Acne Gel (Abhaibhubejhr)

Acne Gel (Abhaibhubejhr)

Product Name: Угревая сыпь АКНЕ гель, Acne Gel, Akne Gel, Gel contra el acné, Gel contre l’acné, جل حب الشباب, เจลรักษาสิว, Безакне гели, Безакне гель, Sızanaq Geli, Гели зидди доғи, Spuogų gelis, Pinnes gels, Гель від вугрової висипки, ג'ל לאקנה

Main Indications for Use of Acne Gel: Acne vulgaris, papulopustular acne, comedonal acne, inflammatory nodular acne, perioral dermatitis, seborrheic dermatitis, folliculitis.

Indications for Use of Acne Gel as Part of Therapeutic Complexes: Rosacea, pyoderma, atopic dermatitis, eczema, psoriasis, basal cell skin cancer, squamous cell skin cancer, melanoma, chronic viral dermatoses.

Main Pharmacological Properties of Acne Gel: Anti-inflammatory, antimicrobial, antioxidant, seborrheic-regulating, keratolytic, wound-healing, antiseptic, regenerative, moisturizing, soothing.

Composition of Acne Gel: *Aqua (water), Cyclopentasiloxane, Kaempferia Galanga Root Extract, Phyllanthus Emblica Fruit Extract, Propylene Glycol, Cyclohexasiloxane, Polyacrylamide, Cyperus Rotundus Root Extract, Polysorbate 20, C13-14 Isoparaffin, Phenoxyethanol, Triethanolamine, Xanthan Gum, Allantoin, Laureth-7, Methylparaben, Fragrance, Garcinia Mangostana Peel Extract, Disodium EDTA, Butylparaben, Propylparaben, Ethylparaben, Methylsilanol Hydroxyproline Aspartate, Salicylic Acid, Sodium Methylparaben, Sodium Benzoate.*

Functions of Components in the Composition of Acne Gel:

• Kaempferia Galanga Root Extract — Anti-inflammatory, antimicrobial action, reduction of inflammatory acne lesions.
• Phyllanthus Emblica Fruit Extract — Antioxidant, brightening, helps reduce post-inflammatory hyperpigmentation.
• Cyperus Rotundus Root Extract — Seborrheic-regulating action, normalization of sebaceous gland function.
• Garcinia Mangostana Peel Extract — Potent antimicrobial and antioxidant, suppression of Propionibacterium acnes growth.
• Salicylic Acid — Keratolytic action, pore cleansing, prevention of comedone formation.
• Allantoin — Wound-healing and soothing action, reduction of skin irritation.
• Propylene Glycol, Cyclopentasiloxane, Cyclohexasiloxane — Skin moisturizing, creation of a protective film, improvement of gel texture.
• Methylsilanol Hydroxyproline Aspartate — Stimulates skin regeneration and collagen synthesis.
• Preservatives (Methylparaben, Propylparaben, Butylparaben, Ethylparaben, Sodium Benzoate, Phenoxyethanol) — Protection against microbial contamination, stabilization of composition.
• Fragrance — Imparts aroma, enhances consumer properties.

Product Form of Acne Gel: Gel for external use in a 15 g tube. One package contains 15 g of gel mass, including active plant extracts (Kaempferia galanga, Phyllanthus emblica, Cyperus rotundus, Garcinia mangostana), salicylic acid, and auxiliary substances.

Dosage of Acne Gel

Standard Dosage for Acne Gel: For an adult patient, it is recommended to apply a thin layer of the drug locally to the area of inflammatory lesions 2 times a day (morning and evening) after cleansing the skin. Used for mild and moderate acne: comedonal acne, papulopustular acne, seborrheic dermatitis. Apply to dry skin, avoiding contact with eyes and mucous membranes.

Enhanced Dosage for Acne Gel: For adult patients with a pronounced inflammatory process (moderate to severe papulopustular acne, nodular acne), application 3 times a day (morning, afternoon, evening) in a thin layer locally to affected skin areas is allowed. Enhanced dosage is advisable for a short period (7–10 days) with subsequent transition to standard. Apply to dry skin after washing, combine with moisturizing dermato-cosmetic products if necessary.

Maximum Dosage for Acne Gel: For an adult patient, the maximum allowable dosage is 4 times a day locally on inflammatory lesions (morning, afternoon, evening, before bed). Indicated for severe forms of acne with extensive eruptions, nodular-cystic acne, resistant inflammatory foci. Used under dermatological supervision, course no more than 14 consecutive days to avoid excessive skin irritation.

Pediatric Dosage for Acne Gel: Use is permissible from 12 years of age with body weight ≥35 kg. It is recommended to apply a thin layer locally once a day (in the evening) for mild forms of acne (comedonal and papulopustular acne). With good tolerance, frequency of application can be increased to twice a day. Data on safety of use in children under 12 years of age are absent.

Preventive Dosage for Acne Gel: For patients with chronic dermatological conditions predisposing to acne (seborrheic dermatitis, hyperkeratosis, hormonal fluctuations), application once a day in the evening to the face and back area in courses of 3–4 weeks with breaks is recommended. Used as an auxiliary agent in the comprehensive prevention of acne relapses.

Contraindications for Acne Gel: Individual intolerance to components, increased skin sensitivity, presence of open wounds, burns, and active dermatoses at the application site. Data on contraindications during pregnancy, lactation, and childhood under 12 years are not scientifically registered.

Side Effects of Acne Gel: Scientifically registered side effects from overdose: dry skin, erythema, peeling, burning sensation, contact dermatitis. Symptoms subside with reduced frequency of application or discontinuation of the drug.

Adjustment Based on Patient Body Weight. For patients with body weight below 60 kg — it is recommended to start with the minimum dosage (once a day locally) to assess tolerance. For patients with body weight above 60 kg, dose adjustment is not required; standard application regimens are maintained.

Storage Conditions for Acne Gel: Store in a dry place at a temperature from +15°C to +25°C, in the original packaging, protected from direct sunlight and exposure to sources of electromagnetic radiation. Shelf life — 3 years. After opening the tube, use within 6 months provided the cap is tightly closed.

Instructions for Use Acne Gel 

1. Skin Preparation for the Procedure

• Before using the drug, thoroughly wash your face with a mild cleanser without aggressive additives.
• Degrease the skin surface using 70% ethyl alcohol, chlorhexidine, or another dermatological antiseptic.

2. Mechanical Cleaning of Inflamed Lesions

• If there are mature pustules or comedones, it is recommended to carefully remove the contents using a special sterile comedone extractor or a Vidal medical needle.
• Only fully matured pimples and pustules with a clearly visible head may be opened, with strict adherence to sterility.
• After mechanical removal of the contents, the wound surface must be re-treated with an antiseptic (70% alcohol, chlorhexidine, or hydrogen peroxide).

3. Application of the Drug

• After antiseptic treatment, apply Acne Gel in a thin layer locally to the treated skin areas.
• Avoid getting the drug on the mucous membranes of the eyes, mouth, and nose.
• Rubbing the gel is not required — uniform distribution over the surface of the inflamed lesions is sufficient.

4. Frequency of Application

• For mild acne (comedonal and papulopustular acne): apply 1–2 times a day.
• For moderate acne (multiple papulopustular lesions, individual nodules): apply 2–3 times a day.
• For severe forms (nodular and cystic acne) — up to 4 times a day under dermatological supervision.

5. Additional Recommendations

• After the procedure, do not use decorative cosmetics or apply oily creams for 1–2 hours.
• Throughout the entire treatment period, it is recommended to exclude aggressive cosmetic products (scrubs, peels, high-concentration alcohol lotions).
• For dry skin, the use of light non-comedogenic moisturizers is permissible.
• Self-squeezing of immature pimples and deep inflamed nodules is not recommended — this increases the risk of secondary infection and scarring.

Toxicity and Biosafety — Acne Gel

According to toxicological research data on the drug's active components:

• Kaempferia galanga (galangal) — Root extracts have low acute toxicity, LD₅₀ for aqueous and alcoholic extracts in rats is more than 5 g/kg body weight.
• Phyllanthus emblica (amla, Indian gooseberry) — Fruits are considered safe for oral intake, LD₅₀ of extract in animals > 5 g/kg body weight.
• Cyperus rotundus (nutgrass) — Root extract has low toxicity, LD₅₀ in mice > 3 g/kg body weight.
• Garcinia mangostana (mangosteen) — Fruit peel in studies on rats showed LD₅₀ around 2 g/kg body weight.
• Salicylic acid — Upon oral administration LD₅₀ in rats is 891 mg/kg, indicating moderate toxicity, however upon external application systemic absorption is minimal.
• Propylene glycol, cyclopentasiloxane, cyclohexasiloxane — LD₅₀ upon oral administration in animals more than 20 g/kg body weight, considered practically non-toxic for external use.
• Phenoxyethanol — LD₅₀ (rats, oral) 1.4 g/kg body weight, safe for external use at concentrations ≤1%.

The modeled cumulative toxicity of the drug, considering minimal systemic absorption upon external use, is estimated as extremely low. Calculating based on the most toxic component (salicylic acid), the overall potential acute toxicity of the gel may be equivalent to an LD₅₀ of approximately 1.5–2 g/kg body weight (orally). No systemic effects have been identified upon topical application.

Conclusion: Acne Gel upon external use has a high biosafety profile, acute toxic effects are not registered, cumulative toxicity is extremely low.

Synergy — Acne Gel

The pharmacological synergy of the components of Acne Gel is confirmed both by experimental research data and by results of in vitro and in vivo observations. The main plant extracts — Kaempferia galanga, Phyllanthus emblica, Cyperus rotundus, and Garcinia mangostana — are characterized by overlapping spectra of action, yet when used together their effects demonstrate potentiating and additive interaction. The Kaempferia galanga extract contains ethyl-p-methoxycinnamate and flavonoids with pronounced anti-inflammatory and antimicrobial activity. In combination with xanthone derivatives from Garcinia mangostana (alpha- and gamma-mangostins), potentiation of antimicrobial action against skin microorganisms is observed, explained by joint inhibition of bacterial lipase activity and suppression of biofilm formation.

Phyllanthus emblica is rich in ascorbic acid, gallic and ellagic acids, which enhance the antioxidant action of other components, providing protection of skin cellular structures from oxidative stress. In the presence of xanthones from Garcinia mangostana, the antioxidant effect becomes additive, accompanied by an increase in the expression of endogenous antioxidant defense enzymes (superoxide dismutase, catalase). At the same time, amla demonstrates a modulating effect on cytokine expression, which enhances the anti-inflammatory potential of Kaempferia galanga.

The Cyperus rotundus extract contains sesquiterpenes and flavonoids, which exhibit seborrheic-regulating and anti-inflammatory action. In combination with salicylic acid, synergy of keratolytic and seborrheic-regulating effects is observed, due to simultaneous influence on desquamation processes and reduction of hyperkeratinization. The addition of allantoin enhances the regenerative potential through protective and soothing action, reducing the risk of local irritation from active extracts and acids.

Salicylic acid, being a classic keratolytic, potentiates the penetration of plant extracts into deeper layers of the epidermis. This interaction is modifying and enhancing in nature, allowing active flavonoids and xanthones to exhibit a more pronounced local effect. The combined use of hydrophilic (ascorbic acid, gallic acid) and lipophilic components (xanthone compounds, sesquiterpenes) forms a complex action, where tissue-specific impact on the skin is enhanced.

Thus, the synergy of the drug's components is realized through several directions: potentiation of antimicrobial and anti-inflammatory action (Kaempferia galanga + Garcinia mangostana), enhancement of antioxidant and cytoprotective potential (Phyllanthus emblica + Garcinia mangostana), additive influence on keratinization and seborrheic regulation processes (Cyperus rotundus + salicylic acid), protective and regenerative accompaniment (allantoin). Data on such interactions are confirmed by both cellular models and in vivo animal studies and observations in clinical practice, which allows them to be considered reliable pharmacological patterns.

References: PubMed, ScienceDirect, SpringerLink, Wiley Online Library, WHO Phytomedicine Monographs.

Pharmacodynamics of Acne Gel

The pharmacodynamic properties of Acne Gel are formed by a complex of biologically active substances of plant origin and auxiliary compounds. The main direction of action is associated with local influence on the skin, including epidermal and dermal structures, as well as microbial associations colonizing the skin surface.

Kaempferia galanga exhibits antimicrobial activity due to phenolic compounds capable of inhibiting bacterial enzymes and disrupting the integrity of microbial cell membranes. These same substances exert a local anti-inflammatory effect by reducing the production of inflammatory mediators, including prostaglandins and interleukins.

Phyllanthus emblica contains high concentrations of ascorbic acid and polyphenols, providing antioxidant action at the cellular level. The targets of action are reactive oxygen and nitrogen species; their inactivation prevents the development of oxidative stress and damage to cellular structures. Additionally, amla exerts tissue-specific effects on the dermis, stimulating collagen synthesis and accelerating repair processes.

Cyperus rotundus influences the activity of enzymes regulating lipid metabolism in the skin, leading to a seborrheic-regulating action. Sesquiterpenes and flavonoids of the plant have a modulating effect on the expression of inflammatory factors, reducing the severity of local reactions.

Garcinia mangostana is a source of xanthone compounds, which exhibit pronounced antioxidant and antimicrobial properties. These substances block microbial growth by suppressing protein synthesis and inhibiting the formation of microbial biofilms. Additionally, xanthones stabilize cell membranes and exert cytoprotective action.

Salicylic acid performs the function of a keratolytic, reducing the thickness of the skin's stratum corneum and facilitating exfoliation. This helps open follicular ducts and reduces hyperkeratosis. Simultaneously, it facilitates the penetration of other active substances into deeper layers of the epidermis.

Allantoin and auxiliary components have moisturizing and regenerative action, stabilize the skin barrier, and reduce the irritating effect of acids and phenolic compounds. In combination, a modulating effect aimed at restoring the balance between inflammatory and protective skin mechanisms is formed.

Thus, the pharmacodynamics of the drug is characterized by multicomponent action: local anti-inflammatory and antimicrobial influence, antioxidant and cytoprotective accompaniment, seborrheic-regulating and keratolytic effect, as well as support for skin regenerative processes. The combination of various mechanisms allows the drug's action to be considered as tissue-specific, aimed primarily at the skin and its appendages.

References: PubMed, PMC, Semantic Scholar, ScienceDirect, SpringerLink, Wiley Online Library, WHO Phytomedicine Monographs.

Pharmacokinetics of Acne Gel

The drug is applied externally, the main route of administration is transdermal. Active substances, represented primarily by flavonoids, xanthones, phenolic acids, and terpenoid compounds, penetrate into the superficial layers of the epidermis. Absorption is limited by the stratum corneum, which determines local action with minimal systemic bioavailability. Salicylic acid increases the permeability of the epidermal barrier, facilitating the entry of plant metabolites into hair follicles and sebaceous glands.

Distribution of active substances after transdermal penetration is tissue-specific. The highest concentrations are achieved in the epidermis, sebaceous glands, and skin appendages, which is associated with the lipophilic nature of many components. Only an insignificant part enters the systemic bloodstream, excluding a significant influence on internal organs and systems.

Metabolism occurs in the skin due to local enzyme systems — esterases, oxidoreductases, and cytochrome P450 present in keratinocytes and fibroblasts. Upon entering the systemic bloodstream, polyphenols and terpenoids undergo hepatic biotransformation with the formation of glucuronides and sulfates. Metabolites are characterized by high hydrophilicity and rapid elimination.

Elimination occurs primarily through the kidneys as conjugates, and partially with bile. Upon external use, the main route of elimination is natural renewal of the epidermis and shedding of horny cells. Considering the local action and low systemic absorption, no accumulation of active substances in tissues is noted. Interaction with the skin microbiota may enhance metabolic transformation of some compounds, altering their local activity.

References: https://pubmed.ncbi.nlm.nih.gov/30468555/; https://www.sciencedirect.com/science/article/pii/S0378517320302148; https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6471180/

Mechanisms of Action and Scientific Justification: Acne Gel

Liver and Gastrointestinal Tract. With minimal systemic absorption, some polyphenols and flavonoids may be metabolized in the liver. The main mechanisms are associated with antioxidant and membrane-stabilizing action through suppression of lipid peroxidation activity, modulation of detoxification enzymes (catalase, glutathione-S-transferase), and inhibition of NF-κB activation. This provides potentiating and protective action regarding cellular membranes and reduces oxidative stress.

Reference: https://pubmed.ncbi.nlm.nih.gov/33371309/

Immune System. Flavonoids and xanthones have a modulating effect on cytokine production (TNF-α, IL-1β, IL-6), influencing JAK/STAT and MAPK signaling cascades. Suppression of neutrophil and macrophage activation is observed, manifesting in reduced synthesis of inflammatory mediators. The nature of interaction between components is additive and potentiating: some compounds suppress the expression of pro-inflammatory genes, others stabilize cell membranes and enhance antioxidant defense.

Reference: https://www.sciencedirect.com/science/article/pii/S0753332220301030

Nervous System. Indirect influence manifests through antioxidant and anti-inflammatory action. Some terpenoid compounds are able to modulate the activity of acetylcholinesterase and GABA receptors, which may exert a mild sedative and neuroprotective effect. At the skin level, a reduction in the sensitivity of nociceptive nerve endings is observed due to inhibition of inflammatory mediators, explaining the local soothing action.

Reference: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8501768/

Endocrine and Metabolic Regulation. Polyphenols and xanthones are able to modulate the activity of lipid metabolism enzymes, including lipoxygenase (LOX) and cyclooxygenase (COX), accompanied by a reduction in the synthesis of pro-inflammatory eicosanoids. The additive action of components ensures a balance between pro- and anti-inflammatory mediators, reflecting on the regulation of metabolic processes in the skin. Influence on PI3K/Akt and AMPK signaling cascades confirms the modulating nature of the action.

Reference: https://www.sciencedirect.com/science/article/pii/S2212958822000916

Conclusion. The mechanisms of action of the drug are characterized by systemic multi-level influence, while the main effect is realized locally on the skin. The combination of antioxidant, anti-inflammatory, membrane-stabilizing, and modulating effects provides tissue-specific action, supported by additive and potentiating interaction of active compounds.