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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 is directed to treating melasma or reducing a sign or a symptom of melasma by topically administering to a subject in need thereof a transdermal formulation. The transdermal formulation includes two active agents, where the two active agents consist of a buffering agent and tranexamic acid. The buffering agent is selected from sodium carbonate, sodium bicarbonate, and triethanolamine.
The disclosure also describes buffering agents in topical and transdermal compositions and relates pH buffering behavior to pH modulation. It further presents tranexamic acid in alkaline systems, including tranexamic acid alone and combinations of tranexamic acid with glycolic acid and with retinoic acid.
Overall, the core concept integrates tranexamic acid with a buffering agent in a transdermal formulation for melasma treatment, including melasma caused by or exacerbated by birth control pills, pregnancy, hormone therapy, stress, thyroid disease, and sun exposure. The document also describes formulations as cream, lotion, and ointment, and includes example studies and assessments of outcomes and tolerance, including skin irritation and formulation effectiveness.
Claims Coverage
The independent claim coverage is directed to topical transdermal melasma treatment using a two-active-agent formulation consisting of a buffering agent and tranexamic acid. The main inventive features are the two-agent composition, the specific buffering agent selection, and use for melasma associated with enumerated causes or exacerbating factors.
Two-active-agent transdermal melasma formulation (buffering agent plus tranexamic acid)
A method for treating melasma or reducing a sign or a symptom of melasma by topically administering to a subject in need thereof a transdermal formulation having two active agents, wherein the two active agents consist of a buffering agent and tranexamic acid.
Buffering agent selection for the transdermal formulation
The buffering agent is selected from sodium carbonate, sodium bicarbonate, and triethanolamine.
Melasma associated with enumerated causes or exacerbating factors
The melasma is caused by or exacerbated by one or more of birth control pills, pregnancy, hormone therapy, stress, thyroid disease, and sun exposure.
Cream, lotion, or ointment transdermal melasma formulation
A method for treating melasma or reducing a sign or a symptom of melasma by topically administering to a subject in need thereof a transdermal formulation formulated as a cream, lotion, or ointment and having two active agents, wherein the two active agents consist of a buffering agent and tranexamic acid.
Specified sodium carbonate, sodium bicarbonate, and tranexamic acid levels
The transdermal formulation comprises about 1% w/w sodium carbonate and/or about 1% w/w sodium bicarbonate and comprises about 6% tranexamic acid.
The claim coverage centers on topically administering a transdermal formulation containing exactly two active agents consisting of a buffering agent and tranexamic acid, with the buffering agent limited to sodium carbonate, sodium bicarbonate, or triethanolamine, for melasma linked to the enumerated causes or exacerbating factors. One independent claim additionally requires a cream, lotion, or ointment form and specified levels for sodium carbonate or sodium bicarbonate and tranexamic acid.
Stated Advantages
Reduces a sign or a symptom of melasma.
Treats melasma.
Reduces abnormal skin pigmentation in melasma.
Includes skin irritation tolerance and formulation effectiveness assessments.
Documented Applications
Treating melasma or reducing a sign or a symptom of melasma in a subject.
Melasma treatment using transdermal formulations with tranexamic acid and buffering agents.
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