Pharmaceutical preparation
Inventors
Tsukada, Yusuke • Tsujimoto, Hiroyuki • Sakaguchi, Makoto
Assignees
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Publication Number
US-7897751-B2
Publication Date
2011-03-01
Expiration Date
Abstract
A pharmaceutical preparation comprises nano-level particles (nanospheres) of a biocompatible polymer having, as held on their surfaces, an NFκB decoy capable of binding to NFκB to inhibit its activity. With penetration of the nanoparticles inside cells, the NFκB decoy may be delivered to an affected site and the NFκB decoy may be released from the surfaces of the nanoparticles and may be thereby efficiently and specifically introduced into the affected site.
Core Innovation
The invention provides a pharmaceutical preparation containing biocompatible polymer nanoparticles that are coated with a cationic polymer on their surfaces, and an NFbaB decoy oligonucleotide absorbed and held thereon. The NFbaB decoy oligonucleotide is further included inside the nanoparticles, so the preparation includes both surface-absorbed/held decoy and internal decoy within the same nanoparticle carrier.
In disclosed embodiments, the NFbaB decoy comprises an NFbaB binding consensus sequence and binding-sequence variants, including double-stranded decoys. The polymer carrier is described using biocompatible polymers such as PLGA, with optional additional decoy incorporation inside the particles and optional inclusion of the decoy within an outer binder layer.
The disclosed carrier design is presented as improving delivery for skin disease treatment by providing a quick-acting effect from the surface-held NFbaB decoy and a more sustained component from the decoy included inside the particles.
Claims Coverage
The claim set centers on biocompatible polymer nanoparticles coated with a cationic polymer and carrying an NFbaB decoy oligonucleotide on the surface and inside the nanoparticles. Independent coverage identifies 3 core inventive features, with dependent refinements on sequence content, loading, size, and therapeutic use.
Biocompatible polymer nanoparticles with surface cationic polymer coating and NFbaB decoy held thereon
Biocompatible polymer nanoparticles are coated with a cationic polymer on their surfaces, and have an NFbaB decoy oligonucleotide absorbed and held thereon.
NFbaB decoy oligonucleotide further included inside the nanoparticles
The NFbaB decoy oligonucleotide is further included inside the nanoparticles in addition to being absorbed and held on the surfaces.
NFbaB binding sequence among SEQ ID NOs: 1 to 4
The NFbaB decoy oligonucleotide includes an NFbaB binding consensus sequence and variants, including SEQ ID NO: 1 and the sequences of SEQ ID NOs: 2 to 4.
Overall, the claim coverage is directed to a nanoparticle carrier that combines surface-holding and internal inclusion of an NFbaB decoy oligonucleotide, with dependent features on specific sequences, loading, particle size, and use for atopic dermatitis.
Stated Advantages
Provides quick-acting potency for skin disease treatment from surface-holding NFbaB-decoy PLGA nanospheres.
Provides sustained effect by gradual release from the interior for longer-lasting delivery.
Improves efficacy for NFbaB-decoy PLGA nanospheres versus decoy-including-only or mixed/decoy-powder controls in an in vivo OVA-induced DTH model.
Documented Applications
Treatment of skin diseases, specifically atopic dermatitis, using NFbaB decoy-containing nanoparticle pharmaceutical preparations.
Use in an ovalbumin (OVA)-induced delayed-type hypersensitivity (DTH) model showing enhanced efficacy for surface-holding NFbaB-decoy PLGA nanospheres.
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