Formulations for Rosacea-Associated Inflammation Reduction
Managing rosacea symptoms requires precise control of multiple inflammatory pathways while maintaining skin barrier function. Clinical studies show that untreated rosacea leads to persistent erythema, with inflammatory mediator levels elevated by 2-5 times normal levels. The challenge is further complicated by the skin's heightened sensitivity, where even established active ingredients like retinoids can trigger adverse reactions in over 40% of patients.
The fundamental challenge lies in delivering therapeutic concentrations of active ingredients while preventing the very inflammation these treatments aim to resolve.
This page brings together solutions from recent research—including stabilized retinoid formulations with ergothioneine, TRPV receptor modulators, kallikrein-5 inhibitors, and targeted anti-inflammatory compounds. These and other approaches focus on creating well-tolerated treatments that effectively manage both the immediate symptoms and underlying causes of rosacea.
1. Composition of Ergothioneine and Retinol with Specified Concentration Range
SHANGHAI JIANLIDA BIOTECHNOLOGY CO LTD, 2023
A composition containing ergothioneine and retinol for improving skin condition while reducing side effects of retinol. Ergothioneine, a natural amino acid with antioxidant and anti-aging properties, is added to retinol skincare products at a concentration of 0.01-20%. Ergothioneine improves retinol's stability, reduces its degradation, and mitigates retinol's toxicity, irritation, and inflammation. It also enhances retinol's cell proliferation and migration effects.
2. Composition with Acetylhydroxyproline, Blue Copper Peptide, Centella Asiatica, Allantoin, and Dipotassium Glycyrrhizinate for Sensitive Skin
GUANGZHOU YOUBEI BIOLOGICAL TECH CO LTD, 2023
Soothing and repairing composition for sensitive skin that reduces irritation and discomfort. The composition contains acetylhydroxyproline, blue copper peptide, Centella asiatica, allantoin, dipotassium glycyrrhizinate, and a pH regulator. It aims to alleviate symptoms like redness, itching, dryness, and discomfort when applied to sensitive skin. The composition can be used as a facial mask or skincare product.
3. Cosmetic Composition Containing Methyl Sulfonyl Methane and 4-Alkyl Cyclohexanol Derivatives for TRPV Receptor Modulation
INC BARUNPHARM, 2023
A cosmetic composition for treating inflammatory skin conditions, particularly rosacea, that simultaneously inhibits inflammatory mediator release and activates TRPV receptors. The composition combines methyl sulfonyl methane with 4-alkyl cyclohexanol derivatives, which act as TRPV antagonists. By inhibiting the release of inflammatory mediators and activating TRPV receptors, the composition effectively reduces erythema and discomfort associated with rosacea, particularly in cases where inflammation has progressed.
4. Composition Containing Isochlorogenic Acid with Kallikrein-5 Inhibition Properties
BIOSPECTRUM INC, 2023
Composition for preventing or treating rosacea comprising isochlorogenic acid or a salt thereof as an active ingredient. The composition contains isochlorogenic acid or a salt thereof as an active ingredient, which inhibits the cleavage of cathelicidin into LL-37 through inhibition of the expression and activity of kallikrein-5, a serine protease in the epidermis.
5. Rosacea Repair Composition with Rice, Capers, Hydrolyzed Algae, Centella Asiatica, and Green Tea Polyphenols
SHANGHAI PIBAO BIOTECHNOLOGY DEVELOPMENT CO LTD, 2023
A rosacea repair composition and skin care preparation that combines five scientifically selected active ingredients to prevent and treat rosacea. The composition specifically targets inflammation and neutrophil infiltration, using a synergistic blend of rice, capers, hydrolyzed algae, centella asiatica, and green tea polyphenols. The formulation is optimized through precise proportioning to deliver potent anti-inflammatory and soothing effects, while maintaining product stability. The composition is formulated as a skin care preparation, with a specific formulation ratio of 0.1-5% active ingredient concentration.
6. Retinoid Composition with Teprenone and Phytol for Modulating Inflammatory Pathways
SHENZHEN PURUI HEALTH TECH CO LTD, 2022
Retinoid composition that combines teprenone and phytol to enhance anti-inflammatory effects in skin preparations. The composition specifically targets inflammatory pathways, including reducing IL-16 and TNF-α release, downregulating the P38MAPK and NF-kB signaling pathways, and promoting collagen production. This dual-action approach provides a more comprehensive anti-inflammatory profile compared to traditional retinoids alone.
7. Liniment Composition with Metronidazole, Centella Asiatica Extract, and Dexamethasone Sodium Phosphate
Guangzhou Banyuemei Pharmaceutical Technology Co., Ltd., GUANGZHOU BANYUEMEI PHARMACEUTICAL TECHNOLOGY CO LTD, 2022
A novel external liniment for treating facial acne and rosacea that targets the underlying causes of the condition. The liniment combines a combination of metronidazole, Centella asiatica extract, and dexamethasone sodium phosphate to address the root causes of acne and rosacea. By addressing the bacterial overgrowth, inflammation, and immune system dysregulation, this liniment provides a targeted approach to treating these conditions. The combination of these ingredients has been shown to effectively reduce acne marks and prevent scarring, while also addressing the underlying causes of rosacea.
8. Topical Composition with Olive Oil, Sweet Almond Oil, Helichrysum Oleolite, Vegetable Glycerin, Honey, Garlic Extract, and Beeswax
MOCCI ANTONIO, 2021
Topical composition for treating inflammatory skin disorders like thickening, flaking, redness, and itching. The composition contains olive oil, sweet almond oil, Helichrysum oleolite extract in sweet almond oil, vegetable glycerin, honey, garlic extract, Helichrysum oleolite extract in olive oil, and beeswax. The specific combination of active ingredients, carriers, and excipients promotes penetration through the skin and provides a film-forming, moisturizing, and protective effect to aid repair.
9. Topical Composition Incorporating Modified Polysaccharide Amphiphilic Polymer with Retinoid and Carrier
JOHNSON & JOHNSON CONSUMER INC, JOHNSON & JOHNSON CONSUMER, Johnson & Johnson Consumer Inc., 2021
Topical composition for treating signs of aging, acne, and rosacea that contains a retinoid, a low irritant polymeric cleansing agent (LIPCA), and a cosmetically acceptable carrier. The LIPCA improves retinoid activity compared to using just the retinoid alone. The LIPCA is a modified polysaccharide with amphiphilic properties derived from a superhydrophilic polysaccharide by post-polymerization modification. The LIPCA enhances retinoid efficacy without increasing irritation levels.
10. Topical Rosacea Treatment with Zinc-Dithiocarbamate Ionophore Complex for Enhanced Skin Penetration
RYTHERA THERAPEUTICS INC, 2021
A topical treatment for rosacea that utilizes a zinc ionophore complexed with a thiocarbamate to enhance penetration through the skin's stratum corneum. The treatment delivers sufficient zinc ion to subcutaneously activate the skin's natural antimicrobial peptides, thereby reducing inflammation and skin thickening in rosacea. The zinc ionophore complex forms a stable zinc-dithiocarbamate complex that can penetrate the skin barrier, while the thiocarbamate enhances its delivery through the stratum corneum. This combination provides a targeted approach to treating rosacea through both zinc ion delivery and antimicrobial activity.
11. Topical Formulations with Controlled Release of Brimonidine Tartrate and Stabilizing Agent
GALDERMA PHARMA SA, 2021
Topical formulations for treating rosacea that deliver a targeted dose of α2 adrenergic receptor agonists to the skin, specifically brimonidine tartrate, through controlled release mechanisms. The formulations combine brimonidine with a stabilizing agent like benzalkonium chloride and a buffer system to maintain therapeutic efficacy while minimizing systemic side effects. The formulations are designed to provide sustained delivery of brimonidine to the skin, with the dosing regimen optimized for both efficacy and patient comfort.
12. Composition of Retinoids and Silybum Marianum Extracts Containing Silymarin and β-Sitosterol
PIERRE FABRE DERMO-COSMETIQUE, 2021
A combination of retinoids and extracts of Silybum marianum (L.) Gaertn. for treating acne, seborrheic dermatitis, rosacea, and seborrheic dermatitis. The combination includes retinoids such as retinaldehyde and extracts of Silybum marianum, particularly its achene, which contains silymarin and β-sitosterol. The combination provides synergistic skin benefits through the synergistic action of retinoids and Silybum marianum.
13. Composition with Dual-Temperature Plant Extract Blend for Rosacea Treatment
YUNNAN BOTANEE BIOTECHNOLOGY GROUP CO LTD, 2020
A composition and preparation for rosacea that utilizes a novel combination of natural plant extracts to provide targeted therapeutic benefits. The composition comprises ceramide, cholesterol, and butylene glycol as high-temperature components, while 4-terpineol, salvia root extract, syringa extract, and purple algae extract serve as low-temperature components. This balanced blend addresses the complex pathophysiology of rosacea through its synergistic effects on skin barrier function, inflammation, and sebum regulation.
14. Oxymetazoline Cream Formulation with Emulsifiers and Emollients
ACLARIS THERAPEUTICS INC, 2019
Cream formulation of oxymetazoline for treating rosacea and telangiectasia. The formulation combines oxymetazoline with a combination of emulsifiers, emollients, and other excipients to create a stable, cosmetically acceptable cream. The formulation provides effective treatment of rosacea erythema and telangiectasias while addressing the underlying inflammatory and vascular components of the condition.
15. Topical Skin Care Composition with Aloe Vera, Coconut Oil, Caprylic/Capric Triglycerides, Salicylic Acid, and Phytosphingosine
OCUSOFT INC, 2019
A topical skin care composition for reducing skin redness and inflammation that addresses the underlying causes of the condition. The composition combines natural ingredients like aloe vera, coconut oil, and caprylic/capric triglycerides with salicylic acid phytosphingosine to create a stable, effective, and non-irritating treatment. The composition is formulated to dry quickly and cleanly without leaving residue, while maintaining its moisturizing properties. It can be used to treat rosacea, allergic reactions, and cosmetic surgery-induced redness, and is suitable for daily use for 60 days or longer.
16. Gel Composition with Sequentially Arranged Erythromycin Alcohol, Ginger Extract, Lactic Acid Bacteria Ferment, Ceramide 3, and Fruit Extracts
GAO YIRU, 2019
Moisturizing and soothing gel composition for sensitive skin that provides rapid anti-inflammatory, soothing, and moisturizing effects to repair damaged skin. The composition contains specific ingredients like Erythromycin alcohol, ginger extract, lactic acid bacteria ferment, ceramide 3, and fruit extracts in a specific order (anti-inflammation, soothing, rebuilding, moisturizing) to sequentially manage sensitive skin.
17. Topical Formulations with Pentadecalactone-Solubilized Proteasome Inhibitors
ARBISER JACK, 2019
Topical formulations of proteasome inhibitors that effectively treat skin disorders associated with proteasome activity, including psoriasis, acne, and eczema, by targeting the proteasome pathway. The formulations contain pentadecalactone or a structurally similar solvent that solubilizes the proteasome inhibitors, enabling their topical application. The solvents are particularly effective at solubilizing the proteasome inhibitors, which are otherwise poorly soluble in conventional topical formulations. The formulations can be used to treat skin disorders that are resistant to conventional treatments, including those associated with inflammation and infections.
18. Composition of Retinoids and NF-kB Inhibitors with Targeted NF-kB Transcription Factor Activity
JOHNSON & JOHNSON CONSUMER COMPANIES INC, 2019
A composition that combines retinoids with NF-kB inhibitors to enhance retinoid efficacy while minimizing irritation. The composition contains a retinoid and an NF-kB inhibitor, with the NF-kB inhibitor specifically targeting NF-kB transcription factor activity. This synergistic combination provides enhanced retinoid activity through CRAPBII gene expression enhancement, while maintaining lower retinoid concentrations compared to traditional retinoid formulations.
19. Skin Composition with Plant Extracts and Moisturizers for Capillary Elasticity and Inflammation Reduction
GUANGZHOU RUIYU CHEMICAL TECHNOLOGY CO LTD, 2019
Skin composition to remove red blood streaks that contains active ingredients like Centella asiatica extract, Glycyrrhiza glabra root extract, Artemisia angustifolia leaf extract, Vaccinium angustifolia fruit extract, Ginkgo biloba extract, and Rosehip oil. The composition also has moisturizing ingredients like oat beta-glucan, ectoine, grape seed oil, brown rice fermentation filtrate, and trehalose. The composition aims to reduce red blood streaks on the skin by improving capillary elasticity, reducing permeability, and soothing inflammation.
20. Topical Formulation of α1-Adrenoceptor Agonists with Penetration-Enhancing Agents for Direct Vascular Smooth Muscle Delivery
ALLERGAN INC, 2018
A novel treatment for rosacea and other conditions characterized by increased erythema (redness) through the use of α1-adrenoceptor agonists. The treatment involves topical administration of α1-adrenoceptor agonists, such as oxymetazoline, in combination with penetration-enhancing agents and vehicles. This formulation enables the delivery of α1-adrenoceptor agonists directly to the vascular smooth muscle in the skin, providing a novel approach for reducing and preventing skin redness and telangiectasias.
21. Topical Combination Therapy with Timolol and Rosacea-Specific Active Compound
ALMIRALL SA, 2018
Combination therapy for rosacea treatment that combines timolol with an active compound specifically approved for rosacea. The combination provides enhanced efficacy compared to using timolol alone, with the active compound addressing specific pathophysiological mechanisms of rosacea. The combination can be administered through topical application, with the active compound being either administered alone or in combination with timolol.
22. Water-Free Oleogel Cosmetic Composition with Soybean-Derived Phospholipid, Medium Chain Triglycerides, Jojoba Ester, and Antioxidant Blend
KOKO KOSMETIKVERTRIEB GMBH & CO KG, 2018
A cosmetic composition for topical use in rosacea and systemic treatment that combines a phospholipid, medium chain triglycerides, jojoba ester, and natural antioxidants to provide sustained therapeutic benefits. The composition contains a native soybean-derived phospholipid, medium chain triglycerides, jojoba ester, and a blend of natural and synthetic antioxidants, including azelaic acid, betulinic acid, and palmitic acid ethanolamide, in a water-free oleogel formulation.
23. Cosmetic Composition with Pongamia Oil and 4-t-butylcyclohexanol for Vascular and Inflammatory Modulation
FABRE PIERRE DERMO COSMETIQUE, 2018
A cosmetic composition that prevents and treats rosacea through the synergistic action of pongamia oil and 4-t-butylcyclohexanol. The combination targets the underlying vascular mechanisms of rosacea, specifically the abnormal vasodilation and inflammation associated with the condition. Pongamia oil, with its natural anti-inflammatory properties, and 4-t-butylcyclohexanol, as a TRPV1 antagonist, work together to prevent excessive blood vessel dilation and inflammation that characterize rosacea. This combination provides a novel, non-steroidal treatment approach for rosacea that addresses both the vascular and inflammatory components of the condition.
24. Topical Emulsion Formulation Containing Ivermectin with Fatty Body Oily Phase
GALDERMA SA, 2018
Topical ivermectin formulation for treating rosacea, comprising ivermectin in a cream or lotion emulsion. The formulation contains ivermectin in concentrations between 0.1% and 5% by weight, with the emulsion comprising fatty bodies as the oily phase. The formulation is designed for topical application and can be presented in various forms, including ointments, creams, and gels.
25. Composition Containing Niacinamide, Bisabolol, and Panthenol with Capillary Expansion Inhibiting Properties
GUANGZHOU JUJIKE GREEN CHEMISTRY COMMON TECHNOLOGY RESEARCH INSTITUTE CO LTD, 2018
A composition for inhibiting telangiectasia, the enlarged and visible capillaries that cause facial redness and discoloration. The composition contains a combination of ingredients including niacinamide, bisabolol, and panthenol that work together to effectively reduce capillary expansion. This provides a daily skincare product for inhibiting telangiectasia. The composition aims to address the lack of targeted products for inhibiting capillary dilation, which can be caused by factors like wind, UV, hormones, and diseases.
26. Histone Hyperacetylating Agent with Selective Epigenetic Modulation for Skin Disorders
SUNNY PHARMTECH INC, 2018
A histone hyperacetylating agent enables targeted treatment of skin disorders through epigenetic regulation. The agent selectively hyperacetylates histones, leading to increased acetylated histone levels and epigenetic modifications that modulate gene expression and cellular behavior. This therapeutic approach targets specific skin conditions like rosacea, pityriasis rosea, and rhinophyma by modulating histone acetylation patterns, providing a novel mechanism for skin regeneration and disease management.
27. Topical Formulation with Microencapsulated Solid Benzoyl Peroxide for Controlled Release
Sol-Gel Technologies Ltd., 2018
A topical benzoyl peroxide formulation for treating rosacea that provides sustained release and enhanced efficacy. The formulation comprises benzoyl peroxide in solid form, encapsulated in microcapsules, which enables controlled release of the active agent over a prolonged period. The encapsulation process ensures the benzoyl peroxide maintains its therapeutic properties while minimizing systemic side effects. The formulation demonstrates improved treatment outcomes compared to conventional benzoyl peroxide formulations, with significant improvements in rosacea symptom relief and clearance rates.
28. Biocompatible Topical Compositions with Combined Anti-inflammatory, Vascular Repair, Neurogenic, Sebum Suppression, and Exfoliating Agents
ZO SKIN HEALTH INC, 2017
Biocompatible topical compositions and methods for treating rosacea, including administering a novel combination of anti-inflammatory, vascular repair, neurogenic, sebum suppression, and exfoliating agents to treat, prevent, and stabilize rosacea conditions and symptoms. The compositions address the underlying pathophysiology of rosacea through a synergistic combination of anti-inflammatory, vascular repair, and neurogenic agents, while maintaining a fragrance-free, gluten-free, and paraben-free formulation.
29. Pharmaceutical Composition with 7-(1H-imidazol-4-ylmethyl)-5,6,7,8-tetrahydroquinoline and Derivatives
Allergan Inc., ALLERGAN INK, ALLERGAN INC, 2017
Treatment of skin diseases and conditions through the administration of a pharmaceutical composition containing 7- (1H-imidazol-4-ylmethyl) -5,6,7,8-tetrahydroquinoline or its enantiomers, or tautomers, or their salts. The composition is effective for treating rosacea, psoriasis, erythema, acne, atopic dermatitis, telangiectasia, angiectasia, rhinophyma, contact dermatitis, and other skin conditions characterized by inflammation and vascular abnormalities.
30. Topical Composition with Variable Concentration Pyrithione Zinc in Carrier Medium
SUTICH PAUL, 2016
A novel topical treatment for Rosacea and erythema that utilizes pyrithione zinc at varying concentrations to effectively manage symptoms. The composition, comprising 1% pyrithione zinc in a carrier medium like cocoa butter, provides localized anti-inflammatory and anti-redness effects. The treatment can be administered as a single application or in combination with other over-the-counter treatments, offering a more affordable alternative to prescription-grade medications. The zinc concentration can be adjusted based on the severity of symptoms, making it accessible to individuals with mild to moderate Rosacea.
31. Topical Composition with Terpine-4-ol and Matrix for Enhanced Skin Penetration
TISSUE TECH INC, 2016
A novel treatment for rosacea and related skin conditions that combines topical delivery of terpine-4-ol (T4O) with a skin delivery system. The treatment involves applying a T4O solution containing 0.6-20% w/w T4O and a compatible matrix to the affected area, followed by massaging the composition into the skin. The T4O solution can be used as a standalone treatment or in combination with a matrix to enhance penetration. The treatment can be administered daily for five weeks, with the matrix providing a physical barrier for the T4O to penetrate the skin. The combination of T4O delivery and matrix provides a synergistic approach to treating rosacea and related conditions.
32. Encapsulated Diindolylmethane Formulation with Vitamin A Derivatives and Zinc for Enhanced Bioavailability
SKINTECH LIFE SCIENCE LTD, 2016
A novel treatment for rosacea that utilizes diindolylmethane (DIM) as a potent anti-inflammatory agent. The treatment combines DIM with vitamin A derivatives, zinc, and other natural compounds to address the underlying causes of rosacea. The formulation is encapsulated in a light-resistant capsule, with the DIM component exhibiting enhanced bioavailability through specific formulation and delivery strategies. The treatment demonstrates significant efficacy in reducing rosacea symptoms, particularly when combined with vitamin A derivatives, zinc, and other natural compounds.
33. Stabilized Oxymetazoline Cream with Complex Oil Phase for Enhanced Dermal Penetration
ALLERGAN INC, 2015
A stabilized cream formulation of oxymetazoline for treating rosacea that provides sustained therapeutic efficacy and excellent patient tolerability. The formulation combines a complex oil phase with oxymetazoline, a potent alpha-2 adrenergic agonist, to create a stable, cosmetically elegant delivery system. The complex oil phase achieves increased flux and enhanced penetration compared to traditional formulations, while maintaining the drug's efficacy profile. The formulation is specifically designed for once- or twice-daily application to the face, with a 28-day study demonstrating excellent patient compliance and safety profile.
34. Composition of Methylsulfonylmethane and 4-tert-butyl-cyclohexanol for Modulating Inflammatory Pathways
GENERAL TOPICS S.R.L, 2015
Composition for treating rosacea and other inflammatory skin conditions through the modulation of inflammatory pathways. The composition combines methylsulfonylmethane with 4-tert-butyl-cyclohexanol, a compound that specifically antagonizes transient receptor potential channels (TRPCs) involved in inflammatory signaling. The combination effectively suppresses the release of pro-inflammatory cytokines and mediators while simultaneously blocking TRPC channel activation, thereby preventing the sensation of inflammation and discomfort associated with these conditions.
35. Topical Formulation with Cetirizine and Emu Oil for Skin Condition Management
ZEMTSOV ENTERPRISES LLC, 2015
A topical formulation for treating skin conditions like acne, rosacea, and psoriasis that combines a non-sedating antihistamine with emu oil. The formulation combines cetirizine with emu oil to create a synergistic treatment that not only prevents retinoid dermatitis but also provides potent anti-inflammatory and anti-pruritic effects. The combination addresses the unique challenges of skin conditions like atopic dermatitis and psoriasis, where both topical steroids and retinoids can cause adverse reactions.
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