Dental varnishes that release specifically targeted antimicrobial peptides and/or fluoride
Inventors
Schauer, Evan • Baudys, Miroslav • Varnum, Brian C. • Kaplan, Christopher W. • Eckert, Randal H. • Turetzky, Jay • Soriaga, Angela
Assignees
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Publication Number
US-11633341-B2
Publication Date
2023-04-25
Expiration Date
Abstract
In various embodiments a dental varnish system having improved peptide release and fluoride release properties is provided. In various embodiments a dental varnish system that provides release of an antimicrobial peptide, or specifically targeted antimicrobial peptide (STAMP), e.g., the peptide C16G2, is provided, with or without a fluoride. In various embodiments, a dental varnish system that provides release of a fluoride, with or without an antimicrobial peptide or STAMP is provided. In certain embodiments the dental varnish system comprises a first component that is a dry powder, said first component comprising a an antimicrobial peptide, with or without a fluoride, and a bulking agent, and a second component that is a fluid, said second component comprising a varnish solution, where combination of said first component with said second component provides a varnish formulation for application to the surface of a tooth.
Core Innovation
The invention relates to a dental varnish system for the sustained delivery of a specifically targeted antimicrobial peptide (STAMP). The system comprises a first component that is a dry powder comprising a STAMP having the amino acid sequence TFFRLFNRSFTQAL GKGGGKNLRIIRKGIHIIKKY (C16G2, SEQ ID NO:1), and a second component that is a fluid varnish solution comprising an aminomethacrylate polymer and ethanol 200 proof USP.
In the combined formulation, ethanol is a solvent for the dry powder first component. When the resulting fluid varnish formulation is applied to the surface of a tooth, it delivers an effective amount of the STAMP that retains antimicrobial activity on the surface of the tooth for at least 4 hours after application.
The invention also includes a dental varnish comprising the STAMP and a varnish solution comprising an aminomethacrylate polymer and ethanol 200 proof USP. Additional claimed variants specify release of an effective amount of STAMP for specified time periods after application, and/or release of at least 80% of STAMP within specified time windows, while maintaining the varnish solution structure and sustained antimicrobial activity requirement.
Claims Coverage
The independent claims define a two-component dental varnish system and a dental varnish composition. The core inventive features number 4: a specific STAMP identity, a dry powder and fluid varnish system, an aminomethacrylate polymer and ethanol 200 proof USP varnish solution, and sustained antimicrobial activity on a tooth surface for at least 4 hours after application.
Specifically targeted antimicrobial peptide identity
A dental varnish system or varnish comprising a specifically targeted antimicrobial peptide (STAMP) having the amino acid sequence TFFRLFNRSFTQAL GKGGGKNLRIIRKGIHIIKKY (C16G2, SEQ ID NO:1).
Two-component dental varnish system using ethanol as solvent for STAMP powder
A first component that is a dry powder comprising the STAMP, and a second component that is a fluid varnish solution comprising an aminomethacrylate polymer and ethanol 200 proof USP, where ethanol is a solvent for the dry powder first component.
Aminomethacrylate polymer varnish solution in ethanol 200 proof USP
A fluid varnish solution comprising an aminomethacrylate polymer and ethanol 200 proof USP.
Sustained retention of antimicrobial activity on the tooth surface
Application to the surface of a tooth delivers an effective amount of the STAMP that retains antimicrobial activity on the surface of the tooth for at least 4 hours after application, with dependent embodiments specifying longer retention or release thresholds.
The independent claims center on sustained delivery of the specific STAMP (C16G2, SEQ ID NO:1) using an aminomethacrylate/ethanol varnish, with ethanol as the solvent for the STAMP and retention of antimicrobial activity for at least 4 hours after application.
Stated Advantages
Retains antimicrobial activity on the surface of a tooth for at least 4 hours after application.
In certain embodiments, delivers an effective amount that retains antimicrobial activity for at least 6, 8, 12, 24, or 48 hours after application.
In certain embodiments, releases at least 80% of the STAMP within specified time windows after application.
Documented Applications
Caries prevention, inhibiting S. mutans, improving hardness, and tooth desensitization.
Applied to the surface of a tooth to deliver an effective amount of STAMP with antimicrobial activity retained for at least 4 hours after application.
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