Orally bioavailable lipid-based constructs
Inventors
Assignees
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Publication Number
US-8962015-B2
Publication Date
2015-02-24
Expiration Date
Abstract
The present invention is embodied by a composition capable of chaperoning a typically non-orally available therapeutic or diagnostic agent through the environment of the digestive tract such that the therapeutic or diagnostic agent is bioavailable. The composition may or may not be targeted to specific cellular receptors, such as hepatocytes. Therapeutic agents include, but are not limited to, insulin, calcitonin, serotonin, and other proteins. Targeting is accomplished with biotin or metal based targeting agents.
Core Innovation
The invention relates to an orally bioavailable composition comprising gelatin and additional constituents that comprise a liposome, a liposome fragment, and a lipid particle. The composition includes insulin and a biotin-derived targeting agent selected from biotin-X-DHPE and biotin-DHPE, and gelatin reversibly interacts with one or more of the constituents.
A percentage ranging from 5% to 50% of the additional constituents exhibits an average diameter equal to or lower than 20 nanometers. The orally bioavailable composition is directed to enabling passage through intercellular gaps through dynamically sized constituents, with the gelatin reversibly interacting with these dynamically sized liposome, liposome-fragment, and lipid-particle structures.
The lipid components are described as dihexadecyl phosphate, 1,2 distearoyl-sn-glycero-3-phosphocholine, and cholesterol. The disclosed materials further include biotin-derived targeting agents such as biotin-DHPE and biotin-X-DHPE, and gelatin is reversibly associated with the liposomes, liposome fragments, and particles.
Claims Coverage
Two independent claims are identified. Both independent claims share core inventive elements: an orally bioavailable gelatin-associated system that includes insulin, a biotin-derived targeting agent, reversibly interacting gelatin with liposomes, liposome fragments, and lipid particles, and a diameter constraint where 5% to 50% of the relevant constituents have an average diameter equal to or lower than 20 nanometers.
Orally bioavailable gelatin-associated liposome, liposome fragment, and lipid particle composition with insulin and biotin-derived targeting agent
An orally bioavailable composition comprising gelatin and additional constituents including a liposome, a liposome fragment, and a lipid particle; wherein the composition comprises insulin and a biotin-derived targeting agent selected from the group consisting of biotin-X-DHPE and biotin-DHPE; wherein gelatin reversibly interacts with one or more of said constituents; wherein 5% to 50% of said additional constituents exhibits an average diameter equal to or lower than 20 nanometers; and wherein the lipid components comprise dihexadecyl phosphate, 1,2 distearoyl-sn-glycero-3-phosphocholine, and cholesterol.
Method of making an orally bioavailable gelatin-associated composition with insulin, biotin-derived targeting agent, and ≤20 nm fraction
A composition of the invention prepared by a method comprising mixing dihexadecyl phosphate, 1,2 distearoyl-sn-glycero-3-phosphocholine, cholesterol, and a biotin-derived targeting agent selected from biotin-X-DHPE and biotin-DHPE in aqueous media to form a first mixture; subjecting the mixture to homogenization to form a mixture of liposomes, liposome fragments, and particles; adding insulin to form a second mixture; adding the second mixture to gelatin to form a gelatin-associated mixture; and drying to yield the composition, wherein gelatin reversibly interacts with one or more of said liposomes, liposome fragments, and particles; wherein in said composition 5% to 50% of said mixture of liposomes, liposome fragments, and particles exhibits an average diameter equal to or lower than 20 nanometers; and wherein the composition is orally bioavailable in a mammal.
Across both independent claims, the inventive scope is centered on an orally bioavailable gelatin-associated composition containing insulin and a biotin-derived targeting agent associated with liposomes, liposome fragments, and lipid particles that include specified lipid components and have a defined ≤20 nm average-diameter fraction (5% to 50%), with gelatin reversibly interacting with the lipid-based constituents.
Stated Advantages
Orally bioavailable in a mammal.
A percentage ranging from 5% to 50% of the additional constituents exhibits an average diameter equal to or lower than 20 nanometers.
Gelatin reversibly interacts with one or more of the liposomes, liposome fragments, and particles.
Documented Applications
Oral delivery of therapeutics/diagnostics through the digestive tract as described for an orally bioavailable gelatin-associated composition.
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