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.
A61K 9/127 - Vecteurs à bicouches synthétiques, p. ex. liposomes ou liposomes comportant du cholestérol en tant qu’unique agent tensioactif non phosphatidylique
A61K 31/137 - Arylalkylamines, p. ex. amphétamine, épinéphrine, salbutamol, éphédrine
A61K 31/19 - Acides carboxyliques, p. ex. acide valproïque
A61K 31/546 - Composés contenant des systèmes cycliques thia-5 aza-1 bicyclo [4.2.0] octane, c.-à-d. composés contenant un système cyclique de formule , p. ex. céphalosporines, céfaclor, céphalexine contenant d'autres hétérocycles, p. ex. céphalotine
A61K 31/7034 - Composés ayant des radicaux saccharide liés à des composés non-saccharide par des liaisons glycosidiques liés à un composé carbocyclique, p. ex. phloridzine
A61K 31/713 - Acides nucléiques ou oligonucléotides à structure en double-hélice
A61K 38/14 - Peptides contenant des radicaux saccharideLeurs dérivés
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.
A61K 9/127 - Vecteurs à bicouches synthétiques, p. ex. liposomes ou liposomes comportant du cholestérol en tant qu’unique agent tensioactif non phosphatidylique
A61K 31/137 - Arylalkylamines, p. ex. amphétamine, épinéphrine, salbutamol, éphédrine
A61K 31/19 - Acides carboxyliques, p. ex. acide valproïque
A61K 31/546 - Composés contenant des systèmes cycliques thia-5 aza-1 bicyclo [4.2.0] octane, c.-à-d. composés contenant un système cyclique de formule , p. ex. céphalosporines, céfaclor, céphalexine contenant d'autres hétérocycles, p. ex. céphalotine
A61K 31/7034 - Composés ayant des radicaux saccharide liés à des composés non-saccharide par des liaisons glycosidiques liés à un composé carbocyclique, p. ex. phloridzine
A61K 31/713 - Acides nucléiques ou oligonucléotides à structure en double-hélice
A61K 38/14 - Peptides contenant des radicaux saccharideLeurs dérivés
The present invention is directed to one or more macromolecules in a lipid vesicle oral formulation which targets intracellular receptors, in particular for peptides, proteins, nucleic acids and mixtures thereof, optionally in combination with small molecules. The invention encapsulates said macromolecules in a neutral, lipid vesicle comprised of one or more cholesteryl esters. Unique properties of macromolecules encapsulated in said vesicles include high oral bioavailability, defined herein as in at least 50%, i.e., often in excess of 50% on the basis of oral to parenteral AUC. Non-limiting examples are provided, for large hydrophilic molecules such as peptides, proteins and nucleic acids which heretofore have been very poorly absorbed by the mammalian intestine. In prior art, said molecules are generally less than 25% bioavailable, even with protective coatings and optionally absorption enhancing component substances in the formulation. An additional feature of the present invention is high tissue concentrations after oral use, a result of rapid uptake of cholestosomes delivered by chlimicrons to body cells. A preferred embodiment is disclosed for use in the immunotherapy of cancer.
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.
A61K 9/127 - Vecteurs à bicouches synthétiques, p. ex. liposomes ou liposomes comportant du cholestérol en tant qu’unique agent tensioactif non phosphatidylique
A61K 31/137 - Arylalkylamines, p. ex. amphétamine, épinéphrine, salbutamol, éphédrine
A61K 31/19 - Acides carboxyliques, p. ex. acide valproïque
A61K 31/546 - Composés contenant des systèmes cycliques thia-5 aza-1 bicyclo [4.2.0] octane, c.-à-d. composés contenant un système cyclique de formule , p. ex. céphalosporines, céfaclor, céphalexine contenant d'autres hétérocycles, p. ex. céphalotine
A61K 31/7034 - Composés ayant des radicaux saccharide liés à des composés non-saccharide par des liaisons glycosidiques liés à un composé carbocyclique, p. ex. phloridzine
A61K 31/713 - Acides nucléiques ou oligonucléotides à structure en double-hélice
A61K 38/14 - Peptides contenant des radicaux saccharideLeurs dérivés
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.
A61K 9/127 - Vecteurs à bicouches synthétiques, p. ex. liposomes ou liposomes comportant du cholestérol en tant qu’unique agent tensioactif non phosphatidylique
A61K 31/137 - Arylalkylamines, p. ex. amphétamine, épinéphrine, salbutamol, éphédrine
A61K 31/19 - Acides carboxyliques, p. ex. acide valproïque
A61K 31/546 - Composés contenant des systèmes cycliques thia-5 aza-1 bicyclo [4.2.0] octane, c.-à-d. composés contenant un système cyclique de formule , p. ex. céphalosporines, céfaclor, céphalexine contenant d'autres hétérocycles, p. ex. céphalotine
A61K 31/7034 - Composés ayant des radicaux saccharide liés à des composés non-saccharide par des liaisons glycosidiques liés à un composé carbocyclique, p. ex. phloridzine
A61K 31/713 - Acides nucléiques ou oligonucléotides à structure en double-hélice
A61K 38/14 - Peptides contenant des radicaux saccharideLeurs dérivés
The invention broadly comprises a chemical composition including a plurality of cholesteryl esters arranged to form a vesicle. In several embodiments, all of the plurality of cholesteryl esters have a same molecular length, which in some embodiments provides a vesicle having a generally smooth outer surface, while in other embodiments, a portion of the plurality of cholesteryl esters have different molecular lengths, which in some embodiments provides a vesicle having a generally irregular outer surface. In yet further embodiments, a shape of the vesicle is selected from the group consisting of spherical, oval, disc-like, tubular and polyhedral shapes, and in yet other embodiments, a wall of the vesicle is selected from the group consisting of a monolayer and a bilayer. In still further embodiments, the chemical composition further includes a polyethylene glycol coat of mixed polymer size. In some embodiments, the plurality of cholesteryl esters include at least two different cholesteryl esters, and in some of these embodiments, the at least two different cholesteryl esters are selected from the group consisting of cholesteryl myristate, cholesteryl laurate, cholesteryl dodeconate, cholesteryl palmitate, cholesteryl arachidonate, cholesteryl behenate, cholesteryl linoleate, cholesteryl linolenate, cholesteryl oleate and cholesteryl stearate.
A61K 9/127 - Vecteurs à bicouches synthétiques, p. ex. liposomes ou liposomes comportant du cholestérol en tant qu’unique agent tensioactif non phosphatidylique
A61K 47/10 - AlcoolsPhénolsLeurs sels, p. ex. glycérolPolyéthylène glycols [PEG]PoloxamèresAlkyléthers de PEG/POE
A61K 47/28 - Stéroïdes, p. ex. cholestérol, acides biliaires ou acide glycyrrhétinique
A61K 38/17 - Peptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'animauxPeptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'humains
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.
A61K 31/7034 - Composés ayant des radicaux saccharide liés à des composés non-saccharide par des liaisons glycosidiques liés à un composé carbocyclique, p. ex. phloridzine
A61K 31/713 - Acides nucléiques ou oligonucléotides à structure en double-hélice
A61K 39/395 - AnticorpsImmunoglobulinesImmunsérum, p. ex. sérum antilymphocitaire
A61K 31/546 - Composés contenant des systèmes cycliques thia-5 aza-1 bicyclo [4.2.0] octane, c.-à-d. composés contenant un système cyclique de formule , p. ex. céphalosporines, céfaclor, céphalexine contenant d'autres hétérocycles, p. ex. céphalotine
A61K 9/127 - Vecteurs à bicouches synthétiques, p. ex. liposomes ou liposomes comportant du cholestérol en tant qu’unique agent tensioactif non phosphatidylique
The invention broadly comprises a chemical composition including a plurality of cholesteryl esters arranged to form a vesicle. In several embodiments, all of the plurality of cholesteryl esters have a same molecular length, which in some embodiments provides a vesicle having a generally smooth outer surface, while in other embodiments, a portion of the plurality of cholesteryl esters have different molecular lengths, which in some embodiments provides a vesicle having a generally irregular outer surface. In yet further embodiments, a shape of the vesicle is selected from the group consisting of spherical, oval, disc-like, tubular and polyhedral shapes, and in yet other embodiments, a wall of the vesicle is selected from the group consisting of a monolayer and a bilayer. In still further embodiments, the chemical composition further includes a polyethylene glycol coat of mixed polymer size. In some embodiments, the plurality of cholesteryl esters include at least two different cholesteryl esters, and in some of these embodiments, the at least two different cholesteryl esters are selected from the group consisting of: cholesteryl myristate, cholesteryl laurate, cholesteryl dodeconate, cholesteryl palmitate, cholesteryl arachidonate, cholesteryl behenate, cholesteryl linoleate, cholesteryl linolenate, cholesteryl oleate and cholesteryl stearate.
A61K 9/127 - Vecteurs à bicouches synthétiques, p. ex. liposomes ou liposomes comportant du cholestérol en tant qu’unique agent tensioactif non phosphatidylique
A61K 47/10 - AlcoolsPhénolsLeurs sels, p. ex. glycérolPolyéthylène glycols [PEG]PoloxamèresAlkyléthers de PEG/POE
A61K 47/28 - Stéroïdes, p. ex. cholestérol, acides biliaires ou acide glycyrrhétinique
A61K 38/17 - Peptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'animauxPeptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'humains
The present invention may be embodied as a retrievable device capable of sensing one or more properties of an individual (e.g., chemical or physical parameters, etc.) In use, the retrievable device can continuously determine the chemical concentrations within the vaginal tract. An embodiment of the retrievable device comprises a first housing having a light source and an image capture device, a second housing removably connected to the first housing and having a sensor, and a fitting for retrieving the device. The sensor may be an analyte sensor configured to obtain at least one measurement of a concentration of an analyte in a fluid. The analyte sensor comprises a sensor substance in a sol-gel material so the sensor substance reversibly interacts with an analyte of interest. In addition, the retrievable device can be configured to determine different physical parameters and re-implanted.
A61B 1/00 - Instruments pour procéder à l'examen médical de l'intérieur des cavités ou des conduits du corps par inspection visuelle ou photographique, p. ex. endoscopesDispositions pour l'éclairage dans ces instruments
A61B 1/303 - Instruments pour procéder à l'examen médical de l'intérieur des cavités ou des conduits du corps par inspection visuelle ou photographique, p. ex. endoscopesDispositions pour l'éclairage dans ces instruments pour le vagin, c.-à-d. vaginoscopes
A61B 1/04 - Instruments pour procéder à l'examen médical de l'intérieur des cavités ou des conduits du corps par inspection visuelle ou photographique, p. ex. endoscopesDispositions pour l'éclairage dans ces instruments combinés avec des dispositifs photographiques ou de télévision
A61B 1/05 - Instruments pour procéder à l'examen médical de l'intérieur des cavités ou des conduits du corps par inspection visuelle ou photographique, p. ex. endoscopesDispositions pour l'éclairage dans ces instruments combinés avec des dispositifs photographiques ou de télévision caractérisés par le fait que le capteur d'images, p. ex. l'appareil photographique, est placé dans la partie de l'extrémité distale
A61B 1/06 - Instruments pour procéder à l'examen médical de l'intérieur des cavités ou des conduits du corps par inspection visuelle ou photographique, p. ex. endoscopesDispositions pour l'éclairage dans ces instruments avec dispositifs d'éclairement
The present invention may be embodied as a retrievable device capable of sensing one or more properties of an individual (e.g., chemical or physical parameters, etc.) In use, the retrievable device can continuously determine the chemical concentrations within the vaginal tract. An embodiment of the retrievable device comprises a first housing having a light source and an image capture device, a second housing removably connected to the first housing and having a sensor, and a fitting for retrieving the device. The sensor may be an analyte sensor configured to obtain at least one measurement of a concentration of an analyte in a fluid. The analyte sensor comprises a sensor substance in a sol-gel material so the sensor substance reversibly interacts with an analyte of interest. In addition, the retrievable device can be configured to determine different physical parameters and re-implanted.
A61B 1/04 - Instruments pour procéder à l'examen médical de l'intérieur des cavités ou des conduits du corps par inspection visuelle ou photographique, p. ex. endoscopesDispositions pour l'éclairage dans ces instruments combinés avec des dispositifs photographiques ou de télévision
11.
A DEVICE AND METHOD FOR CONTINUOUS CHEMICAL SENSING
The present invention may be embodied as an ingestible device capable of sensing one or more chemical parameters. In use, the device can continuously determine the chemical concentrations within an alimentary canal tract. An embodiment of the device comprises a housing resistant to degradation by alimentary canal fluid, a light source, and image capture device. An analyte sensor is configured to obtain at least one measurement of a concentration of analyte in the fluid. The analyte sensor comprises a sensor substance in a sol-gel material so the sensor substance reversibly interacts with an analyte of interest. In addition, the analyte sensor is configured to generate a trigger signal for controlling the operation of subsystems in the device.
A61B 5/05 - Détection, mesure ou enregistrement pour établir un diagnostic au moyen de courants électriques ou de champs magnétiquesMesure utilisant des micro-ondes ou des ondes radio
A61B 5/103 - Dispositifs de mesure pour le contrôle de la forme, du dessin, de la dimension ou du mouvement du corps ou de parties de celui-ci, à des fins de diagnostic
brevets
