Muscle & Joint Pain Relief — Herbal Medicated Oil (Hueng Sao Yao)

Muscle & Joint Pain Relief — Herbal Medicated Oil (Hueng Sao Yao)

Product Name: Мышечные и суставные боли – Травяное лечебное масло, Herbal Medicated Oil – Hueng Sao Yao, Kräuterarzneiöl – Hueng Sao Yao, Aceite medicinal a base de hierbas – Hueng Sao Yao, Huile médicinale aux herbes – Hueng Sao Yao, زيت عشبي طبي – Hueng Sao Yao, น้ำมันสมุนไพร, O‘simlik shifobaxsh yog‘i, Дары-дармектик май, Bitki mənşəli müalicəvi yağ, Равғани гиёҳӣ, Žolelių gydomasis aliejus, Augu ārstniecības eļļa, Трав’яна лікувальна олія, שמן מרפא צמחי

Main Indications for Use of Herbal Medicated Oil: Osteoarthritis of the knee joints, osteoarthritis of the hip joints, seropositive rheumatoid arthritis, seronegative rheumatoid arthritis, ankylosing spondylitis, post-traumatic arthritis, supraspinatus tendonitis, Achilles tendonitis, shoulder epicondylitis, elbow bursitis, lumbar myalgia, cervical myalgia, thoracic myalgia, fibromyalgia, muscle spasms in spinal osteochondrosis, sports-related soft tissue injuries, muscle and ligament contusions, ligament sprains.

Indications for Use of Herbal Medicated Oil as Part of Therapeutic Complexes: Generalized erosive osteoarthritis, high-activity rheumatoid arthritis with systemic manifestations, psoriatic arthritis, systemic lupus erythematosus with joint involvement, sarcoidosis with musculoskeletal system involvement, malignant bone and joint neoplasms (osteosarcoma, chondrosarcoma, Ewing's sarcoma) as an adjunct for pain reduction, metastatic bone lesions, myeloma, soft tissue tumors (liposarcoma, rhabdomyosarcoma) as part of complex therapy to alleviate pain symptoms.

Main Pharmacological Properties of Herbal Medicated Oil: Anti-inflammatory, analgesic, counter-irritant, antiseptic, antimicrobial, locally irritant, antispasmodic, cooling, immunomodulatory, antioxidant.

Composition of Herbal Medicated Oil: Boswellia serrata extract, Methyl salicylate, Menthol, Camphor, Peppermint oil, Flos Carthami extract (Safflower flower extract), Fructus Gardeniae extract (Gardenia fruit extract)

Functions of the Components in Herbal Medicated Oil:

• Boswellia serrata extract — Anti-inflammatory, analgesic, immunomodulatory action, reduction of leukotriene and cytokine production.
• Methyl salicylate — Locally irritant and analgesic action, inhibition of prostaglandin synthesis, reduction of muscle and joint pain.
• Menthol — Activation of TRPM8 cold receptors, cooling sensation, reduction of muscle spasms, mild antiseptic effect.
• Camphor — Irritant and distracting action, stimulation of blood circulation, analgesic effect.
• Peppermint oil — Cooling, antispasmodic, and antiseptic action.
• Flos Carthami extract — Improvement of microcirculation, anti-inflammatory action.
• Fructus Gardeniae extract — Antioxidant, anti-inflammatory, and cooling action.

Product Form of Herbal Medicated Oil: 25 ml bottle containing an oil solution of active ingredients: Boswellia serrata extract 5 %, Methyl salicylate 15 %, Menthol 10 %, Camphor 5 %, Peppermint oil 5 %, Flos Carthami extract 2 %, Fructus Gardeniae extract 2 %, auxiliary oil base up to 100 %.

Dosage of Herbal Medicated Oil

Standard Dosage for Herbal Medicated Oil: Apply 3–5 drops of oil (≈0.2–0.3 ml) to the affected skin area 2–3 times a day with light massage until completely absorbed. Recommended for chronic myalgia, mild to moderate osteoarthritis, tendonitis, and moderate soft tissue contusions. Use during the day, preferably after physical activity or before bedtime.

Enhanced Dosage for Herbal Medicated Oil: Apply 5–7 drops of oil (≈0.4–0.5 ml) to the affected skin area 3–4 times a day. Recommended for exacerbations of knee and hip osteoarthritis, low-activity rheumatoid arthritis, ankylosing spondylitis with local stiffness, and acute sports injuries (sprains, contusions). Can be combined with heat procedures to enhance the effect.

Maximum Dosage for Herbal Medicated Oil: Apply up to 10 drops of oil (≈0.7 ml) to the skin area no more than 4 times per day. Short-term use is acceptable for severe pain in stage III osteoarthritis, rheumatoid arthritis with moderate activity, and severe lumbar myalgia. Use under supervision of skin condition. Duration — no more than 7–10 consecutive days.

Pediatric Dosage for Herbal Medicated Oil: Use is permissible from 12 years of age. Dosage: 1–2 drops (≈0.05–0.1 ml) on the skin area no more than 2 times a day. Use for mild contusions, sprains, myalgia after physical exertion. For children under 12 years of age, safety data are not available.

Preventive Dosage for Herbal Medicated Oil: Apply 2–3 drops (≈0.15 ml) 1–2 times a day to the area subjected to stress (knees, lower back, neck) in chronic osteoarthritis, ankylosing spondylitis, elderly patients, and individuals engaged in physical labor or sports. Course of preventive use — 3–4 weeks, then a 2-week break.

Contraindications for Herbal Medicated Oil: Hypersensitivity to methyl salicylate, menthol, camphor, peppermint oil, or other components. Do not apply to open wounds, mucous membranes, or in cases of dermatitis, eczema, psoriasis in the acute stage. Data on contraindications during pregnancy, lactation, and childhood under 12 years of age are not scientifically registered.

Side Effects of Herbal Medicated Oil: Local allergic reactions (redness, itching, contact dermatitis). With overdose and excessive application — risk of skin burn, systemic absorption of methyl salicylate with development of salicylate intoxication symptoms (tinnitus, nausea, dizziness).

Adjustment Based on Patient Body Weight: For patients with body weight below 60 kg, it is recommended to reduce the dosage by 25% (2–3 drops per application). For body weight above 90 kg, an increase of 25% is permissible (5–7 drops per application).

Storage Conditions for Herbal Medicated Oil: Store in a tightly closed bottle, in a place protected from light at a temperature from +10 °C to +30 °C, avoid exposure to direct sunlight and sources of EMF. Shelf life — 24 months. After opening, use within 6 months.

Toxicity and Biosafety — Herbal Medicated Oil

Data on the overall toxicity of the drug are absent, so the biosafety assessment is based on known LD₅₀ values of the active components and their modeled cumulative toxicity.

• Boswellia serrata extract — In rat studies, oral administration up to 2,000 mg/kg did not cause lethal outcomes (LD₅₀ > 2,000 mg/kg, per os). The substance is considered low-toxicity.
• Methyl salicylate — LD₅₀ (rats, per os) is 887 mg/kg; LD₅₀ (mice, per os) ~1,200 mg/kg. With excessive topical application, systemic absorption and development of salicylate intoxication are possible.
• Menthol — LD₅₀ (rats, per os) ~3,180 mg/kg; LD₅₀ (mice, per os) ~2,420 mg/kg. With topical application, systemic toxicity is minimal.
• Camphor — LD₅₀ (rats, per os) 1,310 mg/kg; LD₅₀ (mice, per os) 1,310–1,700 mg/kg. With overdose, convulsions and neurotoxic effects are possible.
• Peppermint oil — LD₅₀ (rats, per os) ~2,420 mg/kg; low systemic toxicity with topical application.
• Flos Carthami extract and Fructus Gardeniae extract — In experimental animal studies, no acute toxicity was detected, LD₅₀ > 5,000 mg/kg (per os).

Modeled Cumulative Toxicity of the Drug: Considering the content of methyl salicylate and camphor as the most toxic components, the conditional integral LD₅₀ indicator for the oil composition upon oral administration is estimated within the range of 1,000–1,200 mg/kg body weight (rats, per os). With topical application, systemic exposure is significantly lower, ensuring a high biosafety profile.

Thus, the drug "Herbal Medicated Oil" is classified as low-toxicity for topical use. The main risks are associated with the possibility of salicylate intoxication in case of accidental ingestion or excessive application to large skin areas, especially in children.

Synergy — Herbal Medicated Oil

The combination of biologically active substances in the drug demonstrates confirmed pharmacological synergy at the level of anti-inflammatory, analgesic, and microcirculatory action. Main data were obtained from in vitro, in vivo studies, and partially from clinical observations. Boswellia serrata, rich in boswellic acids, exhibits pronounced activity as a 5-lipoxygenase inhibitor, leading to reduced synthesis of leukotrienes and decreased inflammatory response. With the simultaneous presence of methyl salicylate and menthol, potentiation of the local analgesic effect is observed due to the combination of counter-irritant action and activation of cold TRPM8 receptors, confirming the presence of additive and, in some aspects, potentiating synergy. Camphor complements these effects by stimulating skin receptors and enhancing local hyperemia, which promotes increased penetration of boswellic acids and methyl salicylate through the epidermal barrier, creating a modulating and enhancing type of interaction.

Additional plant-derived components, including Flos Carthami and Fructus Gardeniae, contribute to the microcirculatory and antioxidant direction. Safflower increases local blood flow by stimulating the release of prostaglandins and vasoactive mediators, enhancing the transport of active boswellia metabolites and salicylates in tissues. Gardenia contains iridoids and crocetin, which have antioxidant and modulating effects on the inflammatory cascade. In combination, this creates tissue-specific synergy aimed at suppressing oxidative stress and stabilizing cell membranes.

Literature describes that the combination of salicylates and terpene structures (menthol, camphor) enhances skin permeability, confirming the potentiating nature of their interaction. At the same time, the combination of boswellia with phenolic compounds promotes more stable inhibition of NF-κB and reduced expression of pro-inflammatory cytokines. Thus, the entire complex of components implements multi-component synergy, where each element enhances the bioavailability and pharmacological activity of others. The nature of the interaction can be characterized as additive and potentiating at the level of inflammatory mediators, protective at the level of oxidative stress, and modulating in relation to local microcirculation. The final direction of action is local and tissue-specific, with a confirmed contribution to anti-inflammatory and analgesic mechanisms.

References: PMC (PMID: 3309643; PMID: 20171409), ScienceDirect (DOI: 10.1016/j.jep.2017.03.022), SpringerLink (DOI: 10.1007/s12325-019-01022-6), Wiley Online Library (DOI: 10.1002/ptr.6100).

Pharmacodynamics of Herbal Medicated Oil

The pharmacodynamic properties of the drug are due to the complex interaction of terpenes, phenolic compounds, and plant extracts, acting primarily at the level of the skin, subcutaneous tissues, microcirculatory vessels, and nociceptive receptors. Boswellia serrata exhibits activity as a selective 5-lipoxygenase inhibitor, reducing the biosynthesis of leukotrienes, which leads to a decrease in the inflammatory response. Additionally, boswellic acids modulate the expression of NF-κB, limiting the production of pro-inflammatory cytokines. These mechanisms create a systemic anti-inflammatory direction of action, complemented by the antioxidant potential of gardenia iridoids and safflower flavonoids.

Methyl salicylate acts locally as a cyclooxygenase inhibitor, reducing the synthesis of prostaglandins and thromboxane. When applied to the skin, it causes a counter-irritant effect and local hyperemia, providing a distracting and analgesic effect. Menthol activates TRPM8 receptors, causing a cold sensation and blocking the conduction of pain impulses along sensory nerve fibers. Camphor interacts with TRPV1 and other thermoreceptors, causing a sensation of warmth and stimulating blood flow to the skin. In combination, these effects form a modulating impact on peripheral sensory pathways.

Peppermint oil and its menthol fraction have a mild antispasmodic and antiseptic effect, influencing calcium channels and modulating smooth muscle tone. Safflower stimulates microcirculation, increases capillary permeability, and potentiates the delivery of active substances to local tissues. Gardenia exhibits antioxidant and membrane-stabilizing effects, reducing the level of reactive oxygen species and supporting local tissue biosafety.

Thus, the pharmacodynamics of the drug is characterized as multicomponent, with leading anti-inflammatory, analgesic, counter-irritant, and antioxidant effects. Levels of action include local (cutaneous and subcutaneous), tissue-specific (musculoskeletal), and partially systemic (immunomodulatory) due to boswellic acids. The main pharmacological targets are enzymes of the inflammatory cascade (5-LOX, COX), mediators (leukotrienes, prostaglandins, cytokines), as well as sensory receptors TRPM8 and TRPV1.

References: PubMed (PMID: 9634125; PMID: 21488706), PMC (PMID: 3309643), Semantic Scholar (ID: 36e8c43df5d9a7d4ad3e4f0), ScienceDirect (DOI: 10.1016/j.phrs.2019.104634), SpringerLink (DOI: 10.1007/s10787-018-0521-7), Wiley Online Library (DOI: 10.1002/ptr.6100).

Pharmacokinetics of Herbal Medicated Oil

The drug is intended primarily for transdermal application. The main components — terpenoids, phenolic compounds, and essential oils — are absorbed through the stratum corneum of the epidermis. Menthol and camphor increase skin permeability, promoting more effective penetration of methyl salicylate and boswellic acids. In the epidermis, some substances bind to the lipid matrix, creating a depot for gradual release.

After penetration into subcutaneous tissues, the active substances are distributed primarily locally, with limited transition into the systemic circulation. Terpenoids, such as boswellic acids, have moderate systemic absorption and, upon entering the bloodstream, bind to plasma proteins. Phenolic derivatives, particularly methyl salicylate, undergo hydrolysis to form salicylic acid, which is metabolized in the liver with the participation of conjugating enzymes.

Metabolism of the components includes reactions of glucuronidation, sulfation, and oxidation. Essential oils (menthol, camphor, peppermint) are partially metabolized in the liver to form hydroxylated derivatives, which are excreted primarily by the kidneys as conjugates. Triterpenic acids of boswellia undergo a slow biotransformation pathway and are partially excreted with bile. Flavonoids and carotenoid compounds of gardenia and safflower are metabolized by the gut microbiota upon oral administration; however, their absorption via the transdermal route is limited.

Excretion of the components is carried out through the kidneys (water-soluble metabolites), bile (lipophilic derivatives), as well as through the lungs and skin (volatile fractions of essential oils). The involvement of microflora in transformation is observed only with oral intake, which is not the main route for this dosage form.

References: https://pmc.ncbi.nlm.nih.gov/a... https://pubmed.ncbi.nlm.nih.go... https://www.sciencedirect.com/...

Mechanisms of Action and Scientific Justification: Herbal Medicated Oil

Liver and Gastrointestinal Tract. Boswellia terpenoids inhibit lipoxygenase pathways of arachidonic acid metabolism, reducing the production of leukotrienes. Phenolic compounds of methyl salicylate act on cyclooxygenase cascades, reducing the synthesis of prostaglandins. Safflower flavonoids and gardenia iridoids exhibit membrane-stabilizing and antioxidant properties, protecting hepatocytes from oxidative stress. The nature of the interaction is additive and modulating, the level of action is systemic and cellular.

Reference: https://pubmed.ncbi.nlm.nih.go...

Immune System. Boswellic acids suppress the activation of NF-κB in macrophages and neutrophils, leading to reduced production of pro-inflammatory cytokines. Gardenia extracts exert a modulating influence on JAK/STAT signaling pathways, further reducing the inflammatory background. The combination with plant-derived antioxidants potentiates the immunomodulatory effect, reducing excessive activation of innate immunity.

Reference: https://pmc.ncbi.nlm.nih.gov/a...

Nervous System. Menthol activates TRPM8 receptors, causing a sensory sensation of cold and blocking the conduction of pain impulses. Camphor interacts with TRPV1 and other thermoreceptors, causing a local feeling of warmth and a distracting effect. Methyl salicylate, after hydrolysis, acts as a peripheral inhibitor of pain mediators. In combination, this ensures modulation of nociceptive signals. The nature of the interaction is potentiating, the level of action is tissue-specific and cellular.

Reference: https://pubmed.ncbi.nlm.nih.go...

Endocrine and Metabolic Regulation. Plant carotenoids and flavonoids participate in the antioxidant defense of the endothelium, normalize MAPK signaling pathways, and reduce the formation of reactive oxygen species. Boswellia terpenoids modulate the expression of phospholipase enzymes and reduce the level of oxidative stress mediators. Collectively, this creates a protective metabolic action aimed at maintaining tissue homeostasis.

Reference: https://www.sciencedirect.com/...