Bisphosphocin gel formulations and uses thereof
Inventors
Kates, Steven A. • Johnson, Keith Arthur
Assignees
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Publication Number
US-12156883-B2
Publication Date
2024-12-03
Expiration Date
Abstract
Gel formulations having antimicrobial activity are disclosed. Methods of using the gel formulation are further disclosed.
Core Innovation
The disclosure provides low-pH topical gel formulations that include Nu-3 or a pharmaceutically acceptable salt, combined with a fatty alcohol thickening agent and a nonionic polymer emulsifier. The formulation includes defined weight/weight ranges for Nu-3, the fatty alcohol thickening agent, the nonionic polymer emulsifier, and a diluent, and the gel formulation has a pH of about pH 1 to about pH 3.
The formulations use fatty alcohol thickening agents and nonionic polymer emulsifiers to produce a topical gel while maintaining the acidic pH associated with retaining antimicrobial activity. Specific nonionic polymer emulsifiers include polysorbate 20, polysorbate 60, polysorbate 80, ceteareth-12, ceteareth-20, ceteareth-30, ceteth-10, ceteth-20, steareth-10, steareth-20, steareth-40, steareth-100, and combinations thereof.
The diluent can include water, glycerol, mannitol, saline, phosphate buffered saline, or combinations thereof. The patent also describes formulation preparation and evaluation context for Nu-3, including pH, HPLC, and viscosity measurement approaches and gel compounding examples, together with biological evaluation in an in vivo murine dermal infection model.
Claims Coverage
The independent claim covers one acidic gel formulation with Nu-3 or a pharmaceutically acceptable salt thereof, a fatty alcohol thickening agent, a nonionic polymer emulsifier, and a diluent. Four inventive features are defined by component identity or class and concentration ranges, plus the pH condition; dependent claims refine the formulation by specifying acceptable component selections and narrower ranges, and by adding an intended therapeutic use to treat infection in a patient.
Nu-3 gel formulation at acidic pH range
A gel formulation containing from about 1% to about 20% (weight/weight) of a Nu-3, or a pharmaceutically acceptable salt thereof, where the gel formulation has a pH of about pH 1 to about pH 3.
Fatty alcohol thickening agent concentration
The gel formulation includes from about 1% to about 10% (weight/weight) of a fatty alcohol thickening agent.
Nonionic polymer emulsifier concentration
The gel formulation includes from about 0.5% to about 5% (weight/weight) of a nonionic polymer emulsifier.
Diluent content to form a gel
The gel formulation includes from about 65% to about 97.5% (weight/weight) of a diluent.
The core claim coverage is the combination of Nu-3 or a pharmaceutically acceptable salt in an acidic gel with a fatty alcohol thickening agent, a specified range of a nonionic polymer emulsifier, and a diluent making up the remainder of the formulation by weight. Dependent refinements include enumerated diluent options, enumerated nonionic polymer emulsifiers, concentration tightening for specific components, and specifying the formulation for treating an infection in a patient.
Stated Advantages
Produces low-pH topical gel formulations intended to retain antimicrobial activity at acidic pH.
Provides topical adherence and viscosity via the fatty alcohol thickening agent and gel formulation.
Provides pH stability for the formulation at acidic pH.
Provides compatibility versus ionic polymers as described in the disclosure.
Documented Applications
Treating microbial infections in patients using the low-pH topical gel formulation, including biofilm-associated infections.
Treating diabetic foot ulcers.
Treating burn wounds.
Treating complicated venous leg ulcers.
Treating otitis externa.
Treating acne vulgaris.
Treating onychomycosis.
Treating conjunctivitis.
A murine dermal MRSA infection model in SKH1 mice where topical Nu-3 in a pH 1.5 fatty-alcohol gel significantly reduces Staphylococcus aureus CFU versus untreated and vehicle groups.
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