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AssigneeTherasyn Sensors, Inc.
InventorsJerome J. Schentag, Mary P. McCourt, Lawrence Mielnicki, Julie Hughes
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The present invention is directed to a cargo-loaded cholesteryl ester nanoparticle with a hollow compartment (“cholestosome”) consisting essentially of at least one non-ionic cholesteryl ester and one or more encapsulated active molecules which cannot appreciably pass through an enterocyte membrane in the absence of said molecule being loaded into said cholestosome, the cholestosome having a neutral surface and having the ability to pass into enterocytes in the manner of orally absorbed nutrient lipids using cell pathways to reach the golgi apparatus. Pursuant to the present invention, the novel cargo loaded cholestosomes according to the present invention are capable of depositing active molecules within cells of a patient or subject and effecting therapy or diagnosis of the patient or subject.
A pharmaceutical composition comprising a population of cargo-loaded vesicles wherein at least one pharmaceutically active agent is encapsulated in the core of said vesicles by a surface layer, wherein said surface layer comprises at least one cholesteryl ester obtained from cholesterol and a C8-C26 fatty acid and said ester(s) enable intact vesicles to pass through cell membranes by passive diffusion or facilitated diffusion and thereby arrive in an intact form in the cytoplasm of said cells wherein said pharmaceutically active agents are released in said cytoplasm by the intracellular action of cholesteryl ester hydrolase on the surface layer of said vesicles, said cargo-loaded vesicle being capable of delivering said pharmaceutically active agents within body cells of a patient administered said cargo-loaded vesicles to an intracellular concentration level at least 2 times the level obtainable by said pharmaceutically active agent in the absence of said vesicle.
A pharmaceutical composition in oral dosage form of an enterically coated tablet or capsule for release of said composition at one or more intestinal locations to include duodenum, jejunum, ileum and colon comprising a cargo-loaded vesicle having a neutral surface comprising a core containing a pharmaceutically active agent and a surface layer surrounding said core and said active agent, whereby said surface layer consists of one or more non-ionic cholesteryl esters produced from cholesterol and at least one C8-C26 fatty acid, wherein the mass ratio of the pharmaceutically-active agent to said one or more cholesteryl esters in said cargo-loaded vesicle is between about 4:96 to about 96:4, said cargo-loaded vesicle being capable of delivering said active agent within cells of a patient or subject to a concentration level of at least 2 times to at least 1000 times the level obtainable by oral administration of said pharmaceutically active agent that is not contained in said vesicles.
A pharmaceutical composition in parenteral dosage form comprising a population of cargo-loaded vesicles wherein at least one pharmaceutically active agent is encapsulated in the core of said vesicles by a surface layer, wherein said surface layer comprises at least one cholesteryl ester obtained from cholesterol and a C8-C26 fatty acid and wherein after administration of said vesicles to a patient, said ester(s) enables said vesicles to pass through cell membranes of cells and enter the cytoplasm of said cells wherein said one or more of said pharmaceutically active agents is released into cytoplasm by the intracellular action of cholesteryl ester hydrolase on the surface layer of said vesicles, wherein an intracellular concentration of said active pharmaceutical agents is substantially greater than when said agent is delivered to said cells in the absence of said vesicles.
A pharmaceutical composition adapted for oral administration to the duodenum of a patient or subject comprising a population of cargo-loaded vesicles wherein at least one pharmaceutically active agent is encapsulated in the core of said vesicles by a surface layer, said surface layer consisting essentially of one or more cholesteryl esters, wherein said vesicles are stable to stomach acid and are not broken by cholesteryl ester transporters on the surface of duodenal enterocytes during absorption of said cargo-loaded vesicles after administration to said patient or subject, wherein said cargo-loaded vesicles enter said duodenal enterocytes intact and said duodenal enterocytes add said intact cargo-loaded vesicles into chylomicrons to produce transformed chylomicrons for transport of said cargo-loaded vesicles to body cells of said patient or subject, wherein said composition is optionally enterically coated, wherein the pharmaceutically active agent is at least one agent selected from the group consisting of a hydrophilic peptide, an insulin composition, human growth hormone, prolactin, oxytocin, calcitonin, GLP-1, PYY36, Oxyntomodulin, GLP-2, Glucagon, interferon, ceftaroline, WAP-8924A, vancomycin, bevacizumab, trastuzumab, adalimumab and an anti-PCSK-9 monoclonal antibody.
Dependencies are inferred from the claim text.