Coated controlled release polymer particles as efficient oral delivery vehicles for biopharmaceuticals
First Claim
1. A composition comprising(i) a plurality of nanoparticles having a diameter between about 10 nm and 1000 nm, the nanoparticles comprising(a) an amphiphilic block co-polymer core encapsulating an active agent,(b) a mucoadhesive coating comprising a material selected from the group consisting of lectins and positively charged polymers, the coating being present on the core and interacting through electrostatic interactions with the amphiphilic block co-polymer to form a coated nanoparticle, and(c) a targeting agent;
- and(ii) a pharmaceutically acceptable carrier.
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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.
375 Citations
52 Claims
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1. A composition comprising
(i) a plurality of nanoparticles having a diameter between about 10 nm and 1000 nm, the nanoparticles comprising (a) an amphiphilic block co-polymer core encapsulating an active agent, (b) a mucoadhesive coating comprising a material selected from the group consisting of lectins and positively charged polymers, the coating being present on the core and interacting through electrostatic interactions with the amphiphilic block co-polymer to form a coated nanoparticle, and (c) a targeting agent; - and
(ii) a pharmaceutically acceptable carrier. - 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, 52)
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27. A method for administering an active agent to an individual, comprising:
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orally or nasally administering to the patient a composition comprising; (i) a plurality of nanoparticles having a size between about 10 nm and 1000 nm, the nanoparticles comprising (a) an amphiphilic block co-polymer core encapsulating active agent; (b) a mucoadhesive coating comprising a material selected from the group consisting of lectins and positively charged polymers, the coating present on the amphiphilic block co-polymer core and interacting through electrostatic interactions with the amphiphilic polymer to form a coated nanoparticle, and (c) a targeting agent; and (ii) a pharmaceutically acceptable carrier. - View Dependent Claims (28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51)
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Specification