Bioadhesive microspheres and their use as drug delivery and imaging systems
First Claim
1. A drug formulation comprising drug encapsulated within a microsphere having a diameter between about 1 μ
- m and 5 mm and a synthetic polymeric surface with a composition and morphology providing a sufficient concentration of carboxylic acid end groups at the surface, such that the surface adhesive force is equivalent to an adhesive force of between 110 N/m2 and 100,000 N/m2 measured on rat intestine.
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Accused Products
Abstract
Bioadhesive polymers in the form of, or as a coating on, microcapsules containing drugs or bioactive substances which may serve for therapeutic, or diagnostic purposes in diseases of the gastrointestinal tract, are described. The polymeric microspheres all have a bioadhesive force of at least 11 mN/cm2 (110 N/m2). Techniques for the fabrication of bioadhesive microspheres, as well as a method for measuring bioadhesive forces between microspheres and selected segments of the gastrointestinal tract in vitro are also described. This quantitative method provides a means to establish a correlation between the chemical nature, the surface morphology and the dimensions of drug-loaded microspheres on one hand and bioadhesive forces on the other, allowing the screening of the most promising materials from a relatively large group of natural and synthetic polymers which, from theoretical consideration, should be used for making bioadhesive microspheres.
307 Citations
20 Claims
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1. A drug formulation comprising drug encapsulated within a microsphere having a diameter between about 1 μ
- m and 5 mm and a synthetic polymeric surface with a composition and morphology providing a sufficient concentration of carboxylic acid end groups at the surface, such that the surface adhesive force is equivalent to an adhesive force of between 110 N/m2 and 100,000 N/m2 measured on rat intestine.
- View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 13, 14)
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12. A drug formulation comprising drug encapsulated within a microsphere having a polymeric surface with an adhesive force equivalent to an adhesive force of between 110 N/m2 and 100,000 N/m2 measured on rat intestine,
wherein the polymer is a hydrogel modified by a compound that enhances binding, which compound is selected from the group consisting of sialic acid, neuraminic acid, n-acetyl-neuraminic acid, n-glycolylneuraminic acid, 4-acetyl-n-acetylneuraminic acid, diacetyl-n-acetylneuraminic acid, glucuronic acid, iduronic acid, galactose, glucose, mannose, fucose, mucoproteins, mucopolysaccharides, mucopolysaccharide-protein complexes, lectins, and antibodies immunoreactive against proteins on the mucosal surface.
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15. A method for delivering a drug comprising administering to a mucosal surface a drug formulation comprising drug encapsulated within a microsphere having a diameter between about 1 μ
- m and 5 mm and a synthetic polymeric surface with a composition and morphology providing a sufficient concentration of carboxylic acid end groups at the surface, such that the surface adhesive force is equivalent to an adhesive force of between 110 N/m2 and 100,000 N/m2 measured on rat intestine, in combination with a pharmaceutical carrier.
- View Dependent Claims (16, 17, 18, 19, 20)
Specification