University of Kentucky Research Foundation

The University of North Carolina at Chapel Hill

Michael Joseph Jay

Russell John Mumper

James Huckle

Matthew Sadgrove

Anthony J Di Pasqua

U Yun Ryo

G Thomas Kluemper

Xiuling Lu

Sang Hun Kim

The present invention relates to trisodium diethylenetriamine pentaacetic acid (DTPA) prodrugs, such as, for example, DTPA di-ethyl esters. The invention further relates to compositions comprising DTPA prodrugs and methods of using the same.

DTPA prodrugs, compositions thereof, and methods of using the same

A composition and method to alleviate oral mucosal discomfort and irritation in an orthodontic patient. A wax matrix containing less that 15% analgesic/anesthetic agent such as benzocaine and excipients enhanced and extended release of the analgesic/anesthetic agent compared to known art formulations. The composition exhibited desirable aesthetic properties, was easy to apply, and the relatively lower concentration of active agent provided enhanced safety.

Sustained release of topical anesthetics

The present invention provides radiotherapeutic agents and compositions and methods for making and using the same. In some embodiments, the radiotherapeutic agent is a nanoparticle comprising a radionuclide and a carrier moiety. In some embodiments, the radionuclide is produced by activating a stable activatable particle via neutron activation.

Stable activatable particles as radiotherapeutic agents for the treatment of disease

The present invention relates to pH-sensitive mucoadhesive film-forming gels and wax-film composites suitable for topical and mucosal delivery of molecules of interest, namely active pharmaceuticals. The gels comprise a pharmaceutically acceptable pH-sensitive polymer that responds to a lowering of pH by precipitating into films when in contact with the skin or mucosal surface. The films also comprise an adhesive polymer that allows the film to remain in contact with the tissue for an extended period of time. The wax-film composites comprise a bi-layer film having both the said pH-sensitive mucoadhesive layer to promote strong adherence to the skin and mucosal surfaces as well as a specially bonded wax layer intended to extend the adherence of the film to tissues for a prolonged period of time. The invention also relates to the use of said pH-sensitive film-forming gels and wax-film composites to deliver molecules of interest, such as small molecules, peptides, proteins, and nucleic acids either locally to act at the site of administration or for the absorption of said molecules of interest across biological membranes into the systemic circulation.

pH-sensitive mucoadhesive film-forming gels and wax-film composites suitable for topical and mucosal delivery of molecules

A composition for removing a radioactive element or compound such as systemic transuranic compounds, from mammals comprises a pharmaceutical carrier and a decorporation agent comprising ester and amide derivatives of DTPA. A method of treating a mammal to remove systemic compounds utilizing the DTPA derivatives is also disclosed.

Methods and pharmaceutical compositions for decorporation of radioactive compounds

pH-Sensitive mucoadhesive film-forming gels and wax-film composites suitable for topical and mucosal delivery of molecules

The preparation of novel microemulsions to be used as precursors for solid nanoparticles is described. The microemulsion precursors consist of either alcohol-in-fluorocarbon microemulsions, liquid hydrocarbon-in-fluorocarbon microemulsions, or liquid hydrocarbon-in-water microemulsions. The formed solid nanoparticles have diameters below 200 nanometers and can be made to entrap various materials including drugs, magnets, and sensors. The solid nanoparticles can be made to target different cells in the body by the inclusion of a cell-specific targeting ligand. Methods of preparing the novel microemulsion precursors and methods to cure solid nanoparticles are provided.

Microemulsions as precursors to solid nanoparticles

The present invention relates to the use of nanoscintillation systems, or nanoparticles containing fluor molecules, that can be used to detect an electron-emitting or alpha-particle-emitting radioisotope in the absence of organic-solvents commonly used in organic-based liquid scintillation cocktails. The invention also relates to compositions and use of three oil-in-water microemulsion precursors that can be engineered rapidly, reproducibly, and cost-effectively to produce useful nanoparticles less than 100 nanometers.

Nanoscintillation systems for aqueous-based liquid scintillation counting

The present invention provides, inter alia, formulations useful to ameliorate symptoms associated with mucosal abrasions, specifically those due to dental orthodontic brackets; oral surgery; periodontal surgery or other procedures. For instance, there is a formulation comprising: 65 to 75% microcrystalline wax; 5 to 15% non-ionic polymer; 15 to 25% topical anesthetic; and 1 to 5% surfactant, wherein the ratio of non-ionic polymer to microcrystalline wax is no greater than 0.2. Preferably, for solid topical anesthetics, the particle size is less than the apertures of a 100-mesh screen. However, the topical anesthetic may also be a liquid. Formulations wherein the mixture is a homogeneous matrix is preferred.

Formulations for sustained-release of topical anesthetics and methods of

A biodegradable, low biological toxicity, particulate radiographic contrast medium comprises biodegradable polymeric spheres of average molecular weight average diameter about 10-1,000 nm or about 0.01-1.0 micron carrying in at least radiographic contrasting amount of a radiographically opaque element. A method of obtaining a tomographic image of the body portion of a subject comprises administering to the subject a radiographically-detectable amount of the biodegradable, low-toxicity radiographic medium of claim 1; allowing for the spheres to be taken-up by the body portion; and X-raying an area comprising the body portion. A method of improving the contrast of a tomographic image of a body portion of a subject comprises administering to the subject a radiographically-detectable amount of the biodegradable, low-toxicity radiographic medium of claim 1; allowing for the spheres to be selectively taken-up by the body portion; and X-raying an area comprising the body portion.

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Lexington, KY, United States of America

Michael Joseph Jay