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AssigneeBrown University Research Foundation
InventorsEdith Mathiowitz, Donald Chickering, III, Jules S. Jacob
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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.
A drug formulation comprising drug encapsulated within a microsphere having a diameter between about 1 μm 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.
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,
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 μm 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.
Dependencies are inferred from the claim text.