Coated Controlled Release Polymer Particles as Efficient Oral Delivery Vehicles for Biopharmaceuticals
First Claim
1. A composition for delivering an active agent to a patient, comprising:
- a polymer core encapsulating a predetermined amount of the active agent; and
a mucoadhesive coating disposed about the core to form a coated particle, whereinthe polymer is derivatized with a poly(alkylene glycol), the mucoadhesive coating is retained on the core through one or more of covalent interactions, electrostatic interactions, affinity interactions, metal coordination, physical adsorption, host-guest interactions, and hydrogen bonding interactions,a molecular weight and cross-link density of the polymer is selected such that the polymer core will decompose in a predetermined time interval,the mucoadhesive coating is selected to facilitate transfer of the particle through the intestinal mucosa, anda fraction of the predetermined amount of the active agent entering the systemic circulation during the predetermined time interval is between about 0.25% and about 25%.
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Accused Products
Abstract
A composition for delivering an active agent to a patient. The composition includes a polymer core encapsulating the active agent and a mucoadhesive coating disposed about the core. The polymer may include covalently linked poly(ethylene glycol) chains, and the mucoadhesive coating may be selected to facilitate transfer of the particle through the intestinal mucosa. A molecular weight and cross-link density of the polymer may be selected such that the polymer core will decompose in a predetermined time interval. The fraction of the dose of the drug entering the system at circulation during the predetermined time interval may be between about 0.25% and about 25%. The composition may be formulated as a plurality of nanoparticles or microparticles that are combined with a pharmaceutically acceptable carrier to produce an edible or inhalable drug product.
171 Citations
90 Claims
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1. A composition for delivering an active agent to a patient, comprising:
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a polymer core encapsulating a predetermined amount of the active agent; and a mucoadhesive coating disposed about the core to form a coated particle, wherein the polymer is derivatized with a poly(alkylene glycol), the mucoadhesive coating is retained on the core through one or more of covalent interactions, electrostatic interactions, affinity interactions, metal coordination, physical adsorption, host-guest interactions, and hydrogen bonding interactions, a molecular weight and cross-link density of the polymer is selected such that the polymer core will decompose in a predetermined time interval, the mucoadhesive coating is selected to facilitate transfer of the particle through the intestinal mucosa, and a fraction of the predetermined amount of the active agent entering the systemic circulation during the predetermined time interval is between about 0.25% and about 25%. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29)
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30. A composition for administering an active agent to a patient, comprising:
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a plurality of particles, each particle comprising a polymer core encapsulating a predetermined amount of the active agent and a mucoadhesive coating disposed about the core to form a coated particle; and a pharmaceutically acceptable carrier combined with the plurality of particles, wherein the pharmaceutically acceptable carrier is edible or inhalable, wherein; the mucoadhesive coating is retained on the core through one or more of covalent interactions, electrostatic interactions, affinity interactions, metal coordination, physical adsorption, host-guest interactions, and hydrogen bonding interactions, a molecular weight and cross-link density of the biodegradable polymer is selected such that the polymer core will decompose in vivo in a predetermined time interval, and a fraction of the predetermined amount of the bioactive agent entering the systemic circulation during the predetermined time interval is between about 0.25% and about 25%. - View Dependent Claims (31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59)
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60. A method for administering an active agent to a patient, comprising:
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orally or nasally administering to the patient a composition comprising; A) a plurality of particles, each particle comprising; a polymer core encapsulating a predetermined amount of the active agent; and a mucoadhesive coating disposed about the core to form a coated particle; and B) a pharmaceutically acceptable carrier, wherein the pharmaceutically acceptable carrier is edible or inhalable, wherein the mucoadhesive coating is retained on the core through one or more of covalent interactions, electrostatic interactions, affinity interactions, metal coordination, physical adsorption, host-guest interactions, and hydrogen bonding interactions, a molecular weight and cross-link density of the polymer is selected such that the polymer core will decompose in vivo in a predetermined time interval, and a fraction of the predetermined amount of the bioactive agent entering the systemic circulation during the predetermined time interval is between about 0.25% and about 25%. - View Dependent Claims (61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90)
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Specification