Polymeric compositions containing ambient-temperature stable biopharmaceuticals and methods for formulation thereof
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Publication Number
US-10272033-B2
Publication Date
2019-04-30
Expiration Date
Abstract
Biopharmaceuticals, such as vaccine agents and probiotics, are encapsulated in carbohydrate-glass particles and embedded in an amorphous polymer substrate to produce polymeric compositions containing ambient-temperature stable biopharmaceuticals for syringeless administration to patients such as via dissolvable films, micro-needle patches and similar medical delivery devices. The amorphous polymer substrate is soluble in both water and volatile organic solvents, yet the carbohydrate-glass particles are insoluble in organic solvents. A method for formulation of the polymeric compositions containing ambient-temperature stable biopharmaceuticals includes combining biopharmaceuticals encapsulated in carbohydrate-glass particles with polymer in organic solvent and evaporating the organic solvent to yield a water soluble polymeric composition containing ambient-temperature stable biopharmaceuticals.
Core Innovation
The invention relates to a method for preparing delivery devices from water-soluble polymeric compositions containing ambient-temperature stable biopharmaceuticals. One or more biopharmaceuticals are immobilized in carbohydrate-glass and the carbohydrate-glass is micronized to form a carbohydrate-glass powder containing the biopharmaceuticals. The carbohydrate-glass powder is subsequently introduced into a polymer solution in which it is not dissolved.
The method includes identifying and selecting one or more bi-soluble polymeric excipients and a volatile organic solvent. The polymeric excipients are soluble in both water and the volatile organic solvent, while the volatile organic solvent is selected as one that does not dissolve the carbohydrate-glass powder. The bi-soluble polymeric excipients and one or more plasticizers are dissolved in the volatile organic solvent to form the polymer solution, and the carbohydrate-glass powder is introduced into the polymer solution.
The polymer solution is cast to produce either a polymeric film or a water dissolvable micro-needle patch, followed by evaporating the organic solvent to form the film or patch. The film is configured for water-soluble mucosal delivery, and the micro-needle patch is configured for water-soluble transdermal delivery to a patient. The invention is positioned around ambient-temperature stable biopharmaceuticals that can be preserved for needle-free delivery by incorporating vaccine agents or probiotics into carbohydrate-glass and embedding them in the amorphous polymer substrate formed by organic solvent evaporation.
Claims Coverage
The provided excerpt includes two independent claims. Across both independent claims, the core inventive features are directed to immobilizing biopharmaceuticals in micronized carbohydrate-glass, selecting bi-soluble polymeric excipients and a volatile organic solvent that does not dissolve the carbohydrate-glass, forming a polymer solution with plasticizers, casting into a polymeric film or a water dissolvable micro-needle patch, and evaporating the organic solvent to enable mucosal or transdermal delivery.
Micronized carbohydrate-glass immobilization of ambient-temperature stable biopharmaceuticals
Immobilizing one or more biopharmaceuticals in carbohydrate-glass and micronizing the carbohydrate-glass to form a carbohydrate-glass powder containing said biopharmaceuticals.
Selecting bi-soluble polymeric excipients and a volatile organic solvent that does not dissolve carbohydrate-glass powder
Identifying and selecting one or more bi-soluble polymeric excipients and a volatile organic solvent, wherein the one or more bi-soluble polymeric excipients is/are selected as being soluble in both water and the volatile organic solvent, and wherein the volatile organic solvent is selected as one that does not dissolve the carbohydrate-glass powder.
Forming a polymer solution with bi-soluble excipients and plasticizers, then introducing carbohydrate-glass powder
Dissolving the one or more bi-soluble polymeric excipients and one or more plasticizers in the volatile organic solvent to form a polymer solution, and introducing said carbohydrate-glass powder containing said biopharmaceuticals into said polymer solution.
Casting into polymeric film or water dissolvable micro-needle patch and evaporating organic solvent for mucosal/transdermal delivery
Casting said polymer solution containing the carbohydrate-glass powder to produce a polymeric film, or a water dissolvable micro-needle patch, and evaporating the organic solvent from said polymer solution containing said carbohydrate-glass powder to form the film or patch, wherein the film or patch is configured for water-soluble mucosal or transdermal delivery, respectively, for delivering said one or more biopharmaceuticals to a patient.
Acetone-soluble bi-soluble excipients and triacetin polymer solution that does not dissolve carbohydrate-glass powder
Identifying and selecting one or more bi-soluble polymeric excipients, wherein the one or more bi-soluble polymeric excipients is/are selected as being soluble in both water and acetone, wherein the one or more polymeric excipients is selected from the group consisting of hydroxypropyl cellulose, cellulose acetate or a combination thereof; dissolving the one or more bi-soluble polymeric excipients and triacetin in acetone to form a polymer solution; and introducing the carbohydrate-glass powder containing the biopharmaceuticals into the polymer solution, wherein the carbohydrate-glass powder is not dissolved in the polymer solution.
Casting acetone-based polymer solution into film or water dissolvable micro-needle patch and evaporating acetone
Casting the polymer solution to produce a polymeric film, or a water dissolvable micro-needle patch, and evaporating the acetone from the polymer solution containing said carbohydrate-glass powder.
Both independent claims share a common inventive architecture: biopharmaceuticals immobilized in micronized carbohydrate-glass are combined with bi-soluble polymeric excipients and a volatile organic solvent that does not dissolve the carbohydrate-glass, then cast into either a polymeric film for water-soluble mucosal delivery or a water dissolvable micro-needle patch for water-soluble transdermal delivery. The second independent claim specifies an acetone/triacetin system with specific bi-soluble polymeric excipients and expressly requires that the carbohydrate-glass powder not be dissolved in the polymer solution before casting and evaporating acetone.
Stated Advantages
Preservation enables ambient-temperature stable biopharmaceuticals for delivery.
Needle-free delivery via water-soluble mucosal or water-soluble transdermal delivery using polymeric films or water dissolvable micro-needle patches.
Solvent selection enables formation of water-soluble devices by evaporating the organic solvent without dissolving the carbohydrate-glass powder.
PBV/PFF foam drying is positioned as enabling thermostable preserved powders compared to freeze-drying and spray-drying.
Biopharmaceutical survival/activity is maintained after drying and storage.
Documented Applications
Water-soluble mucosal delivery of the one or more biopharmaceuticals to a patient using a polymeric film.
Water-soluble transdermal delivery of the one or more biopharmaceuticals to a patient using a water dissolvable micro-needle patch.
Needle-free delivery of ambient-temperature stable biopharmaceuticals including vaccine agents or probiotics.
Use of PBV/PFF foam drying to enable thermostable preserved powders of the biopharmaceuticals for incorporation into the water-soluble delivery devices.
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