Abstract: Pharmaceutical pegylated liposomal formulations for photodynamic therapy are presented. The pegylated liposomal formulation provides therapeutically effective amounts of the photosensitizer for intravenous administration. At least one of the phospholipids in the liposomes has been linked with poly ethylene glycol (PEG) as an integral part of the phospholipids. The formed pegylated liposomes contain the hydrophobic photosensitizer within the lipid bilayer membrane. Pegylation of liposomes carrying the hydrophobic photosensitizer helps to maintain the drug level within the therapeutic window for longer time periods and provides the drug a longer circulating half life in vivo. Further the pegylated formulation of hydrophobic photosensitizers shows improved pharmacokinetics over standard non-liposomal formulations thus enhancing the efficacy of PDT with the pegylated liposomal formulations.
Type:
Grant
Filed:
February 7, 2006
Date of Patent:
March 24, 2015
Assignee:
Biolitec Pharma Marketing Ltd
Inventors:
Volker Albrecht, Alfred Fahr, Dietrich Scheglmann, Susanna Gräfe, Wolfgang Neuberger
Abstract: The present invention provides a long circulating non-pegylated liposomal doxorubicin hydrochloride composition for parenteral administration and a process for its preparation. The circulation time in Swiss albino mice is at least 25 times longer than conventional non-liposomal formulations. The non-pegylated liposomes are stable, exhibit low toxicity and have been found to be efficacious in different tumor models.
Abstract: A phospholipid microbubble comprising a shell which comprises a plurality of polyunsaturated fatty acid (“PUFA”)-containing phospholipids, and a core of inert gas surrounded by the shell comprising the plurality of PUFA-containing phospholipids. The present invention also provides methods of delivering a prophylactically or therapeutically effective amount of PUFA to an area of disease or injury in a subject. The present invention also provides methods of preventing or treating a disease in a subject using a prophylactically or therapeutically effective amount of the aforementioned phospholipid microbubbles.
Abstract: An object of the present invention is to further enhance the antitumor effect when oxaliplatin is administered in combination with a combination drug containing tegafur, gimeracil and oteracil potassium. According to the present invention, by using oxaliplatin encapsulated in a liposome preparation, combination therapy of oxaliplatin plus a combination drug containing tegafur, gimeracil and oteracil potassium, is revealed to show remarkably enhanced antitumor effect without increasing side effects.
Type:
Grant
Filed:
January 29, 2009
Date of Patent:
January 27, 2015
Assignees:
The University of Tokushima, Taiho Pharmaceutical Co. Ltd.
Abstract: The present invention provides pharmaceutical compositions comprising a glucocorticoid or glucocorticoid derivative stably encapsulated in a liposome. The glucocorticoid or glucocorticoid derivative is selected from an amphipathic weak base glucocorticoid or glucocorticoid derivative having a pKa equal or below 11 and a logD at pH 7 in the range between ?2.5 and 1.5; or an amphipathic weak acid GC or GC derivative having a pKa above 3.5 and a logD at pH 7 in the range between ?2.5 and 1.5. The therapeutic effect of the pharmaceutical composition of the invention was exhibited in vivo with appropriate models of multiple sclerosis and cancer.
Type:
Grant
Filed:
September 11, 2005
Date of Patent:
January 13, 2015
Assignee:
Yissum Research Development Company of the Hebrew University of Jerusalem
Inventors:
Yechezkel Barenholz, Alberto A. Gabizon, Yuval Avnir
Abstract: The present invention relates compositions for delivering therapeutic agents from a medical device including an expandable and collapsible structure and methods employing them. A lipid coating including one or more fatty acids increases the amount of therapeutic agent released from the device at the delivery site. The therapeutic agent can be in a matrix including a hydrophilic polymer or an amphiphilic polymer. Release and adhesion coatings can also facilitate delivery of therapeutic agent.
Type:
Grant
Filed:
June 30, 2011
Date of Patent:
January 6, 2015
Assignee:
SurModics, Inc.
Inventors:
Ralph A. Chappa, Emily R. Rolfes Meyering
Abstract: A novel pharmaceutical composition is provided by which nonsteroidal anti-inflammatory drugs (NSAIDs) are added directly to phospholipid-containing oil such as lecithin oils or to a bio-compatible oil to which an phospholipid has been added to make a NSAID-containing formulation that possess low gastrointestinal (GI) toxicity and enhanced therapeutic activity to treat or prevent inflammation, pain, fever, platelet aggregation, tissue ulcerations and/or other tissue disorders. The composition of the invention are in the form of a non-aqueous solution, paste, suspension, dispersion, colloidal suspension or in the form of an aqueous emulsion or microemulstion for internal, oral, direct or topical administration.
Type:
Grant
Filed:
September 16, 2010
Date of Patent:
December 16, 2014
Assignee:
The Board of Regents of the University of Texas System
Abstract: The present invention concerns methods of joint lubrication and/or prevention of cartilage wear making use of liposomes having membranes with at least one phospholipid (PL) of the group consisting of a glycerophospholipid (GPL) having two, being the same or different, C12-C16 hydrocarbon chain and a sphingolipid (SPL) having a C12-C15 hydrocarbon chain, the one or more membranes having a phase transition temperature in which solid ordered (SO) to liquid disordered (LD) phase transition occurs, the phase transition temperature being within a temperature of about 20° C. to about 39° C. for lubrication of joints.
Type:
Grant
Filed:
March 26, 2009
Date of Patent:
November 25, 2014
Assignees:
Technion Research and Development Foundation Ltd., Hadasit Medical Research Services & Development Limited, Yissum Research Development Company of the Hebrew University of Jerusalem
Abstract: The invention relates generally to methods of making formulations for delivering biological agents to a patient. In one aspect, proliposomal drug-delivery systems for medicaments are provided. In another aspect, coated proliposomal formulations for poorly water soluble drugs, and methods for making the same, are provided. Certain embodiments of the present invention provide enhanced stability and bioavailability for pharmaceutical formulations.
Abstract: Provided herein is a process for preparing a microparticulate complex of a particle-forming component (“PFC”) and a nucleic acid-like component (“NAC”) in a monophasic composition comprising water and a water-miscible organic solvent. Also provided is a microparticulate complex that comprises a particle-forming component complexed to a nucleic acid-like component, and a composition comprising water and the microparticulate complex. Further provided is a method of delivery of a nucleic acid-like component to a cell or to a patient by contacting the cell with or administering to the patient a composition comprising water and the microparticulate complex described herein. Still further, a charge-changing composition represented by the formula A-X—B is provided.
Type:
Grant
Filed:
July 11, 2013
Date of Patent:
November 11, 2014
Assignee:
Sutter West Bay Hospitals
Inventors:
Keelung Hong, Wei Wen Zheng, Daryl C. Drummond, Dmitri B. Kirpotin, Mark Eamon Hayes
Abstract: The present invention provides pH-responsive liposomes which are capable of holding a desired substance in an acidic pH environment and releasing the desired substance in a basic pH environment. The present invention uses pH-responsive liposomes comprising, as constituent lipids thereof, a cationic amphiphilic molecule and at least one of an anionic amphiphilic molecule and a twitterionic amphiphilic molecule, wherein the liposomes, when dispersed in an aqueous medium, have a positive zeta potential in an acidic environment where the dispersion has a pH of less than 6.5 and have a negative zeta potential in a basic environment where the dispersion has a pH of 8.5 or more.
Abstract: A novel pharmaceutical composition is provided by which nonsteroidal anti-inflammatory drugs (NSAIDs) are added directly to phospholipid-containing oil such as lecithin oils or to a bio-compatible oil to which an phospholipid has been added to make a NSAID-containing formulation that possess low gastrointestinal (GI) toxicity and enhanced therapeutic activity to treat or prevent inflammation, pain, fever, platelet aggregation, tissue ulcerations and/or other tissue disorders. The composition of the invention are in the form of a non-aqueous solution, paste, suspension, dispersion, colloidal suspension or in the form of an aqueous emulsion or microemulstion for internal, oral, direct or topical administration.
Type:
Grant
Filed:
September 16, 2010
Date of Patent:
October 21, 2014
Assignee:
The Board of Regents of the University of Texas System
Abstract: Disclosed is a technique for allowing an active ingredient as an agent for improving or maintaining the dermal environment to reach a dermis. Specifically disclosed is a vesicle comprising the following components 1) to 3): 1) an ?,?-bis(?-N—(C10-30)acylglutamyl)lysine and/or a salt thereof; 2) ceramide and/or a derivative thereof; and 3) one or more selected from a glycerin fatty acid ester, a polyglycerin fatty acid ester and a pyroglutamic acid glycerin fatty acid ester. The acyl group in the ?,?-bis(?-N—(C10-30)acylglutamyl)lysine is preferably a lauroyl group. The ceramide or the derivative thereof is preferably ceramide type-2 or ceramide type-3. The vesicle can encapsulate an active ingredient. The vesicle can be contained in an external preparation for the skin.
Abstract: Compositions comprising microaggregates containing hydrophobic drugs, as well as methods for their production, are described. Such microaggregates may include micelle structures or combinations thereof with liposomes, and constitute an effective delivery vehicle for a hydrophobic agent. Methods for microaggregate production include the use of preferred lipid compounds and processing conditions favoring the production of small aggregates for improved filter sterilization.
Type:
Grant
Filed:
June 19, 2009
Date of Patent:
October 7, 2014
Assignee:
Valeant Pharmaceuticals International, Inc.
Inventors:
Ronald Erwin Boch, Dev Mitra Ranji Singh, Iman Karmadi
Abstract: A stanol composition containing in addition to sitostanol as the main component, also a substantial amount of at least 10% campestanol has been found to effectively lower serum cholesterol levels when incorporated in edible commodities. Upon esterification the composition is especially useful in edible fats and oils and in fat-containing foods.
Type:
Grant
Filed:
December 18, 2012
Date of Patent:
October 7, 2014
Assignee:
Raisio Nutrition Ltd.
Inventors:
Ingmar Wester, Tapio Palmu, Tatu Miettinen, Helena Gylling
Abstract: Compositions and methods for transport or release of therapeutic and diagnostic agents or metabolites or other analytes from cells, compartments within cells, or through cell layers or barriers are described. The compositions include a membrane barrier transport enhancing agent and are usually administered in combination with an enhancer and/or exposure to stimuli to effect disruption or altered permeability, transport or release. In a preferred embodiment, the compositions include compounds which disrupt endosomal membranes in response to the low pH in the endosomes but which are relatively inactive toward cell membranes, coupled directly or indirectly to a therapeutic or diagnostic agent. Other disruptive agents can also be used, responsive to stimuli and/or enhancers other than pH, such as light, electrical stimuli, electromagnetic stimuli, ultrasound, temperature, or combinations thereof.
Type:
Grant
Filed:
July 14, 2011
Date of Patent:
September 30, 2014
Assignees:
University of Washington, University of Massachusetts
Inventors:
Allan S. Hoffman, Patrick Stayton, Oliver W. Press, Niren Murthy, Chantal Lackey Reed, Lawrence A. Crum, Pierre D. Mourad, Tyrone M. Porter, David Tirrell
Abstract: This invention comprises a sterically stabilized liposome carrier encapsulating a selected drug for the aerosol delivery of the drug effectual in the treatment of the lungs of a mammal, a composition containing the sterically stabilized liposome carrier and the selected drug effective for the treatment of the lungs of a mammal for asthma and inflammation of the lungs of the mammal as an aerosol and a method of, treatment using the composition. The composition provides effective treatment for the longer of a period of time at least twice as long as the selected drug alone or up to at least one week.
Type:
Grant
Filed:
July 18, 2008
Date of Patent:
September 30, 2014
Assignee:
VGSK Technologies, Inc.
Inventors:
Kameswari S. Konduri, Sandhya Nandedkar, Nejat Duzgunes, Ramakrishna Pattisapu
Abstract: The present invention provides lipid emulsions and methods of intravenously administering lipid emulsions to treat systemic toxicity caused by foreign lipophilic and amphiphilic substances. In particular, methods are provided to treat cardiovascular impairment, such as cardiotoxicity, asystole and ischemia of the brain and heart, and neurological impairments, such as seizures and comas, caused by foreign lipophilic and amphiphilic substances, including cardiovascular impairment caused by local anesthetics, tricyclic antidepressants, sodium channel blockers, and calcium channel blockers.
Abstract: The invention provides a method for obtaining local anesthetics encapsulated in liposomes, such as multi vesicular liposomes, with high encapsulation efficiency and slow release in vivo. When the encapsulated anesthetic is administered as a single intracutaneous dose, the duration of anesthesia and half-life of the drug at the local injection site is increased as compared to injection of unencapsulated anesthetic. The maximum tolerated dose of the encapsulated anesthetic is also markedly increased in the liposomal formulation over injection of unencapsulated anesthetic. These results show that the liposomal formulation of local anesthetic is useful for sustained local infiltration and nerve block anesthesia.
Abstract: Disclosed are methods and compositions for the controlled release of a drug or agent from a liposome using light or radiation. Also disclosed are compositions comprising liposomes having a lipid layer, wherein the liposomes contain an agent, an enzyme capable of releasing the agent from the liposome, and an enzyme activator sequestered by a molecular cage. In another aspect, methods of delivering an agent to a target in a subject are disclosed.
Type:
Grant
Filed:
March 31, 2010
Date of Patent:
August 19, 2014
Assignee:
The Board of Trustees of the University of Arkansas
Inventors:
Daniel Fologea, Greg Salamo, Ralph Henry, Michael J. Borrelli, Peter M. Corry