pH-sensitive hydrogel technology for enhanced oral delivery of high molecular weight therapeutic proteins

This invention describes a pH-sensitive hydrogel for oral delivery of therapeutic proteins like factor VIII or IX, used in hemophilia treatment. It protects proteins in the stomach and releases them in the intestine, enhancing bioavailability.

Background

Delivering therapeutic proteins orally presents significant challenges due to the body's natural mechanisms for breaking down proteins in the digestive tract. Proteins must maintain their structure and functionality through the acidic environment of the stomach and the neutral pH of the small intestine, all while avoiding degradation by digestive enzymes. Traditional delivery methods, such as injections, are invasive and can lead to patient non-compliance due to discomfort and inconvenience.

Although there have been efforts to develop pH-responsive hydrogels for oral delivery, these systems often suffer from low bioavailability, especially for high molecular weight proteins such as factor VIII and IX used in hemophilia treatment. The need for a more effective oral delivery system that protects therapeutic proteins from degradation and enhances their absorption remains a critical challenge in pharmaceutical development.

Technology description

The technology is a composition for the oral delivery of therapeutic proteins, specifically high molecular weight proteins like factor VIII or factor IX, which are crucial in treating hemophilia. This composition utilizes a pH-sensitive crosslinked copolymer made from methacrylic acid and poly (ethylene glycol) monomethyl ether methacrylate. The copolymer is crosslinked with agents like tetra (ethylene glycol) Di methacrylate, forming a hydrogel network that responds to pH changes.

This network remains stable in the acidic stomach environment and swells in the neutral pH of the small intestine, facilitating the release and absorption of the therapeutic protein. The copolymer's structure protects the protein during transit through the digestive system, enhancing its bioavailability when administered orally, potentially reducing the need for injections.

This technology is differentiated by its ability to deliver high molecular weight therapeutic proteins orally, overcoming the traditional barriers of protein degradation in the gastrointestinal tract. The pH-sensitive hydrogel network is a key innovation, allowing the composition to remain stable in the stomach and release the protein in the small intestine. This targeted release mechanism ensures that the therapeutic proteins are absorbed effectively, which is a significant advancement over previous methods that required injections. The technology offers a more convenient and less invasive treatment option for patients, improving compliance and quality of life while reducing healthcare costs associated with injectable therapies. The use of this copolymer composition represents a significant step forward in the oral delivery of protein-based therapeutics.

Benefits

Enhances bioavailability of high molecular weight proteins like factor VIII or IX
Enables oral delivery of therapeutic proteins, reducing the need for injections
Protects proteins during transit through the digestive system
pH-Sensitive hydrogel network allows targeted release in the small intestine
Potentially improves patient quality of life and reduces treatment costs
Offers a more convenient and less painful administration method compared to injections
May reduce systemic side effects due to high specificity of protein therapeutics