Controlled release formulations
Inventors
Maggio, Edward T. • Meezan, Elis • Pillion, Dennis J. • Morgan, Sarah L. • Baggott, Joe
Assignees
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Publication Number
US-8470370-B2
Publication Date
2013-06-25
Expiration Date
Abstract
The present invention provides stable, self-assembling, biocompatible and biodegradable hydrogel formulations, into which one or more compounds may be incorporated allowing for delayed release or controlled release of the incorporated compounds as the hydrogel is degraded in the body.
Core Innovation
The invention relates to controlled release formulations using self-assembling biodegradable hydrogels formed from nonionic gelators, specifically alkylglycosides and sucrose esters. The hydrogels entrap therapeutic agents without chemical modification, and release the therapeutic agents via gel degradation. Delayed or controlled release is enabled by selecting gelators with different degradation and sensitivity behavior.
A key aspect is the use of sucrose ester gelators, including combinations of sucrose stearate and sucrose distearate, in hydrogel compositions that include a buffer and a therapeutic agent. The hydrogel is formed by heat treatment of a suspension of the therapeutic agent, the sucrose ester combination, and the buffer at temperatures between 37-45° C. The resulting hydrogel is suitable for transdermal or transmucosal delivery by contacting an epidermal or mucosa layer.
The disclosure further includes bilayer formulations using different gelators to achieve differential release behavior. It describes example therapeutic agents and differentiated release timing based on gelator characteristics, including methotrexate and folic acid. The document also describes therapeutic use cases including rheumatoid arthritis treatment, transdermal delivery, intranasal or pulmonary delivery with increased residency time, and Alzheimer's disease via methylene blue.
Claims Coverage
The relevant independent claim set consists of one independent claim covering a method for transdermal or transmucosal delivery using a hydrogel formed from a therapeutic agent, a specific sucrose ester combination, and a buffer by heat treatment at 37-45° C, with the hydrogel resulting from that formation step.
Transdermal or transmucosal hydrogel delivery using sucrose stearate/sucrose distearate gelator combination
A method for transdermal or transmucosal delivery comprising contacting an epidermal or mucosa layer with a composition comprising a therapeutic agent, a sucrose ester combination of sucrose stearate and sucrose distearate, and a buffer.
Hydrogel formation by heat treatment at 37-45° C
The composition is a hydrogel formed by heat treatment of a suspension of the therapeutic agent, the sucrose ester combination, and the buffer at temperatures between 37-45° C.
Across the identified independent claim, the inventive coverage centers on delivering a therapeutic agent by contacting epidermal or mucosa layers with a hydrogel composition containing a sucrose stearate/sucrose distearate combination gelator and a buffer, where the hydrogel is formed by heat treatment in the stated 37-45° C range.
Stated Advantages
Not explicitly described in patent.
Documented Applications
Rheumatoid arthritis treatment.
Transdermal delivery.
Intranasal delivery.
Pulmonary mucosa delivery including increasing residency time.
Alzheimer's disease via methylene blue.
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