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Publication Number
US-11744853-B2
Publication Date
2023-09-05
Expiration Date
Abstract
Provided herein are formulations for topical and/or transdermal administration, and methods of using these formulations for the treatment of proliferative diseases related to cancer such as cancers and related conditions, and solid tumors. Also provided are formulations for topical and/or transdermal administration, and methods of using these formulations for melasma, gout, skin disorders, and other diseases and disorders described herein as well as methods for modulating the pH (e.g. raising) of a tissue or microenvironment proximal to a tumor, modulating pH, or improving the effectiveness of know chemotherapeutic agents, immunotherapy and the like for the prevention, treatment of cancers and related conditions described herein.
Core Innovation
The invention relates to topical transdermal buffering formulations for treating rheumatoid arthritis or reducing a symptom of rheumatoid arthritis. A method includes identifying a subject having rheumatoid arthritis or having a symptom thereof and topically administering a transdermal formulation that comprises a penetrant or a penetration enhancer and one or more buffering agents effective in treating rheumatoid arthritis or reducing a symptom thereof.
The buffering agents are selected from sodium bicarbonate, sodium carbonate, a carbonate salt, a bicarbonate salt, a phosphate buffer, TRIS, and lysine, and are present in an effective amount from about 10% to about 56% w/w relative to the formulation. The transdermal formulation optionally comprises menthol and can be implemented in dosage forms such as a cream, lotion, or ointment.
The invention further encompasses co-administration of an analgesic, an anti-inflammatory, a corticosteroid, a nonsteroidal anti-inflammatory drug, or a disease modifying anti-rheumatic agent before, contemporaneously with, or after the transdermal buffering-agent formulation. When a disease modifying anti-rheumatic agent is used, the agent is one or more of azathioprine, cyclosporin, gold, hydroxychloroquine, methotrexate, penicallamine, and sulphasalazine.
Claims Coverage
The provided content includes two independent claims. The claims cover topical transdermal treatment of rheumatoid arthritis using a buffering-agent formulation at about 10% to about 56% w/w, with specified buffering agents and a penetrant or penetration enhancer, and one claim further adds optional menthol plus timed co-administration of additional rheumatoid-arthritis therapeutics.
Topical transdermal buffering-agent treatment for rheumatoid arthritis
A method for treating rheumatoid arthritis or reducing a symptom of rheumatoid arthritis by identifying a subject having rheumatoid arthritis or having a symptom thereof and topically administering a transdermal formulation.
Penetrant or penetration enhancer with specified buffering agents
The transdermal formulation comprises a penetrant or a penetration enhancer and an amount of one or more buffering agents effective in treating rheumatoid arthritis or reducing a symptom thereof, wherein the one or more buffering agents are selected from sodium bicarbonate, sodium carbonate, a carbonate salt, a bicarbonate salt, a phosphate buffer, TRIS, and lysine.
Effective buffering-agent concentration range
The amount of the one or more buffering agents effective in treating rheumatoid arthritis or reducing a symptom thereof is from about 10% to about 56% w/w relative to the formulation.
Buffering-agent formulation with optional menthol
A method where the transdermal formulation comprises a buffering agent effective in treating rheumatoid arthritis or reducing a symptom thereof, wherein the buffering agent comprises sodium bicarbonate, sodium carbonate, a second carbonate salt, a second bicarbonate salt, TRIS, and/or lysine, and optionally comprises menthol.
Timed co-administration of additional rheumatoid-arthritis therapeutics including DMAR agents
Administering an analgesic, an anti-inflammatory, a corticosteroid, or a nonsteroidal anti-inflammatory drug, or a disease modifying anti-rheumatic agent before, contemporaneously with, or after administering the transdermal formulation, wherein the disease modifying anti-rheumatic agent, when administered, is one or more of azathioprine, cyclosporin, gold, hydroxychloroquine, methotrexate, penicallamine, and sulphasalazine.
Across the independent claims, the claim coverage centers on topical transdermal treatment of rheumatoid arthritis using a buffering-agent system at an effective amount of about 10% to about 56% w/w and, depending on the claim, specified buffer selections, optional menthol, a penetrant or penetration enhancer, and co-administration of listed rheumatoid-arthritis therapeutics.
Stated Advantages
Faster pain resolution versus placebo in the described acute gout topical sodium bicarbonate transdermal lotion study results.
No treatment-related adverse events were reported in the described acute gout results.
Pigment reduction was observed in melasma subjects receiving alkaline transdermal formulations with tranexamic acid, including combination conditions described as generally improved outcomes.
Urine pH elevation was reported in preclinical urine pH assessments for certain buffering transdermal agents.
Documented Applications
Topical/transdermal buffering formulations for acute gout, including a placebo comparison using sodium bicarbonate transdermal lotion and reported outcomes such as pain NRS, time to 50% pain reduction, range of motion, and satisfaction.
Alkaline transdermal formulations for melasma, including tranexamic acid with comparative conditions involving additional agents and reported pigment reduction outcomes.
Preclinical assessment of buffering transdermal agents, including urine pH elevation and differences in skin irritation for tested buffering compositions and selected penetration enhancers.
Oncology/immunotherapy example sections were briefly outlined as using topical sodium bicarbonate to modulate tumor microenvironment acidity and improve therapeutic outcomes, including reference to immunotherapy and B16 melanoma.
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