Light activated gasotransmitter generating compositions
Inventors
Assignees
Publication Number
US-11369682-B2
Publication Date
2022-06-28
Expiration Date
2039-04-24
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Abstract
A composition comprising an organic photoactivator, a gasotransmitter salt which converts into a gasotransmitter via electron transfer, and an electron donor which donates an electron to the photoactivator when the photoactivator is in a photo-excited state.
Core Innovation
The invention disclosed provides compositions comprising an organic photoactivator, a gasotransmitter salt which converts into a gasotransmitter via electron transfer, and an electron donor which donates an electron to the photoactivator when in a photo-excited state. These compositions enable the generation of gasotransmitters such as nitric oxide and hydrogen sulfide through light activation. The photoactivator includes structures like benzophenone, anthraquinone, and thioxanthone, with derivatives potentially water soluble. Electron donors may be selected from groups like alcohols, amines, and thiols, including specific examples such as isopropyl alcohol and triethylamine. Gasotransmitter salts include nitrite, nitrate, sulfate, sulfite, or thiosulfate salts with various cations.
The problem addressed relates to the challenges in delivering gasotransmitters, especially nitric oxide, in a controlled and targeted manner. Nitric oxide, while important in physiological regulation and antimicrobial activity, is a gas at ambient conditions with a short half-life, limiting its practical therapeutic application. Existing methods lack controlled delivery, thus restricting nitric oxide's use in treatments such as bacterial infections and wound healing.
The invention solves this by providing a system where the photoactivator, upon excitation by light in specific wavelengths (typically between about 300 nm and 750 nm), receives an electron from an electron donor. The reduced photoactivator then initiates the conversion of the gasotransmitter salt to the active gasotransmitter at the targeted site. This approach allows controlled, localized generation of the gasotransmitter upon light exposure, facilitating therapeutic and disinfecting applications with improved delivery and modulation of gas release.
Claims Coverage
The patent includes several independent claims covering compositions and methods related to light-activated gasotransmitter generation. The main inventive features center on composition components and their functional interactions, activation wavelengths, and applications.
Composition comprising an organic photoactivator, electron donor, and gasotransmitter salt
The composition includes an organic photoactivator that receives an electron in a photo-excited state, an electron donor from specified chemical groups (alcohols, amines, thiols, sugars, boranes) that donates the electron to the photoactivator to reduce it, initiating conversion of a gasotransmitter salt into a gasotransmitter, specifically nitrite or nitrate salts with defined cations, formulated as ointments, salves, or creams.
Electron donor specificity
The electron donor is selected from secondary alcohols, tertiary amines, and heteroaromatic thiols, including examples like isopropyl alcohol, 2-hexanol, cyclohexanol, triethylamine, and related polycarboxylic acids.
Photoactivation and excitation parameters
The photoactivator is activated to the photo-excited state by incident radiation in the 300 nm to 750 nm range, preferably 320 nm to 420 nm, with a photo-excited state lifetime greater than about 50 nanoseconds and an excited state energy greater than about 100 kJ/mol above the ground state.
Photoactive moiety and hydrophilic character
The photoactivator includes a photoactive moiety selected from benzophenone and thioxanthone derivatives and comprises hydrophilic moieties such as alcohol, amine, amide, carboxylic acid, sulfonic acid, phosphate alkylene oxide oligomers, alkylene oxide polymers, and other specified polymers.
Specific gasotransmitter salts
The gasotransmitter salt is specifically sodium nitrite or sodium sulfite in preferred embodiments.
Methods of use involving light exposure
Methods include making a benefit active by exposing the composition to light; treating acne vulgaris, wounds, or skin; disinfecting surfaces; and removing biofilm by contacting the target and exposing to light.
Compositions with hydrophobic base and amphiphilic compounds
Compositions may further comprise a hydrophobic base consisting of natural or synthetic fats, waxes, and oils, and an amphiphilic compound aiding formulation properties.
Compositions including moisture activated pharmaceutical ingredients
The composition may include moisture activated active pharmaceutical ingredients integrated with the photoactivator, electron donor, and gasotransmitter salt system.
The claims cover compositions comprising specific combinations of a photoactivator, electron donor, and gasotransmitter salt with defined chemical and physical characteristics, activated by light in specific wavelength ranges to produce gasotransmitters. They also encompass methods of using these compositions for therapeutic and disinfecting purposes, and formulations incorporating hydrophobic, amphiphilic, and moisture-activated ingredients to optimize application.
Stated Advantages
The compositions enable controlled and targeted delivery of gasotransmitters such as nitric oxide and hydrogen sulfide, overcoming challenges of their gaseous nature and short half-life in physiological conditions.
Light activation allows spatial and temporal control over gasotransmitter generation, providing on-demand release at target sites.
The approach expands therapeutic applications including antimicrobial activity, wound healing, inflammation alleviation, and biofilm removal.
The compositions can be formulated in various forms such as ointments, salves, creams, and hydrogels enhancing applicability for topical and surface treatments.
Documented Applications
Treatment of wounds by contacting wounded tissue with the composition followed by light exposure.
Treatment of skin conditions including acne vulgaris by topical application and light activation.
Disinfection of surfaces by applying the composition and exposing to light.
Removal of biofilm from surfaces by contacting with the composition and light exposure.
Cleaning and treating oral cavity surfaces, including teeth and dentures, to address issues such as stain bleaching, plaque removal, cavity prevention, and gum inflammation.
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