IP Library Granted Patent US 10,512,607
Granted Patent B2
US 10,512,607 · App. 15/333,312 · Granted Dec 24, 2019

Polymeric particles, method for cytosolic delivery of cargo, methods of making the particles

Inventors: Benjamin G. Keselowsky (Gainesville, FL); Jamal Lewis (Tallahassee, FL); Lawrence Premasiri Fernando (Gainesville, FL); Craig L. Duvall (Nashville, TN); Brian C. Evans (Bartlett, TN); Lirong Yang (Martigny, CH)
Assignees: Vanderbilt University; University of Florida Research Foundation, Inc.
A61K9/146A61K47/32A61K47/34A61K2039/55555
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Quick Facts
Patent No.
US 10,512,607
App. No.
15/333,312
Granted
Dec 24, 2019
Kind
B2
Abstract

Embodiments of the present disclosure include particles, methods of making particles, methods of delivering an active agent using the particle, and the like.

Claims (14)

1. A particle, comprising:

a composite material of poly(lactide-coglycolide) (PLGA) and a membrane-destabilizing agent, wherein the composite material includes an active agent and forms a microparticle substantially encapsulating the active agent, wherein the membrane-destabilizing agent is a poly(alkylacrylic acid) homopolymer and wherein the ratio of PLGA to membrane-destabilizing agent is about 100:1 to 10:1.

2. The particle of claim 1 , wherein the particle has an average pH of about 6.5 or lower.

3. The particle of claim 1 , wherein the poly(alkylacrylic acid) homopolymer is selected from the group consisting of: polypropylacrylic acid (PPAA) homopolymer, poly(2-ethylacrylic acid) (PEAA) homopolymer, (2-methylacrylic acid) (PMAA) homopolymer, and a combination thereof.

4. The particle of claim 1 , wherein the poly(alkylacrylic acid) homopolymer is polypropylacrylic acid (PPAA).

5. The particle of claim 1 , wherein the particles have a Zeta potential less than −20 mV at physiological pH.

6. The particle of claim 1 , wherein PLGA is the product of lactic acid and glycolic acid, wherein the ratio of lactic acid to glycolic acid when making PLGA is about 0.1:100 to 100:0.1.

7. The particle of claim 1 , wherein the PLGA has a molecular weight of about 10 to 100 kg/mol.

8. The particle of claim 1 , wherein the particle has an average diameter of about 0.5 to 1 μm.

9. The particle of claim 1 , wherein the particle has a diameter of about 0.2 to 100 μm.

10. The particle of claim 1 , wherein the active agent is selected from the group consisting of: small molecules, peptides, proteins, imaging contrast agents, and nucleic acids.

11. The particle of claim 1 , made by a process comprising:

combining the PLGA, the active agent and the poly(alkylacrylic acid) homopolymer to form a composite material;

homogenizing the composite material in water having an acidic pH to form the microparticles.

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 6, 2019
From: LEWIS, JAMAL
To: UNIVERSITY OF FLORIDA RESEARCH FOUNDATION, INC.
Reel/Frame 050939/0182 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 27, 2017
From: KESELOWSKY, BENJAMIN G.; FERNANDO, LAWRENCE PREMASIRI; YANG, LIRONG
To: UNIVERSITY OF FLORIDA RESEARCH FOUNDATION, INC.
Reel/Frame 041747/0644 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 27, 2017
From: DUVALL, CRAIG L.; EVANS, BRIAN C.
To: VANDERBILT UNIVERSITY
Reel/Frame 041747/0800 →
Continuity (3)
Provisional Application 62248452 · Oct 30, 2015
Provisional Application 62298039 · Feb 22, 2016
Related Publication 20170119668A1 · May 4, 2017