Abstract: The present invention includes compositions and methods for making and using a rapid dissolving, high potency, substantially amorphous nanostructured aggregate for pulmonary delivery of tacrolimus and a stabilizer matrix comprising, optionally, a polymeric or non-polymeric surfactant, a polymeric or non-polymeric saccharide or both, wherein the aggregate comprises a surface area greater than 5 m2/g as measured by BET analysis and exhibiting supersaturation for at least 0.5 hours when 11-15-times the aqueous crystalline solubility of tacrolimus is added to simulated lung fluid.

Abstract: The present invention includes compositions and methods for making and using a rapid dissolving, high potency, substantially amorphous nanostructured aggregate for pulmonary delivery of tacrolimus and a stabilizer matrix comprising, optionally, a polymeric or non-polymeric surfactant, a polymeric or non-polymeric saccharide or both, wherein the aggregate comprises a surface area greater than 5 m2/g as measured by BET analysis and exhibiting supersaturation for at least 0.5 hours when 11-15-times the aqueous crystalline solubility of tacrolimus is added to simulated lung fluid.

Abstract: The present invention includes compositions and methods for making and using a rapid dissolving, high potency, substantially amorphous nanostructured aggregate for pulmonary delivery of tacrolimus and a stabilizer matrix comprising, optionally, a polymeric or non-polymeric surfactant, a polymeric or non-polymeric saccharide or both, wherein the aggregate comprises a surface area greater than 5 m2/g as measured by BET analysis and exhibiting supersaturation for at least 0.5 hours when 11-15-times the aqueous crystalline solubility of tacrolimus is added to simulated lung fluid.

Abstract: The present invention includes compositions and methods for making and using a rapid dissolving, high potency, substantially amorphous nanostructured aggregate for pulmonary delivery of tacrolimus and a stabilizer matrix comprising, optionally, a polymeric or non-polymeric surfactant, a polymeric or non-polymeric saccharide or both, wherein the aggregate comprises a surface area greater than 5 m2/g as measured by BET analysis and exhibiting supersaturation for at least 0.5 hours when 11-15-times the aqueous crystalline solubility of tacrolimus is added to simulated lung fluid.

Abstract: A process to produce a dispersion comprising feeding ethylcellulose polymer and a dispersant into a melt and mix zone of an extruder wherein the ethylcellulose polymer and dispersant are melted and mixed together to form a melt; conveying the melt to an emulsification zone of the extruder in which the temperature and pressure are controlled; feeding a base and water into the emulsification zone wherein the melt is dispersed to form a high internal phase emulsion; conveying the emulsion to a dilution and cooling zone of the extruder; and feeding water into the dilution and cooling zone to dilute the high internal phase emulsion thereby forming an aqueous dispersion is provided.

Abstract: A solid dispersion comprising at least one active ingredient in at least one hydroxyalkyl methylcellulose having a DS of from 1.0 to 2.7 and an MS of from 0.40 to 1.30, wherein DS is the degree of substitution of methoxyl groups and MS is the molar substitution of hydroxyalkoxyl groups, can be produced by extrusion or spray-drying.

Abstract: A composition designed for application to a mucosa comprises a tonicity-adjusting agent, a methylcellulose, and a liquid diluent, wherein the methylcellulose has anhydroglucose units joined by 1-4 linkages wherein hydroxy groups of anhydroglucose units are substituted with methyl groups such that s23/s26 is 0.36 or less, wherein s23 is the molar fraction of anhydroglucose units wherein only the two hydroxy groups in the 2- and 3-positions of the anhydroglucose unit are substituted with methyl groups and wherein s26 is the molar fraction of anhydroglucose units wherein only the two hydroxy groups in the 2- and 6-positions of the anhydroglucose unit are substituted with methyl groups.

Abstract: Provided is a method of delivering a drug to a mucosal surface in a living body, said method comprising applying a solution to said mucosal surface, wherein said solution comprises a cationic polymer dissolved in water, wherein said cationic polymer comprises a cationic functional group covalently attached to a polysaccharide polymer backbone selected from the group consisting of amylodextrin polymers, methylcellulose polymers, and hydroxypropyl methylcellulose polymers.

Abstract: Provided is an aqueous composition having pH of 8 or higher and comprising (a) a solid phase comprising dispersed particles that comprise an amount of ethylcellulose polymer, (b) an amount of one or more polymeric dispersants, wherein said polymeric dispersant has a weight-average molecular weight of 5,000 daltons or higher, and wherein said polymeric dispersant has an acid value of 60 to 190 mg KOH/g of polymer. Also provided is a method of making such a composition using an extruder. Also provided is a film made by removing water from such a composition.

Abstract: Provided is an aqueous composition having pH of 8 or higher and comprising (i) a solid phase comprising dispersed particles that comprise ethylcellulose polymer, (ii) fatty acid, wherein 25 mole % to 100 mole % of said fatty acid is in ionic form, (iii) 0% to 0.1% colloid stabilizer, by weight based on the dry weight of said ethylcellulose polymer, (iv) 0% to 7% plasticizer, by weight based on the dry weight of said ethylcellulose polymer, and (v) one or more cations of an alkali metal or an alkaline earth, wherein the equivalent ratio of said cations to said fatty acid is 0.1:1 to 2:1. Also provided are a method of spray drying an aqueous composition and a powder composition.

Abstract: Inhalable compositions are described. The inhalable compositions comprise one or more respirable aggregates, the respirable aggregates comprising one or more poorly water soluble active agents, wherein at least one of the active agents reaches a maximum lung concentration (Cmax) of at least about 0.25 ?g/gram of lung tissue and remains at such concentration for a period of at least one hour after being delivered to the lung. Methods for making such compositions and methods for using such compositions are also disclosed.

Abstract: Provided is an aqueous composition comprising (a) dispersed particles that comprise one or more ethylcellulose polymers and (b) one or more additives having molecular weight less than 220 g/mol, Hansen hydrogen bonding parameter greater than 11 MPa1/2 and less than 17.9 MPa1/2, Hansen total solubility parameter greater than 22 MPa1/2, and solubility in water greater than 2 g/L at 25° C. Also provided is a composition comprising particles having a coating, wherein said coating comprises 0-5% water by weight based on the weight of said coating, wherein said coating additionally comprises the ingredients (a) and (b).

Abstract: The present invention includes compositions and methods for making and using a rapid dissolving, high potency, substantially amorphous nanostructured aggregate for pulmonary delivery of tacrolimus and a stabilizer matrix comprising, optionally, a polymeric or non-polymeric surfactant, a polymeric or non-polymeric saccharide or both, wherein the aggregate comprises a surface area greater than 5 m2/g as measured by BET analysis and exhibiting supersaturation for at least 0.5 hours when 11-15-times the aqueous crystalline solubility of tacrolimus is added to simulated lung fluid.

Abstract: A drug-containing microcapillary film having: (a) a matrix comprising a polymer having a glass transition temperature less than 190° C.; wherein the matrix has a thickness from 5 to 2000 microns; (b) channels disposed in parallel in the matrix, wherein the channels are separated from each other by at least 1 micron, and wherein total cross-sectional area of the channels is from 5 to 70% of total cross-sectional area of the film; and (c) at least one drug disposed in the matrix and/or in the channels.

Abstract: A process to produce a dispersion comprising feeding ethylcellulose polymer and a dispersant into a melt and mix zone of an extruder wherein the ethylcellulose polymer and dispersant are melted and mixed together to form a melt; conveying the melt to an emulsification zone of the extruder in which the temperature and pressure are controlled; feeding a base and water into the emulsification zone wherein the melt is dispersed to form a high internal phase emulsion; conveying the emulsion to a dilution and cooling zone of the extruder; and feeding water into the dilution and cooling zone to dilute the high internal phase emulsion thereby forming an aqueous dispersion is provided.

Abstract: A melt-extruded polymer composition comprising a) at least one cellulose ether, b) one or more active ingredients and c) one or more optional additives, wherein said at least one cellulose ether has an MS (hydroxyalkyl) of 0.05 to 0.55 and hydroxyl groups of anhydroglucose units are substituted with methyl groups such that [s23/s26?0.2*MS(hydroxyalkyl)] is 0.32 or less, wherein s23 is the molar fraction of anhydroglucose units wherein only the two hydroxyl groups in the 2- and 3-positions of the anhydroglucose unit are substituted with a methyl group and wherein s26 is the molar fraction of anhydroglucose units wherein only the two hydroxyl groups in the 2- and 6-positions of the anhydroglucose unit are substituted with a methyl group.

Abstract: A composition designed for application to a mucosa comprises a tonicity-adjusting agent, a hydroxyalkyl methylcellulose and a liquid diluent, wherein the hydroxyalkyl methylcellulose has a DS of from 1.6 to 2.7 and an MS of from 0.40 to 1.30, wherein DS is the degree of substitution of methoxyl groups and MS is the molar substitution of hydroxyalkoxyl groups, and at least 55 weight percent of the liquid diluent is water. When the composition comprises additionally a physiologically active agent, the composition may be used for transmucosal administration of the physiologically active agent to an individual.

Abstract: A composition designed for application to a mucosa comprises a tonicity-adjusting agent, a methylcellulose, and a liquid diluent, wherein the methylcellulose has anhydroglucose units joined by 1-4 linkages wherein hydroxy groups of anhydroglucose units are substituted with methyl groups such that s23/s26 is 0.36 or less, wherein s23 is the molar fraction of anhydroglucose units wherein only the two hydroxy groups in the 2- and 3-positions of the anhydroglucose unit are substituted with methyl groups and wherein s26 is the molar fraction of anhydroglucose units wherein only the two hydroxy groups in the 2- and 6-positions of the anhydroglucose unit are substituted with methyl groups.

Abstract: Inhalable compositions are described. The inhalable compositions comprise one or more respirable aggregates, the respirable aggregates comprising one or more poorly water soluble active agents, wherein at least one of the active agents reaches a maximum lung concentration (Cmax) of at least about 0.25 ?g/gram of lung tissue and remains at such concentration for a period of at least one hour after being delivered to the lung. Methods for making such compositions and methods for using such compositions are also disclosed.

Abstract: The present invention includes compositions and methods for making and using a rapid dissolving, high potency, substantially amorphous nanostructured aggregate for pulmonary delivery of tacrolimus and a stabilizer matrix comprising, optionally, a polymeric or non-polymeric surfactant, a polymeric or non-polymeric saccharide or both, wherein the aggregate comprises a surface area greater than 5 m2/g as measured by BET analysis and exhibiting supersaturation for at least 0.5 hours when 11-15-times the aqueous crystalline solubility of tacrolimus is added to simulated lung fluid.