Nanoparticle-Based Targeted Drug Delivery For In Vivo Bone Loss Mitigation
AssigneeSouthwest Research Institute
InventorsHong DIXON, Qingwen NI, Joseph A. McDONOUGH
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Abstract
The present invention is directed to nanoparticle-based targeted drug delivery system for treatment of bone-loss. An enantiomeric phenothiazine is formulated into an in-vivo nanoparticle delivery system which may contain bone-targeting functionality. The nanoparticle formulations and their associated influence on whole bone porosity may now also be evaluated utilizing nuclear magnetic resonance (NMR) and relaxation time profiles, and in particular, median T2 relaxation times.
Claims30
A medicament comprising phenothiazines having the structure:
- wherein A may be selected from the group consisting of linear or branched alkyls and/or linear or branched alkenyl groups having 1 to 5 carbon atoms;
- R1 may be a tertiary amine or thiol group having a structure including N—(R2)3 or S—(R2) wherein R2 comprises the same or different entities selected from the group consisting of hydrogen, alkyl groups, alkenyl groups having 1 to 4 carbon atoms, cyclic alkene groups and heterocyclic alkylene groups comprising a heterocyclic element selected from the group consisting of nitrogen and sulfur;
- wherein said medicament is in nanoparticle form having a largest linear dimension of 1-999 nanometers.
A method of preventing or inhibiting a disease or condition comprising administering to a patient or animal having a risk of having a disease or condition associated with bone loss a therapeutically effective amount of a medicament comprising:
- phenothiazines having the structure:
- wherein A may be selected from the group consisting of linear or branched alkyls and/or linear or branched alkenyl groups having 1 to 5 carbon atoms;
- R1 may be a tertiary amine or thiol group having a structure including N—(R2)3 or S—(R2) wherein R2 comprises the same or different entities selected from the group consisting of hydrogen, alkyl groups, alkenyl groups having 1 to 4 carbon atoms, cyclic alkene groups and heterocyclic alkylene groups comprising a heterocyclic element selected from the group consisting of nitrogen and sulfur;
- wherein said medicament is in nanoparticle form having a largest linear dimension of 1-999 nanometers and wherein said medicament is combined in a pharmaceutically acceptable carrier.
A method for using nuclear magnetic resonance to characterize bone porosity comprising:
- placing a bone sample in an external magnetic field wherein said bone has a whole bone porosity comprising the porosity of the cortical, trabecular and marrow porosity for said bone;
- providing an oscillating radio frequency electromagnetic field for exciting protons within said bone sample;
- providing a receiver to receive signals in the form of data from the excited protons;
- measuring the distribution of protons in said bone sample from said spectrum;
- processing said data to characterize said whole bone porosity wherein said processing step includes determining the median T2 relaxation times from said data.
A method of preventing or inhibiting a disease or condition comprising administering to a patient or animal having a risk of having a disease or condition associated with bone loss a therapeutically effective amount of a nanoparticle medicament including in-vivo bone targeting functionality comprising:
- phenothiazines having the structure:
- wherein A may be selected from the group consisting of linear or branched alkyls and/or linear or branched alkenyl groups having 1 to 5 carbon atoms;
- R1 may be a tertiary amine or thiol group having a structure including N—(R2)3 or S—(R2) wherein R2 comprises the same or different entities selected from the group consisting of hydrogen, alkyl groups, alkenyl groups having 1 to 4 carbon atoms, cyclic alkene groups and heterocyclic alkylene groups comprising a heterocyclic element selected from the group consisting of nitrogen and sulfur;
- wherein said medicament is in nanoparticle form having a largest linear dimension of 1-999 nanometers and said nanoparticle form includes bone targeting functionality.
Dependencies are inferred from the claim text.