Topical polyherbal oleogel composition for the relief of joint pain and muscular / neuropathic pain

Abstract

Topical polyherbal oleogel composition, comprising, in weight percent of the finished product: (i) Boswellia serrata CO2 select extract 1.0–5.0%; (ii) Curcuma longa phytosome 0.5–2.5% with curcuminoids complexed to phospholipids together with turmerone-rich turmeric essential oil 0.2–0.8%; (iii) Zingiber officinale CO2 select extract 0.5–2.5%; (iv) Hypericum perforatum macerate oil 3.0–10.0%; (v) Capsaicinoids in an equivalent amount of 0.01–0.05%, obtained from Capsicum oleoresin, and Mentha piperita oil 0.3–1.0% together with Rosmarinus officinalis oil 0.2–0.6%; (vi) a carrier phase of sesame oil and medium-chain triglycerides in a ratio of 2:1 to 1:1, and castor oil 8–12% and squalane 1.0–3.0%; (vii) a structuring phase of sunflower lecithin 0.8–2.0% and beeswax 3.0–6.0%, providing a lamellar, shear-thinning oleogel; and (viii) mixed tocopherols 0.1–0.3% and a rosemary diterpene antioxidant extract 0.05–0.2%;wherein the composition is anhydrous with a water activity ≤ 0.55, and wherein the mass ratio of total boswellic acids to total curcuminoids is 0.8:1 to 1.6:1 and the mass ratio of menthol to total capsaicinoids is 10:1 to 30:1.;

Description

AREA OF INVENTION

[0001] The present invention relates to topical analgesic compositions. In particular, it relates to an anhydrous, polyherbal oleogel which provides standardized phytochemicals for the symptomatic relief of joint and muscle pain, including neuropathic pain, via a lamellar, penetration-controlled lipid matrix. BACKGROUND OF THE INVENTION

[0002] Conventional topical analgesics rely on single synthetic active ingredients (e.g., salicylates, local anesthetics, high-dose capsaicin) or mixtures of essential oils, which can be sensorially harsh, chemically unstable, and inconsistent in potency. Plant oils often lack standardization and exhibit insufficient dermal deposition, while high capsaicin levels limit user adherence. Therefore, there is a need for an anhydrous, solvent-free formulation from non-renewable sources that (i) uses standardized botanical extracts, (ii) provides rapid onset of action with minimal irritation, (iii) maintains the local availability of anti-inflammatory phytochemicals, and (iv) remains oxidation-stable in warm climates without synthetic preservatives. GOALS OF THE INVENTION

[0003] The invention aims to provide a polyherbal oleogel with a lamellar matrix structured by lecithin-beeswax-squalane, which acts as a dermal depot; the combined administration of CO2-selective extracts of Boswellia and ginger together with phospholipid-complexed curcumin and low-dose capsaicinoids under two ratio specifications that balance efficacy and tolerability; the maintenance of a water activity of ≤0.55 and narrow peroxide value limits under ICH-like stress testing using a dual antioxidant system; and the disclosure of a capsaicinoid-free, neuropathy-suitable variant that retains its efficacy through the synergy of gingerols, turmerones and Hypericum. SUMMARY OF THE INVENTION

[0004] The present invention relates to an anhydrous topical oleogel comprising (a) a carrier phase of sesame oil and medium-chain triglycerides (MCT) with castor oil and squalane, (b) a structuring phase of sunflower lecithin and beeswax, which yields a shear-thinning lamellar gel, (c) standardized phytochemical active ingredients - Boswellia serrata CO2-Select (boswellic acids), Curcuma longa phytosome (curcuminoids bound to phospholipids) with turmerone-rich turmeric oil, Zingiber officinale CO2-Select (gingerols / shogaols), Hypericum perforatum macerate oil and low doses of capsaicinoids - as well as terpenes with menthol and cineole as permeation enhancers, and (d) a dual antioxidant system of mixed tocopherols and a rosemary diterpene extract.Two inventive quantitative ratios control the performance: boswellic acids:curcuminoids at 0.8–1.6 w / w and menthol:total capsaicinoids at 10:1–30:1, resulting in rapid, well-tolerated counterstimulation with sustained anti-inflammatory efficacy. The composition is anhydrous (aw ≤ 0.55) and exhibits a peroxide value of ≤ 10 meq O2 / kg after 6 months at 40 °C / 75% RH. DETAILED DESCRIPTION OF THE INVENTION

[0005] Components and Standardization. The formulation uses a Boswellia CO2 Select extract, standardized to 65-75% total boswellic acids, including KBA / AKBA markers; a Curcuma phytosome in which 18-24% curcuminoids are complexed to phospholipids, along with a turmerone-rich turmeric essential oil; a Ginger CO2 Select extract with at least 20% total gingerols / shogaols; and a Hypericum macerate oil prepared in olive or sunflower oil. Capsicum oleoresin is used in a low dose and standardized to total capsaicinoids. Mentha piperita oil provides menthol, while Rosmarinus officinalis oil serves as a cineole source. The carrier system includes sesame oil, medium-chain triglycerides (C8-C10), castor oil, and squalane. The structuring is achieved via sunflower lecithin and beeswax; the oxidative stability is supported by mixed tocopherols and a rosemary diterpene antioxidant extract.All excipients are, where applicable, Ph.Eur. / USP compliant.

[0006] Quantity ranges (weight percent of the finished composition). The Boswellia CO2 Select extract is 1.0–5.0% (providing 0.65–3.75% boswellic acids). The Curcuma phytosome is 0.5–2.5% (providing 0.09–0.60% curcuminoids), with turmeric essential oil at 0.2–0.8%. The Ginger CO2 Select extract is 0.5–2.5%, the Hypericum macerate oil is 3.0–10.0%, and capsaicinoids from oleoresin are used at 0.01–0.05% equivalent (adjusted for content) or optionally below 0.001% in a neuropathic formulation. Peppermint oil (Mentha piperita) is present at 0.3–1.0%, and rosemary oil (cineole type) at 0.2–0.6%, optionally combined with eucalyptus oil at 0–0.4%. Sunflower lecithin is present at 0.8–2.0%, beeswax at 3.0–6.0%, and squalane at 1.0–3.0%. The sesame:MCT ratio is between 2:1 and 1:1, castor oil at 8–12%, mixed tocopherols at 0.1–0.3%, and rosemary antioxidant extract at 0.05–0.2%. The formulation is anhydrous with a water activity (aw) of no more than 0.55.

[0007] Matrix properties and performance limits. The lecithin-beeswax-squalane system forms a lamellar oleogel with thixotropy; at 25 °C, the storage modulus (G') at 1 Hz is typically 1–5 kPa and the yield strength 30–150 Pa (cone-plate rheometry), enabling rapid distribution while preventing leakage; after shearing, G' recovers at least 70% within 120 s. These functional specifications correlate with wearing comfort and dwell time, which are crucial for analgesic benefit.

[0008] Exemplary compositions (non-limiting). One embodiment for balanced relief contains, by weight percentage: sesame oil 35%, MCT 30%, castor oil 10%, squalane 2%, lecithin 1.5%, beeswax 4%, hypericum macerate oil 5%, boswellia extract 3%, turmeric phytosome 1%, turmeric essential oil 0.5%, ginger CO2 extract 1%, capsaicinoids at 0.025% equivalent, peppermint oil 0.8%, rosemary oil 0.4%, mixed tocopherols 0.2%, and rosemary antioxidant 0.1%. A neuropathy-friendly formulation reflects this composition, but reduces capsaicinoids to below 0.001% equivalent, increases hypericum to 6-9% and ginger CO2 to 1.5-2.0%, and limits peppermint oil to a maximum of 0.5%.

[0009] Manufacturing Overview. The carrier oils—sesame oil, MCT oil, castor oil, and squalane—are heated to 55–60 °C, dissolving the lecithin and melting the beeswax. The mixture is then cooled to approximately 40 °C before the CO2 extracts, phytosome, and St. John's wort oil are incorporated. If used, capsaicinoids are pre-diluted and added at this stage. Cooling continues to 35 °C or below; under nitrogen, the essential oils and antioxidants are added, the mixture is vacuum-deaerated, and filtered through a 5–10 µm polishing filter. The warm mixture is filled into amber glass or internally lacquered aluminum containers. The process yields a preservative-free, anhydrous product (aw ≤ 0.55) with peroxide values ​​within specified limits.

[0010] Advantages. The composition enables dual-action analgesia by combining rapid, well-tolerated counter-stimulation with sustained availability of anti-inflammatory agents; it establishes a lamellar depot that supports controlled dermal deposition; it relies on standardized phytochemicals to ensure batch consistency; it utilizes ratios that minimize irritation while creating a comfort-oriented warm / cold sensation; and it maintains high stability in warm climates without added water or synthetic preservatives.

[0011] Industrial applicability. The formulation is suitable for roll-on oils, tubes, dropper bottles or pump sprays for topical application in adults in sports, geriatric and occupational settings; both the composition and the manufacturing process are compatible with GMP requirements and designed for use in scalable mixing and filling lines.

Claims

[1] Topical polyherbal oleogel composition, comprising, in weight percent of the finished product: (i) Boswellia serrata CO2 select extract 1.0–5.0%; (ii) Curcuma longa phytosome 0.5–2.5% with curcuminoids complexed to phospholipids together with turmerone-rich turmeric essential oil 0.2–0.8%; (iii) Zingiber officinale CO2 select extract 0.5–2.5%; (iv) Hypericum perforatum macerate oil 3.0–10.0%; (v) Capsaicinoids in an equivalent amount of 0.01–0.05%, obtained from Capsicum oleoresin, and Mentha piperita oil 0.3–1.0% together with Rosmarinus officinalis oil 0.2–0.6%; (vi) a carrier phase of sesame oil and medium-chain triglycerides in a ratio of 2:1 to 1:1, and castor oil 8–12% and squalane 1.0–3.0%; (vii) a structuring phase of sunflower lecithin 0.8–2.0% and beeswax 3.0–6.0%, providing a lamellar, shear-thinning oleogel; and (viii) mixed tocopherols 0.1–0.3% and a rosemary diterpene antioxidant extract 0.05–0.2%;wherein the composition is anhydrous with a water activity ≤ 0.55, and wherein the mass ratio of total boswellic acids to total curcuminoids is 0.8:1 to 1.6:1 and the mass ratio of menthol to total capsaicinoids is 10:1 to 30:1.; [2] Composition according to claim 1, wherein the lecithin-beeswax-squalane matrix has a storage modulus (G') of 1-5 kPa at 1 Hz and a yield strength of 30-150 Pa at 25 °C and shows a recovery of ≥ 70 % of G' after high shear within 120 s, thereby achieving good distributability with sufficient residence time for dermal deposition of the active ingredients. [3] Composition according to claim 1, wherein curcumin is present exclusively as a phospholipid complex and the composition additionally comprises turmerone-rich turmeric essential oil 0.2-0.8% as a terpenoid permeability cofactor, such that the boswellic acid:curcuminoid ratio of 0.8-1.6 is maintained, while capsaicinoids ≤ 0.05% (equivalent) and menthol 0.3-1.0% are achieved to provide a rapid but low-irritant counterstimulation. [4] Composition according to claim 1, wherein the antioxidant system and the anhydrous matrix provide oxidative stability, characterized by a peroxide value ≤ 10 meq O2 / kg after 6 months at 40 °C / 75 % r. F. and a retention of menthol and 1,8-cineole content within ± 15 % of the initial value over the same period. [5] Composition according to claim 1, wherein capsaicinoids are absent or present in < 0.001% (equivalent) and the Zingiber officinale CO2 Select extract is 1.5-2.5%, the Hypericum macerate oil is 6.0-10.0% and the Mentha piperita oil is ≤ 0.5%, thereby providing a neuropathy-friendly variant that retains the analgesic benefit with reduced sensory stimulation.