Afobazole nanoparticles formulation for enhanced therapeutics

Patent metadata

Field	Value
Publication number	US-10172867-B2
Application number	US-201715474463-A
Country	US
Kind code	B2
Filing date	Mar 30, 2017
Priority date	Oct 1, 2014
Publication date	Jan 8, 2019
Grant date	Jan 8, 2019

Abstract

A novel nanoparticle drug composition and method of use thereof is presented herein. The nanoparticle drug composition is comprised of at least one nanoparticle carrier, formed from the conjugation of PLGA and PEG, which encapsulates a drug such as afobazole and its derivatives, in a pharmaceutically acceptable carrier. The nanoparticle drug composition may be used to treat various diseases of the central nervous system involving excessive neuronal activity and inflammation such as stroke, Alzheimer's disease and anxiety.

First claim

What is claimed is:

1. A nanoparticle drug composition comprising:
at least one nanoparticle carrier comprising a poly(lactic-co-glycolic acid) polymer conjugated to polyethylene glycol wherein the nanoparticle carrier is coated with glutathione; and
a pharmaceutically active agent encapsulated within the at least one nanoparticle carrier wherein the pharmaceutically active agent is afobazole;
wherein the nanoparticle drug composition is generated by the process consisting essentially of:
dissolving or diluting the poly(lactic-co-glycolic acid) conjugated to the amphiphilic polyol in acetone to form a polymer solution;
dissolving a predetermined quantity of the afobazole in ethanol to form a drug solution;
adding the drug solution to the polymer solution to form an organic phase solution;
adding the organic phase solution to deionized water to form a mixture;
stirring the mixture;
evaporating the acetone from the mixture wherein upon evaporation of the acetone a suspension of nanoparticles is generated; and
coating the suspension of nanoparticles with the glutathione.

2. The composition of claim 1 , wherein the nanoparticle carrier has a mean particle size of between about 100 nm and about 250 nm.

3. A method of treating a central nervous system disorder in a patient in need thereof comprising: administering a therapeutically effective amount of a nanoparticle drug composition according to claim 1 .

4. The method of claim 3 , wherein the central nervous system disorder is characterized by excessive neuronal activity or inflammation.

5. The method of claim 3 , wherein the central nervous system disorder is selected from the group consisting of ischemia, Alzheimer's disease, multiple sclerosis and anxiety.

6. The method of claim 3 , wherein the nanoparticle carrier has a mean particle size of between about 100 nm and about 250 nm.

7. A method of generating a nanoparticle suspension comprising: nanoprecipitation of a polymer, further comprising dissolving or diluting poly(lactic-co-glycolic acid) conjugated with polyethylene glycol (PLGA-PEG) in acetone to form a polymer solution; dissolving a predetermined quantity of afobazole in ethanol to form a drug solution; adding the drug solution to the polymer solution to form an organic phase solution; adding the organic phase solution to deionized water to form a mixture; stirring the mixture; evaporating the acetone from the mixture wherein upon evaporation of the acetone a suspension of nanoparticles is generated; and coating the suspension of nanoparticles with a hydrophilic antioxidant.

8. The method of claim 7 , wherein the hydrophilic antioxidant is glutathione.

9. The method of claim 7 , wherein the acetone is evaporated overnight at room temperature.

Assignees

• Cuevas Javier
• Katnik Christopher
• Sutariya Vijaykumar B
• Univ South Florida

Inventors

• Cuevas Javier
• Katnik Christopher
• Sutariya Vijaykumar B

Classifications

• A61K9/5153

  Polyesters, e.g. poly(lactide-co-glycolide) · CPC title

• A61K9/5192

  Processes · CPC title

• A61K31/5377 Primary

  not condensed and containing further heterocyclic rings, e.g. timolol · CPC title

• A61K9/5146

  obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyamines, polyanhydrides · CPC title

• A61K9/5169

  Proteins, e.g. albumin, gelatin · CPC title