degradable polymer layer and lipase-digestible wax outer layer plus rapid duodenum degradation
The capsule enteric coating comprises a first layer comprising a polymer degradable by a pH of the GI tract, adjacent the mucoadhesive layer, selected from polylactic acid, nylon, polyester, or polyvinyl alcohol, and a second layer comprising a wax material digestible by a lipase as an outer layer, wherein the wax material comprises one of coconut oil or bees wax; wherein the enteric coating degrades in less than one minute in a human duodenum at a dissolution rate from 5 (mg/cm3)/min to 26 (mg/cm3)/min.
Overall, the independent claims define targeted GI delivery using a medicament surrounded by a mucoadhesive layer and an enteric coating having a pH-degradable polymer first layer and a lipase-digestible wax outer layer, with rapid duodenum dissolution or degradation specified by time and dissolution-rate metrics. The second independent claim additionally recites a medicament needle system within a capsule and an expanding element responsive to absorbing fluid to drive the medicament and needle system out of the capsule.
Stated Advantages
Fast enteric coating dissolution or degradation in less than one minute in a human duodenum at a dissolution rate from 5 (mg/cm3)/min to 26 (mg/cm3)/min.
Targeted delivery to a gastrointestinal (GI) tract, including duodenum-targeted behavior.
Exposure and/or attachment of the mucoadhesive layer and medicament at the duodenal wall as a functional outcome linked to rapid enteric degradation.
Deployment of a medicament needle system from a capsule driven by an expanding element expandable in response to absorbing fluid.
Documented Applications
Targeted delivery of medicament comprising biotherapeutics and/or nucleic acids to a subject’s gastrointestinal (GI) tract, including duodenum-targeted delivery using a capsule system and rapid duodenum enteric degradation.
Local delivery of medicament to the GI tract using a medicament needle system deployed from within a capsule via an expanding element responsive to absorbed fluid.
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