Patents by Inventor Francis C. Szoka, Jr.

Francis C. Szoka, Jr. has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Patent number: 10722467
    Abstract: The present invention provides liposome compositions containing sparingly soluble drugs that are used to treat life-threatening diseases. A preferred method of encapsulating a drug inside a liposome is by remote or active loading. Remote loading of a drug into liposomes containing a transmembrane electrochemical gradient is initiated by co-mixing a liposome suspension with a solution of drug, whereby the neutral form of the compound freely enters the liposome and becomes electrostatically charged thereby preventing the reverse transfer out of the liposome. There is a continuous build-up of compound within the liposome interior until the electrochemical gradient is dissipated or all the drug is encapsulated in the liposome. However, this process as described in the literature has been limited to drugs that are freely soluble in aqueous solution or solubilized as a water-soluble complex. This invention describes compositions and methods for remote loading drugs with low water solubility (<2 mg/mL).
    Type: Grant
    Filed: June 27, 2019
    Date of Patent: July 28, 2020
    Assignee: ZONEONE PHARMA, INC.
    Inventors: Mark E. Hayes, Charles O. Noble, Francis C. Szoka, Jr.
  • Patent number: 10507182
    Abstract: The present invention provides liposome compositions containing sparingly soluble drugs that are used to treat life-threatening diseases. A preferred method of encapsulating a drug inside a liposome is by remote or active loading. Remote loading of a drug into liposomes containing a transmembrane electrochemical gradient is initiated by co-mixing a liposome suspension with a solution of drug, whereby the neutral form of the compound freely enters the liposome and becomes electrostatically charged thereby preventing the reverse transfer out of the liposome. There is a continuous build-up of compound within the liposome interior until the electrochemical gradient is dissipated or all the drug is encapsulated in the liposome. However, this process as described in the literature has been limited to drugs that are freely soluble in aqueous solution or solubilized as a water-soluble complex. This invention describes compositions and methods for remote loading drugs with low water solubility (<2 mg/mL).
    Type: Grant
    Filed: September 10, 2018
    Date of Patent: December 17, 2019
    Assignee: ZONEONE PHARMA, INC.
    Inventors: Mark E. Hayes, Charles O. Noble, Francis C. Szoka, Jr.
  • Publication number: 20190314282
    Abstract: The present invention provides liposome compositions containing sparingly soluble drugs that are used to treat life-threatening diseases. A preferred method of encapsulating a drug inside a liposome is by remote or active loading. Remote loading of a drug into liposomes containing a transmembrane electrochemical gradient is initiated by co-mixing a liposome suspension with a solution of drug, whereby the neutral form of the compound freely enters the liposome and becomes electrostatically charged thereby preventing the reverse transfer out of the liposome. There is a continuous build-up of compound within the liposome interior until the electrochemical gradient is dissipated or all the drug is encapsulated in the liposome. However, this process as described in the literature has been limited to drugs that are freely soluble in aqueous solution or solubilized as a water-soluble complex. This invention describes compositions and methods for remote loading drugs with low water solubility (<2 mg/mL).
    Type: Application
    Filed: June 27, 2019
    Publication date: October 17, 2019
    Inventors: Mark E. HAYES, Charles O. NOBLE, Francis C. SZOKA, JR.
  • Publication number: 20190110991
    Abstract: The present invention provides liposome compositions containing sparingly soluble drugs that are used to treat life-threatening diseases. A preferred method of encapsulating a drug inside a liposome is by remote or active loading. Remote loading of a drug into liposomes containing a transmembrane electrochemical gradient is initiated by co-mixing a liposome suspension with a solution of drug, whereby the neutral form of the compound freely enters the liposome and becomes electrostatically charged thereby preventing the reverse transfer out of the liposome. There is a continuous build-up of compound within the liposome interior until the electrochemical gradient is dissipated or all the drug is encapsulated in the liposome. However, this process as described in the literature has been limited to drugs that are freely soluble in aqueous solution or solubilized as a water-soluble complex. This invention describes compositions and methods for remote loading drugs with low water solubility (<2 mg/mL).
    Type: Application
    Filed: September 10, 2018
    Publication date: April 18, 2019
    Inventors: Mark E. HAYES, Charles O. NOBLE, Francis C. SZOKA, JR.
  • Patent number: 10004759
    Abstract: The present invention provides liposome compositions containing sparingly soluble drugs that are used to treat life-threatening diseases. A preferred method of encapsulating a drug inside a liposome is by remote or active loading. However, this process as described in the literature has been limited to drugs that are freely soluble in aqueous solution or solubilized as a water-soluble complex. This invention describes compositions and methods for remote loading drugs with low water solubility (<2 mg/mL). In the preferred embodiment the drug in the solubilizing agent is mixed with the liposomes in aqueous suspension so that the concentration of solubilizing agent is lowered to below its capacity to completely solubilize the drug. This results in the drug precipitating but remote loading is capability retained.
    Type: Grant
    Filed: August 4, 2015
    Date of Patent: June 26, 2018
    Assignee: ZONEONE PHARMA, INC.
    Inventors: Mark E. Hayes, Charles O. Noble, Francis C. Szoka, Jr.
  • Patent number: 9931419
    Abstract: The present invention relates to liposomal vaccine compositions, methods for the manufacture thereof, and methods for the use thereof to stimulate an immune response in an animal. These compositions comprise dimyristoylphosphatidylcholine (“DMPC”); either dimyristoylphosphatidylglycerol (“DMPG”) or dimyristoyltrimethylammonium propane (“DMTAP”) or both DMPC and DMTAP; and at least one sterol derivative providing a covalent anchor for one or more immunogenic polypeptide(s) or carbohydrate(s).
    Type: Grant
    Filed: June 13, 2016
    Date of Patent: April 3, 2018
    Assignees: MOLECULAR EXPRESS, INC., THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Gary Fujii, Francis C. Szoka, Jr., Douglas S. Watson
  • Publication number: 20170239182
    Abstract: The present invention provides liposomes loaded with chelating agents, pharmaceutical formulations including these liposomes and methods of making chelating agent liposomes. Because the chelating agents are loaded in the liposome with high efficiencies, the liposomes are of use in treatment of metal ion overload in subjects. The liposomes can also contain essential trace metals to compensate for the off target effect of removal of endogenous non-target trace metals by administration of the chelator. The liposomes can include two or more different chelating agents of different structures and affinities for metal ions.
    Type: Application
    Filed: August 12, 2015
    Publication date: August 24, 2017
    Inventors: Mark E. HAYES, Charles O. NOBLE, Francis C. SZOKA, JR.
  • Patent number: 9737485
    Abstract: The present invention provides liposome compositions containing sparingly soluble drugs that are used to treat life-threatening diseases. A preferred method of encapsulating a drug inside a liposome is by remote or active loading. Remote loading of a drug into liposomes containing a transmembrane electrochemical gradient is initiated by co-mixing a liposome suspension with a solution of drug, whereby the neutral form of the compound freely enters the liposome and becomes electrostatically charged thereby preventing the reverse transfer out of the liposome. There is a continuous build-up of compound within the liposome interior until the electrochemical gradient is dissipated or all the drug is encapsulated in the liposome. However, this process as described in the literature has been limited to drugs that are freely soluble in aqueous solution or solubilized as a water-soluble complex. This invention describes compositions and methods for remote loading drugs with low water solubility (<2 mg/mL).
    Type: Grant
    Filed: July 21, 2016
    Date of Patent: August 22, 2017
    Assignee: ZONEONE PHARMA, INC.
    Inventors: Mark E. Hayes, Charles O. Noble, Francis C. Szoka, Jr.
  • Publication number: 20170231910
    Abstract: The present invention provides liposomes loaded with chelating agents, pharmaceutical formulations including these liposomes and methods of making chelating agent liposomes. Because the chelating agents are loaded in the liposome with high efficiencies, the liposomes are of use in treatment of metal ion overload in subjects. The liposomes can also contain essential trace metals to compensate for the off target effect of removal of endogenous non-target trace metals by administration of the chelator. The liposomes can include two or more different chelating agents of different structures and affinities for metal ions.
    Type: Application
    Filed: August 12, 2015
    Publication date: August 17, 2017
    Inventors: Mark E. HAYES, Charles O. NOBLE, Francis C. SZOKA, JR.
  • Publication number: 20170202776
    Abstract: The present invention provides liposome compositions containing sparingly soluble drugs that are used to treat life-threatening diseases. A preferred method of encapsulating a drug inside a liposome is by remote or active loading. Remote loading of a drug into liposomes containing a transmembrane electrochemical gradient is initiated by co-mixing a liposome suspension with a solution of drug, whereby the neutral form of the compound freely enters the liposome and becomes electrostatically charged thereby preventing the reverse transfer out of the liposome. There is a continuous build-up of compound within the liposome interior until the electrochemical gradient is dissipated or all the drug is encapsulated in the liposome. However, this process as described in the literature has been limited to drugs that are freely soluble in aqueous solution or solubilized as a water-soluble complex. This invention describes compositions and methods for remote loading drugs with low water solubility (<2 mg/mL).
    Type: Application
    Filed: February 9, 2017
    Publication date: July 20, 2017
    Inventors: Mark E. HAYES, Charles O. NOBLE, Francis C. SZOKA, JR.
  • Publication number: 20170157266
    Abstract: The present invention relates to liposomal vaccine compositions, methods for the manufacture thereof, and methods for the use thereof to stimulate an immune response in an animal. These compositions comprise dimyristoylphosphatidylcholine (“DMPC”); either dimyristoylphosphatidylglycerol (“DMPG”) or dimyristoyltrimethylammonium propane (“DMTAP”) or both DMPC and DMTAP; and at least one sterol derivative providing a covalent anchor for one or more immunogenic polypeptide(s) or carbohydrate(s).
    Type: Application
    Filed: June 13, 2016
    Publication date: June 8, 2017
    Inventors: Gary FUJII, Francis C. SZOKA, JR., Douglas S. WATSON
  • Publication number: 20170128366
    Abstract: The present invention provides liposomes loaded with chelating agents, pharmaceutical formulations including these liposomes and methods of making chelating agent liposomes. Because the chelating agents are loaded in the liposome with high efficiencies, the liposomes are of use in treatment of metal ion overload in subjects. The liposomes can include two or more different chelating agents of different structures and affinities for metal ions.
    Type: Application
    Filed: January 23, 2017
    Publication date: May 11, 2017
    Inventors: Mark E. HAYES, Charles O. NOBLE, Francis C. SZOKA, JR.
  • Publication number: 20160324780
    Abstract: The present invention provides liposome compositions containing sparingly soluble drugs that are used to treat life-threatening diseases. A preferred method of encapsulating a drug inside a liposome is by remote or active loading. Remote loading of a drug into liposomes containing a transmembrane electrochemical gradient is initiated by co-mixing a liposome suspension with a solution of drug, whereby the neutral form of the compound freely enters the liposome and becomes electrostatically charged thereby preventing the reverse transfer out of the liposome. There is a continuous build-up of compound within the liposome interior until the electrochemical gradient is dissipated or all the drug is encapsulated in the liposome. However, this process as described in the literature has been limited to drugs that are freely soluble in aqueous solution or solubilized as a water-soluble complex. This invention describes compositions and methods for remote loading drugs with low water solubility (<2 mg/mL).
    Type: Application
    Filed: July 21, 2016
    Publication date: November 10, 2016
    Inventors: Mark E. HAYES, Charles O. NOBLE, Francis C. SZOKA, JR.
  • Patent number: 9364563
    Abstract: The present invention relates to liposomal vaccine compositions, methods for the manufacture thereof, and methods for the use thereof to stimulate an immune response in an animal. These compositions comprise dimyristoylphosphatidylcholine (“DMPC”); either dimyristoylphosphatidylglycerol (“DMPG”) or dimyristoyltrimethylammonium propane (“DMTAP”) or both DMPC and DMTAP; and at least one sterol derivative providing a covalent anchor for one or more immunogenic polypeptide(s) or carbohydrate(s).
    Type: Grant
    Filed: June 30, 2014
    Date of Patent: June 14, 2016
    Assignees: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA, MOLECULAR EXPRESS, INC.
    Inventors: Gary Fujii, Francis C. Szoka, Jr., Douglas S. Watson
  • Patent number: 8956646
    Abstract: In various embodiments, the present invention provides zwitterionic lipids, encapsulants incorporating these zwitterionic lipids and such encapsulants encapsulating one or more bioactive agent. An exemplary bioactive agent is a nucleic acid. Also provided are pharmaceutical formulations of the encapsulants and methods of using such formulations to deliver a bioactive agent to a subject in treating or diagnosing disease in that subject.
    Type: Grant
    Filed: August 15, 2011
    Date of Patent: February 17, 2015
    Assignee: The Regents of the University of California
    Inventors: Francis C. Szoka, Jr., Colin Walsh, Vincent Venditto, Juliane Nguyen, Emily Perttu
  • Publication number: 20140308341
    Abstract: The present invention relates to liposomal vaccine compositions, methods for the manufacture thereof, and methods for the use thereof to stimulate an immune response in an animal. These compositions comprise dimyristoylphosphatidylcholine (“DMPC”); either dimyristoylphosphatidylglycerol (“DMPG”) or dimyristoyltrimethylammonium propane (“DMTAP”) or both DMPC and DMTAP; and at least one sterol derivative providing a covalent anchor for one or more immunogenic polypeptide(s) or carbohydrate(s).
    Type: Application
    Filed: June 30, 2014
    Publication date: October 16, 2014
    Inventors: Gary FUJII, Francis C. SZOKA, JR., Douglas S. WATSON
  • Publication number: 20140271825
    Abstract: The present invention provides liposomes loaded with chelating agents, pharmaceutical formulations including these liposomes and methods of making chelating agent liposomes. Because the chelating agents are loaded in the liposome with high efficiencies, the liposomes are of use in treatment of metal ion overload in subjects. The liposomes can include two or more different chelating agents of different structures and affinities for metal ions.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Inventors: Mark E. HAYES, Charles O. NOBLE, Francis C. SZOKA, JR.
  • Publication number: 20140220112
    Abstract: Sparingly water-soluble agents can be formulated as cyclodextrin complexes, however, these water-soluble drug-cyclodextrin complexes dissociate when the complex is administered into patients. The dilution of the complex in the patient leads to the drug being released from the complex, so the drug is not effectively targeted. In contrast, drugs encapsulated in the aqueous core of a lipid vesicles are not released when the liposome is diluted in blood. This invention describes compositions and methods whereby cyclodextrin or polyanionic beta-cyclodextrin drug-complexes are mixed with a preformed liposome containing the amine salts of an acidic compound. This results in the drug cyclodextrin complex being transferred into the liposome where it is stably retained. The liposome-encapsulated drug can then be injected into a patient.
    Type: Application
    Filed: February 3, 2014
    Publication date: August 7, 2014
    Inventors: Francis C. SZOKA, JR., Charles O. Noble, Mark E. Hayes
  • Publication number: 20140220110
    Abstract: The present invention provides liposome compositions containing sparingly soluble drugs that are used to treat life-threatening diseases. A preferred method of encapsulating a drug inside a liposome is by remote or active loading. Remote loading of a drug into liposomes containing a transmembrane electrochemical gradient is initiated by co-mixing a liposome suspension with a solution of drug, whereby the neutral form of the compound freely enters the liposome and becomes electrostatically charged thereby preventing the reverse transfer out of the liposome. There is a continuous build-up of compound within the liposome interior until the electrochemical gradient is dissipated or all the drug is encapsulated in the liposome. However, this process as described in the literature has been limited to drugs that are freely soluble in aqueous solution or solubilized as a water-soluble complex. This invention describes compositions and methods for remote loading drugs with low water solubility (<2 mg/mL).
    Type: Application
    Filed: February 3, 2014
    Publication date: August 7, 2014
    Inventors: Mark E. HAYES, Charles O. NOBLE, Francis C. SZOKA, JR.
  • Publication number: 20140220111
    Abstract: The present invention provides liposome compositions containing sparingly soluble drugs that are used to treat life-threatening diseases. A preferred method of encapsulating a drug inside a liposome is by remote or active loading. Remote loading of a drug into liposomes containing a transmembrane electrochemical gradient is initiated by co-mixing a liposome suspension with a solution of drug, whereby the neutral form of the compound freely enters the liposome and becomes electrostatically charged thereby preventing the reverse transfer out of the liposome. There is a continuous build-up of compound within the liposome interior until the electrochemical gradient is dissipated or all the drug is encapsulated in the liposome. However, this process as described in the literature has been limited to drugs that are freely soluble in aqueous solution or solubilized as a water-soluble complex. This invention describes compositions and methods for remote loading drugs with low water solubility (<2 mg/mL).
    Type: Application
    Filed: February 3, 2014
    Publication date: August 7, 2014
    Inventors: Mark E. HAYES, Charles O. NOBLE, Francis C. SZOKA, JR.