Novel formulation for the elimination of cariogenic and opportunistic pathogens within the oral cavity

Abstract

Provided herein are microspheres containing an antimicrobial agent encapsulated within a glycosidic polymer and use thereof, especially to inhibit the growth of carie-causing organisms.

1 . A microsphere comprising an antimicrobial agent encapsulated within a glycosidic polymer. 
     
     
         2 . The microsphere of  claim 1 , wherein the glycosidic polymer comprises an insoluble cross-linked dextran. 
     
     
         3 . The microsphere of  claim 2 , wherein the insoluble cross-linked dextran comprises cross-linked dextran (dextranomer or Sephadex) or a mimetic thereof. 
     
     
         4 . The microsphere of  claim 1 , wherein the antimicrobial agent comprises one or more from the group of hydrogen peroxide, chlorhexidine, penicillin, streptomycin, erythromycin, xylitol, fluoride, triclosan, alcohol, and cetylpyridinium chloride. 
     
     
         5 . The microsphere of  claim 1 , wherein the microsphere has a diameter from about 1 μm (wet size) to about 1000 μm (wet size). 
     
     
         6 . A microsphere of  claim 1  and a carrier and optionally one or more of a flavoring agent, a color, a preservative, a buffer, and a stabilizer. 
     
     
         7 . The microsphere of  claim 1 , wherein the surface area of the microsphere is from about 6×10 7  μm2 to about 6×10 8  μm2 per mg of glycosidic polymer. 
     
     
         8 . The microsphere of  claim 1 , wherein the concentration of an antimicrobial liquid is from about 1 mg/pito about 3 mg/μ0.1 of carrier in the microsphere (prior to processing of the microsphere). 
     
     
         9 . The microsphere of  claim 7 , wherein the concentration of an antimicrobial liquid is from about 1 mg/μ1 to about 3 mg/μ1 of carrier in the microsphere (prior to processing of the microsphere). 
     
     
         10 . The microsphere of  claim 1 , wherein the glycosidic polymer comprises G25-superfine Sephadex. 
     
     
         11 . The microsphere of  claim 4 , wherein the glycosidic polymer comprises G25-superfine Sephadex. 
     
     
         12 . The microsphere of  claim 7 , wherein the glycosidic polymer comprises G25-superfine Sephadex. 
     
     
         13 . A composition comprising a plurality of the microspheres of  claim 1 . 
     
     
         14 . A composition comprising a plurality of the microspheres of  claim 7 . 
     
     
         15 . A composition comprising a plurality of the microspheres of  claim 9 . 
     
     
         16 . The composition of  claim 13 , wherein the plurality of the microspheres have the same or different diameter and/or the same or different antimicrobial agent. 
     
     
         17 . The composition of  claim 14 , wherein the plurality of the microspheres have the same or different diameter and/or the same or different antimicrobial agent. 
     
     
         18 . The composition of  claim 15 , wherein the plurality of the microspheres have the same or different diameter and/or the same or different antimicrobial agent. 
     
     
         19 . The composition of  claim 13 , wherein the composition is formulated as a solid, a semi-solid, or a liquid, and optionally as a gum, a gel, a toothpaste, a mouthwash, a lozenge, or a tablet, a chewable tablet, a suspension, a dissolvable lozenge, or a fluoride rinse. 
     
     
         20 . The composition of  claim 14 , wherein the composition is formulated as a solid, a semi-solid, or a liquid, and optionally as a gum, a gel, a toothpaste, a mouthwash, a lozenge, or a tablet, a chewable tablet, a suspension, a dissolvable lozenge, or a fluoride rinse. 
     
     
         21 . The composition of  claim 15 , wherein the composition is formulated as a solid, a semi-solid, or a liquid, and optionally as a gum, a gel, a toothpaste, a mouthwash, a lozenge, or a tablet, a chewable tablet, a suspension, a dissolvable lozenge, or a fluoride rinse. 
     
     
         22 . The composition of  claim 16 , wherein the composition is formulated as a solid, a semi-solid, or a liquid, and optionally as a gum, a gel, a toothpaste, a mouthwash, a lozenge, or a tablet, a chewable tablet, a suspension, a dissolvable lozenge, or a fluoride rinse. 
     
     
         23 . The composition of  claim 17 , wherein the composition is formulated as a solid, a semi-solid, or a liquid, and optionally as a gum, a gel, a toothpaste, a mouthwash, a lozenge, or a tablet, a chewable tablet, a suspension, a dissolvable lozenge, or a fluoride rinse. 
     
     
         24 . The composition of  claim 18 , wherein the composition is formulated as a solid, a semi-solid, or a liquid, and optionally as a gum, a gel, a toothpaste, a mouthwash, a lozenge, or a tablet, a chewable tablet, a suspension, a dissolvable lozenge, or a fluoride rinse. 
     
     
         25 . The composition of  claim 12 , wherein the composition is formulated as a gum, a gel, a toothpaste, a mouthwash, a lozenge, or a tablet, a chewable tablet, a suspension, a dissolvable lozenge, or a fluoride rinse. 
     
     
         26 . A method for selectively inhibiting the growth of, and/or selectively removing carie-causing organisms from the oral cavity in a subject, comprising administering to the oral cavity of the subject an effective amount of the composition of  claim 16 , thereby inhibiting the growth of, and/or selectively removing carie-causing organisms from the oral cavity. 
     
     
         27 . A method for selectively inhibiting the growth of, and/or selectively removing carie-causing organisms from the oral cavity in a subject, comprising administering to the oral cavity of the subject an effective amount of the composition of  claim 17 , thereby inhibiting the growth of, and/or selectively removing carie-causing organisms from the oral cavity. 
     
     
         28 . A method for treating and/or preventing infective endocarditis (IE) in a subject, comprising administering to the oral cavity of the subject in need thereof, an effective amount of the formulation of  claim 16 , thereby treating and/or preventing infective endocarditis. 
     
     
         29 . A method for treating and/or preventing infective endocarditis (IE) in a subject, comprising administering to the oral cavity of the subject in need thereof, an effective amount of the formulation of  claim 17 , thereby treating and/or preventing infective endocarditis. 
     
     
         30 . The method of  claim 26 , wherein the carie-causing organism is selected from the group of  S. mutans, S. sobrinus, S. oralis, S. gordonii, S. sanguis, S. mitis, S. salivarius, S. cristatus , or combinations thereof. 
     
     
         31 . The method of  claim 27 , wherein the carie-causing organism is selected from the group of  S. mutans, S. sobrinus, S. oralis, S. gordonii, S. sanguis, S. mitis, S. salivarius, S. cristatus , or combinations thereof. 
     
     
         32 .- 35 . (canceled) 
     
     
         36 . A kit comprising the microsphere of  claim 1 , and instructions for use in the methods as disclosed herein 
     
     
         37 . A kit comprising the microsphere of  claim 7 , and instructions for use in the methods as disclosed herein.