IP Library Granted Patent US 10,588,860
Granted Patent B2
US 10,588,860 · App. 15/228,686 · Granted Mar 17, 2020

Poly(vinyl benzoate) nanoparticles for molecular delivery

Inventors: Edward Turos (Wesley Chapel, FL); Raphael Labruere (Creteil, FR); Ryan Scott Cormier (Lutz, FL); Renaud Sicard (Coral Gables, FL)
Assignee: University of South Florida
A61K9/146A61K9/0019A61K9/10A61K9/5138A61K47/10A61K47/6933A61K49/0039A61K49/0043A61K49/0093
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Quick Facts
Patent No.
US 10,588,860
App. No.
15/228,686
Granted
Mar 17, 2020
Kind
B2
Abstract

The present invention comprises poly(vinyl benzoate) nanoparticle suspensions as molecular carriers. These nanoparticles can be formed by nanoprecipitation of poly(vinyl benzoate) in water using Pluronic F68 as surfactant, to create spherical nanostructures measuring about 200-250 nm in diameter which are stable in phosphate buffer and blood serum, and only slowly degrade in the presence of esterases. Kinetics experiments in phosphate buffer indicate that 78% of the coumarin-6 was encapsulated within the polymer matrix of the nanoparticle, and the residual 22% of coumarin-6 was surface-bound and quickly released. The nanoparticles are non-toxic in vitro towards human epithelial cells (IC 50 >1000 μg/mL) and primary bovine primary aortic endothelial cells (IC 50 >500 μg/mL), and exert non-observable bactericidal activity against a selection of representative test microbes (MIC>250 μg/mL). Poly(vinyl benzoate) nanoparticles are suitable carriers for molecular delivery of lipophilic small molecules such as drugs pharmaceutical and imaging agents.

Claims (15)

1. A molecular carrier comprising:

at least one biodegradable nanoparticle in a nanoparticle suspension formed from poly(vinyl benzoate) and a block copolymer based on ethylene oxide and propylene oxide;

wherein the nanoparticle suspension is formed by nanoprecipitation of poly(vinyl benzoate) comprising

adding at least one surfactant to water, wherein the at least one surfactant is a block copolymer based on ethylene oxide and propylene oxide;

dissolving or diluting poly(vinyl benzoate) in acetone;

adding the poly(vinyl benzoate)-acetate solution to the water to form a mixture of the block copolymer based on ethylene oxide and propylene oxide and poly(vinyl benzoate); and

stirring the mixture of the block copolymer based on ethylene oxide and propylene oxide and poly(vinyl benzoate) to leave a suspension of the polyvinyl benzoate nanoparticles.

2. The molecular carrier of claim 1 , wherein the molecular carrier entraps a lipophilic small molecule.

3. The molecular carrier of claim 2 , wherein the size of the lipophilic molecule is up to about 5% by weight.

4. The molecular carrier of claim 2 , wherein the lipophilic molecule is an antibacterial agent.

5. The molecular carrier of claim 2 , wherein the lipophilic molecule is a drug.

6. The molecular carrier of claim 1 , wherein the at least one biodegradable nanoparticle in the nanoparticle suspension have a mean particle size between about 50 nm and about 350 nm.

7. The molecular carrier of claim 1 , wherein the at least one biodegradable nanoparticle in the nanoparticle suspension have a mean particle size between about 200 nm and about 250 nm.

8. The molecular carrier of claim 1 , wherein the molecular carrier slowly degrades in presence of esterases.

9. The molecular carrier of claim 1 , wherein the molecular carrier is stable in blood serum and phosphate buffer.

Assignments (2)
CONFIRMATORY LICENSE Recorded Sep 9, 2016
From: UNIVERSITY OF SOUTH FLORIDA
To: NATIONAL SCIENCE FOUNDATION
Reel/Frame 039980/0611 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 5, 2016
From: TUROS, EDWARD; LABRUERE, RAPHAEL; SICARD, RENAUD; CORMIER, RYAN SCOTT
To: UNIVERSITY OF SOUTH FLORIDA
Reel/Frame 039354/0612 →
Continuity (4)
Division 13897868 · May 20, 2013
Continuation PCTUS2011061429 · Nov 18, 2011
Provisional Application 61415003 · Nov 18, 2010
Related Publication 20160338962A1 · Nov 24, 2016