Temperature-dependent Activation of Catalytic Nucleic Acids for Controlled Active Substance Release

Simple SummaryContent extracted from patent full text and abstract with AI.

This invention discloses a temperature-triggered drug delivery system using catalytically active nucleic acids (like ribozymes or DNAzymes) attached to nanoparticles. In its inactive state, the catalytic nucleic acid is hybridized to an inhibitor strand on a nanoparticle. Upon mild heating—achievable by exposing the magnetic nanoparticles to an external alternating magnetic field—the inhibitor releases the nucleic acid, which then specifically cleaves a substrate molecule attached to a drug-conjugated carrier or nano/microparticle. This cleavage releases the active drug at the targeted site with high specificity and control, mostly in response to local temperature rise.

Use CasesContent extracted from patent full text and abstract with AI.

• Targeted chemotherapy delivery to tumors (particularly solid tumors) via localized heating (e.g., magnetic hyperthermia).
• Localized therapy for bacterial infections by triggering antibacterial agent release at infection sites.
• Controlled release of anti-inflammatory, anti-viral, or neuropharmaceutical agents for chronic disease treatment.
• Pain management through site- and time-specific drug release (such as during acute migraine or post-surgical pain).
• Implant-assisted therapy, where pre-loaded drug carriers are triggered on-demand by heat/external stimulus at a later time.
• Combination treatments with existing cancer therapies (chemotherapy, radiotherapy, hyperthermia) to precisely control drug timing and location.

BenefitsContent extracted from patent full text and abstract with AI.

• Greatly improved control over when and where a drug is released, minimizing side effects to healthy tissue.
• Efficient drug activation at therapeutic concentrations even with small local temperature increases, allowing mild and reversible triggers.
• Versatility in the types of drugs deliverable, from small molecules to biologicals (e.g., RNA, proteins, peptides).
• Reduced risk of premature drug release in circulation because the drug linkage is specifically cleaved by the released nucleic acid catalyst.
• Can be tailored for different temperature triggers and drug types by engineering the nucleic acid and inhibitors.
• Enhances compatibility with imaging modalities (e.g., MRI) due to nanoparticle properties, enabling theranostic applications (therapy + diagnostics).
• Potential for repeated, on-demand treatments with a single implant or depot, reducing the need for frequent dosing.

Technical Classifications (CPCs)

Inventors & Applicants

Patent Abstract

The present invention relates to an active substance release system containing two compounds. The first compound comprises a nanoparticle, combined with an oligonucleotide inhibition strand that is hybridized with a catalytically active nucleic acid. The second compound comprises a carrier, combined with a substrate molecule that is coupled to a therapeutic active substance. By means of external stimulation, the catalytically active nucleic acid of the first compound is released and specifically binds to the substrate molecule of the second compound. This leads to cleavage of the substrate molecule, whereby the active substance bound thereto is released.