A composition with antioxidant lightening effect and inhibiting lipofuscin level, and a preparation method and application thereof

Abstract

This invention belongs to the field of cosmetic technology, and particularly relates to a composition with antioxidant and brightening effects and inhibition of lipofuscin levels, its preparation method, and its application. This composition achieves synergistic effects through the compounding of specific weight parts of tetrahydrocurcumin, glycyrrhizic acid, stearyl glycyrrhetinic acid ester, *Dalbergia odorifera* extract, and *Paeonia suffruticosa* root bark extract. Tetrahydrocurcumin scavenge free radicals and regulates lipofuscin; glycyrrhizic acid and stearyl glycyrrhetinic acid ester construct a dual anti-inflammatory barrier; and *Dalbergia odorifera* extract and *Paeonia suffruticosa* root bark extract synergistically combat glycation and improve skin tone. This invention achieves comprehensive effects of antioxidation, anti-inflammation, anti-glycation, and lipofuscin regulation through multi-target synergy, gently addressing skin aging, dullness, and lipofuscin deposition, balancing high efficacy with gentleness, and is suitable for various skin types.

Description

Technical Field

[0001] This invention belongs to the field of cosmetic technology, and particularly relates to a composition with antioxidant and brightening effects and the ability to inhibit lipofuscin levels, as well as its preparation method and application. Background Technology

[0002] The appearance of dull, lackluster skin and signs of aging is closely related to the abnormal accumulation of lipofuscin in skin cells. Lipofuscin, an oxidative waste product generated during cell metabolism, mainly accumulates in the basal cells of the epidermis and fibroblasts of the dermis, especially in lysosomes. Its accumulation not only directly leads to a "yellowish" complexion and the formation of age spots and other pigmentation, but also affects the normal metabolic function of cells, exacerbates collagen loss, and causes the skin to lose elasticity and transparency. It is one of the core causes of dull, yellowish skin and aging.

[0003] Currently, the mainstream technologies on the market for addressing skin dullness and aging caused by lipofuscin mainly focus on three areas: traditional whitening and anti-oxidation, chemical peels, and traditional anti-aging. However, all of these existing technologies have significant limitations and cannot fundamentally solve the skin problems caused by lipofuscin accumulation. Specific shortcomings are as follows: Firstly, traditional whitening / antioxidant agents (such as vitamin C, vitamin E, arbutin, and kojic acid) primarily work by reducing melanin intermediates, inhibiting tyrosinase activity, or providing electrons to scavenge free radicals. Their core target is melanin, but they lack effective action against lipofuscin, another key culprit behind yellowing skin and age spots. These ingredients struggle to penetrate cells and enter lysosomes, making it impossible to degrade and eliminate lipofuscin. Furthermore, their stability is poor; for example, L-ascorbic acid is easily oxidized and discolored, not only losing its original activity but also potentially producing a pro-oxidative effect that damages skin cells. In addition, these ingredients act only superficially, reaching the epidermis and failing to address lipofuscin accumulated in dermal fibroblasts. The accumulation of lipofuscin in the dermis is the underlying cause of loss of skin elasticity and transparency, thus failing to fundamentally improve dullness and aging skin.

[0004] Secondly, chemical peels (using glycolic acid or salicylic acid) work by accelerating the metabolism of the stratum corneum, quickly removing pigmented keratinocytes from the surface. This only provides temporary radiance and is a superficial solution. This technique does not reduce the total amount of lipofuscin within the basal cells or fibroblasts of the skin, failing to address the core issue of lipofuscin accumulation. Furthermore, long-term use of this technique can damage the skin barrier, leading to skin sensitivity, redness, and potentially increasing the risk of post-inflammatory hyperpigmentation (pigmentation over hyperpigmentation), making it relatively unsafe. In addition, lipofuscin is primarily found inside cells, especially within lysosomes, and cannot be removed through surface exfoliation; therefore, this technique has no direct inhibitory or clearing effect on lipofuscin.

[0005] Thirdly, traditional anti-aging ingredients (such as retinol) primarily stimulate collagen regeneration and accelerate cell renewal, but they have significant limitations. On one hand, retinol is highly irritating, easily causing skin peeling and stinging, and has poor tolerance, making it unsuitable for people with sensitive skin. On the other hand, these ingredients do not directly target lipofuscin, a waste product of aging. Although they can accelerate cell metabolism, they cannot help aging cells with impaired autophagy and reduced clearance ability to clear accumulated lipofuscin granules. Since the cell's own metabolic function is not restored, even if collagen regeneration is stimulated, the anti-aging and brightening effects are only partially achieved, failing to address the root cause of skin dullness and aging problems caused by lipofuscin accumulation.

[0006] In summary, current technologies cannot effectively target and eliminate lipofuscin, and they have significant shortcomings in terms of safety, depth of action, and duration of effect, failing to meet consumers' needs for gentle, effective, and fundamentally improved skin tone, brightening, and anti-aging solutions. Therefore, developing a composition that can precisely target lipofuscin, possess antioxidant and brightening effects, and is gentle, safe, and deeply effective has become a pressing technical problem to be solved in the current skin care field. Summary of the Invention

[0007] The purpose of this invention is to overcome the shortcomings of the prior art and provide a composition with antioxidant brightening effects and inhibition of lipofuscin levels, as well as its preparation method and application. The composition not only provides antioxidant effects through conventional pathways but also specifically inhibits the production of intracellular lipofuscin or promotes its degradation, thereby achieving multi-target skin brightening and anti-aging effects.

[0008] To achieve the above objectives, the technical solution adopted by the present invention includes: In a first aspect, the present invention provides a composition having antioxidant and brightening effects and inhibiting lipofuscin levels, the composition comprising the following components in parts by weight: 0.0001-5 parts of tetrahydrocurcumin, 0.0001-5 parts of glycyrrhizic acid, 0.0001-5 parts of stearyl glycyrrhetinic acid ester and 0.0001-5 parts of peony root bark extract.

[0009] Addressing the technical challenges of poor stability and poor penetration of ordinary curcumin, this invention selects tetrahydrocurcumin (the main metabolite of curcumin) as its core component. Its stronger lipophilicity allows it to easily penetrate skin cell membranes and directly act on mitochondria, precisely eliminating superoxide anions and inhibiting the formation of lipofuscin precursors (lipid peroxides) at their source. Simultaneously, relying on its extremely high stability, it continues to exert its effects, effectively reducing the accumulation of lipofuscin in the skin and fundamentally improving sallow and dull skin conditions. This overcomes the limitations of traditional antioxidants that only act on the epidermis and target a single point.

[0010] Addressing the core issues of skin aging and lipofuscin deposition accompanied by chronic low-grade inflammation, this invention constructs a bidirectional positive-cycle action system through the layered intervention of dual licorice components. Glycyrrhizic acid rapidly acts on the epidermis, effectively neutralizing inflammatory factors and quickly alleviating chronic skin inflammation. Stearyl glycyrrhizinate (a lipid-modified derivative of glycyrrhizic acid) has stronger skin affinity and a longer residence time in the skin, slowly releasing anti-inflammatory activity and forming an "invisible anti-inflammatory protective film" on the skin surface for long-lasting anti-inflammatory effects. Both components reduce free radical production by inhibiting the NF-κB inflammatory pathway; while tetrahydrocurcumin is responsible for scavenging existing free radicals, which in turn reduces skin inflammation, forming a bidirectional regulatory mechanism of "anti-inflammatory reduction of free radicals and antioxidant relief of inflammation," effectively delaying the skin aging process and reducing the risk of inflammation-induced pigmentation.

[0011] Addressing the complex origins of yellowish skin (melanin + lipofuscin causing waxy / dull yellowing + glycation end products), this invention achieves multi-target, three-dimensional improvement through a four-component synergistic approach. Tetrahydrocurcumin targets and inhibits lipofuscin production, resolving the core waxy / dull yellowing issue; the licorice component reduces post-inflammatory hyperpigmentation through anti-inflammatory effects, indirectly assisting in improving the yellowing caused by melanin; the active ingredient paeonol from peony root bark extract helps scavenge free radicals, while slightly dilating capillaries to improve "stagnant dullness" caused by poor blood circulation, and removes AGEs, resolving the yellowing caused by glycation end products, comprehensively brightening skin tone for a more even and radiant complexion.

[0012] In summary, this invention achieves gentle and effective skincare by synergistically regulating the skin's physiological environment through multiple components. Tetrahydrocurcumin, in addition to scavenging free radicals and inhibiting lipid peroxidation, also regulates autophagy; glycyrrhizic acid and stearyl glycyrrhetinic acid esters construct an anti-inflammatory barrier while regulating the autophagic environment; peony root bark extract helps improve skin microcirculation and remove glycation products. These three components, synergistically with tetrahydrocurcumin, form a complete closed loop of "inhibition-scavenging-repair-brightening." Compared to traditional irritating ingredients such as fruit acids and retinol, all components of this invention are gentle and safe, with no significant irritation, suitable for all skin types. It addresses skin problems while protecting the skin barrier, achieving a unified approach of "gentle skincare + systemic improvement," fundamentally addressing the core pain points of skin aging, dullness, and lipofuscin deposition.

[0013] Preferably, the composition comprises the following components in parts by weight: 0.001-0.1 parts of tetrahydrocurcumin, 0.001-0.1 parts of glycyrrhizic acid, 0.001-0.1 parts of stearyl glycyrrhetinic acid ester, and 0.01-1 parts of peony root bark extract.

[0014] Preferably, the composition comprises the following components in parts by weight: 0.1 parts tetrahydrocurcumin, 0.1 parts glycyrrhizic acid, 0.1 parts stearyl glycyrrhetinic acid ester, and 1 part peony root bark extract.

[0015] Experimental studies have revealed that the optimal proportions of the four core components—tetrahydrocurcumin, glycyrrhizic acid, stearyl glycyrrhetinic acid ester, and peony root bark extract—play a crucial role in the overall synergistic effects of the composition in terms of antioxidant activity, skin brightening, and inhibition of lipofuscin levels. The aforementioned proportions represent the optimal range determined through experimental verification. When the four components are combined according to these proportions, the synergistic effects of each component are maximized, effectively avoiding the problem of weakened efficacy or synergistic failure caused by improper dosage of a single component. This maximizes the overall skincare efficacy of the composition, better achieving the core objectives of gently and effectively regulating the skin's physiological environment, improving skin aging and dullness, and inhibiting lipofuscin deposition.

[0016] Preferably, the composition further comprises the following components in parts by weight: 0.001-0.5 parts of palm wood extract.

[0017] Preferably, the composition further comprises the following components in parts by weight: 0.01-0.2 parts of palm wood extract.

[0018] More preferably, the composition further comprises the following component in parts by weight: 0.1 parts of palm wood extract.

[0019] Dalbergia odorifera extract can effectively inhibit the transfer of melanin to keratinocytes, helping to improve the dark yellowing problem caused by melanin. It complements the anti-inflammatory and lightening effects of licorice components, further reducing pigmentation. At the same time, its anti-glycation effect can precisely remove existing AGEs, specifically addressing the "caramel yellow" problem. It works synergistically with the anti-glycation effects of peony root bark extract, filling the gap in the original system's ability to improve yellowing caused by glycation, thereby further assisting in brightening the skin tone.

[0020] Secondly, the present invention provides a method for preparing the aforementioned composition, comprising the following steps: Mix all components thoroughly to obtain the composition.

[0021] Thirdly, the present invention provides the use of the described composition in the preparation of cosmetics.

[0022] Preferably, the cosmetic product includes at least one of serum, lotion, cream, mask, eye cream, and gel.

[0023] Fourthly, the present invention provides a cosmetic having antioxidant and brightening effects and inhibiting lipofuscin levels, the cosmetic comprising the aforementioned composition.

[0024] Preferably, the composition has a mass percentage content of 0.01-5% in the cosmetic.

[0025] Compared with the prior art, the beneficial effects of the present invention are as follows: The composition of this invention is based on "anti-inflammatory as a foundation and lipid metabolism as a target." It achieves synergistic effects through the combination of specific weight parts of tetrahydrocurcumin, glycyrrhizic acid, stearyl glycyrrhetinic acid ester, Dalbergia odorifera extract, and Paeonia suffruticosa root bark extract. It can gently and systematically solve the problems of skin aging, dullness, and lipofuscin deposition. Among them, tetrahydrocurcumin can scavenge free radicals, inhibit lipid peroxidation, and regulate autophagy, inhibiting and metabolizing lipofuscin from the root. Glycyrrhizic acid and stearyl glycyrrhetinic acid ester can target and inhibit the NF-κB inflammatory pathway, reduce the levels of inflammatory factors such as IL-6 and TNF-α, build a dual anti-inflammatory barrier, and optimize the autophagy environment. Dalbergia odorifera extract and Paeonia suffruticosa root bark extract synergistically clear AGEs, solve the yellowing of skin caused by glycation, and at the same time help improve skin microcirculation and reduce melanin transport. The multi-target synergistic effect achieves comprehensive effects of anti-oxidation, anti-inflammation, anti-glycation, and lipofuscin regulation, taking into account both skin-care efficacy and skin gentleness, and is suitable for a variety of skin types. Attached Figure Description

[0026] Figure 1 This is a picture showing the finished product appearance of the composition described in Example 1. Detailed Implementation

[0027] To better illustrate the objectives, technical solutions, and advantages of this invention, the invention will be further described below with reference to specific embodiments. Those skilled in the art should understand that the specific embodiments described herein are merely illustrative of the invention and are not intended to limit the invention.

[0028] Unless otherwise specified, the raw materials used in the following examples and comparative examples are all available through conventional commercial channels.

[0029] Examples 1-6 Examples 1-6 provide compositions that have antioxidant and brightening effects and inhibit lipofuscin levels, respectively. The formulations of the compositions are shown in Table 1. The compositions are obtained by mixing all components evenly.

[0030] Table 1. Formulation table of the compositions described in Examples 1-6 (mass percentage %) Comparative Examples 1-7 Comparative Examples 1-7 each provide a composition, the formulation of which is shown in Table 2. The composition is obtained by uniformly mixing all components.

[0031] Table 2 shows the formulations (mass percentage) of the compositions described in Comparative Examples 1-7. Comparative Example 8 This comparative example provides a composition that differs from Example 1 only in that an equal amount of Tremella fuciformis extract is used to replace Paeonia lactiflora root bark extract, while the remaining components and amounts remain unchanged.

[0032] Comparative Example 9 This comparative example provides a composition that differs from Example 1 only in that an equal amount of silver curcumin is used to replace tetrahydrocurcumin, while the remaining components and amounts remain unchanged.

[0033] Example 1 Lipofuscin is a yellowish-brown pigment produced during cell aging and can be specifically stained with Sudan Black B. The stained complex exhibits characteristic absorbance at a specific wavelength. This method uses human skin fibroblasts as a cell model to construct a lipofuscin deposition model. The compositions described in Examples 1-6 and Comparative Examples 1-9 of this invention were added as test samples. After staining with Sudan Black B, the absorbance values ​​were measured using an ELISA reader. The relative change in absorbance reflects the inhibitory effect of the composition on the relative content of lipofuscin. The lower the absorbance, the better the composition's effect on inhibiting lipofuscin deposition and promoting lipofuscin metabolism. The specific test method is as follows: 1. Cell inoculation 1.1 Human skin fibroblasts in logarithmic growth phase were harvested, digested with 0.25% trypsin-EDTA, resuspended in DMEM medium containing 10% FBS + 1% penicillin-antibody solution, and the cell density was adjusted to 1.5 × 10⁻⁶ cells / year. 5 per mL.

[0034] 1.2 Seed the cell suspension into 96-well plates at 100 μL per well (i.e., 1.5 × 10⁶ cells per well). 4 (cells).

[0035] 1.3 Place the 96-well plate in a 37°C, 5% CO2 incubator for 24 hours to pre-culture until the cells are fully adhered and have a confluence of about 50%.

[0036] 2. Establishment of a lipofuscin deposition model (H2O2-induced method) 2.1 Preparation of induction solution: Freshly prepare 200 μmol / L H2O2 using serum-free DMEM medium (protect from light, prepare and use immediately).

[0037] 2.2 Discard the old culture medium in the 96-well plate and add 100 μL of serum-free DMEM containing 200 μmol / L H2O2 to each well.

[0038] 2.3 Return the 96-well plate to the incubator and continue culturing for 48 hours. Replace the medium with fresh H2O2 every 24 hours during this period.

[0039] 2.4 After 48 hours, the culture medium containing H2O2 was aspirated, and 100 μL of serum-free DMEM was added to each well to gently rinse once to remove residual H2O2. At this point, the lipofuscin deposition cell model is established.

[0040] Control settings: Blank control group (normal cells) were not treated with H2O2 and were cultured in serum-free DMEM for 48 hours (the medium was changed every 24 hours).

[0041] 3. Sample preparation 3.1 Sample preparation: Each test composition (Examples 1-6, Comparative Examples 1-9) was prepared into a stock solution of 10 mg / mL using sterile DMSO. The stock solution was diluted to a 0.5% experimental concentration with DMEM containing 2% FBS immediately before use.

[0042] Solvent control group (negative control): 2% FBS-DMEM containing an equal volume of DMSO.

[0043] 3.2 Drug administration grouping (3 replicates per group): Blank control group: Normal cells (uninduced) were added to 100 μL of 2% FBS-DMEM containing solvent (0.1% DMSO).

[0044] Model control group: Lipofuscin deposition model cells, with 100 μL of 2% FBS-DMEM containing solvent.

[0045] Sample group: Lipofuscin deposition model cells, with 100 μL of 2% FBS-DMEM containing the test composition.

[0046] 3.3 Place the 96-well plate with the added drug back into the incubator and continue culturing for 48 hours.

[0047] 4. Sudan Black B staining and absorbance determination 4.1 Cell fixation: After drug administration and culture, discard the culture medium in the wells. Add 100 μL of pre-cooled 4% paraformaldehyde to each well and fix at room temperature for 15 minutes.

[0048] 4.2 Washing: Discard the fixative, add 150 μL of PBS to each well, gently shake and wash for 2 minutes, then discard. Repeat the washing once (for a total of 2 times).

[0049] 4.3 Preparation of Sudan Black B dye solution: Weigh 0.3g of Sudan Black B powder and dissolve it in 100mL of 70% ethanol. Heat and stir in a 60℃ water bath until completely dissolved, then cool to room temperature. Filter with qualitative filter paper to remove undissolved particles. Store the dye solution away from light and use within one week.

[0050] 4.4 Staining: Add 100 μL of Sudan Black B staining solution to each well and stain at room temperature in the dark for 30 minutes.

[0051] 4.5 Destaining and Washing: Discard the staining solution, add 150 μL of 70% ethanol to each well, shake gently for 3 minutes, and discard. Repeat the washing with 70% ethanol twice to remove unbound dye. Finally, wash once with 150 μL of PBS and discard.

[0052] 4.6 Dye extraction: Add 100 μL of isopropanol (or isopropanol containing 0.1% Triton X-100) to each well, place on a shaker at room temperature and extract for 20 minutes to fully dissolve the Sudan Black B-lipofuscin complex in the cells.

[0053] 4.7 Absorbance Measurement: Transfer the extract to a new 96-well plate. Measure the absorbance of each well at 600 nm using a microplate reader. D600 ).

[0054] Relative lipofuscin content (%) = (OD value of sample group / OD value of model control group) × 100% Table 3. Results of the test on the relative content of lipofuscin in the cell model. Table 3 shows that the compositions (Examples 1-6) prepared from the four core active ingredients—tetrahydrocurcumin, glycyrrhizic acid, stearyl glycyrrhetinic acid ester, and peony root bark extract—had significantly lower relative lipofuscin content than the comparative examples. Example 1, as the optimal technical solution of this invention, achieved the best inhibition of lipofuscin formation, demonstrating the outstanding technical advantages of this invention in brightening the skin and improving skin texture.

[0055] When the compositions described in Comparative Examples 1-7 lack any one of tetrahydrocurcumin, glycyrrhizic acid, stearyl glycyrrhetinic acid ester, or peony root bark extract, and the total formulation weight is the same as in Example 1, the inhibitory ability of the compositions on lipofuscin drops sharply. This fully demonstrates that the above four core components are indispensable in this invention, and together they constitute a highly efficient synergistic system. The absence of any single component will destroy the overall technical effect.

[0056] In Comparative Examples 8-9, when other active components with similar effects were used to replace peony root bark extract and tetrahydrocurcumin, the overall efficacy of the composition was not maintained, and the lipofuscin inhibition effect was significantly lower than that of the embodiments of the present invention. This indicates that the selection of the core components described in the present invention is not a conventional choice in the art, and the synergistic mechanism between its components cannot be obtained through simple substitution or conventional experiments. If the core components are arbitrarily replaced, the synergistic effect between the components will be directly weakened, thereby leading to a significant decrease in the lipofuscin inhibition and antioxidant brightening effects of the composition.

[0057] The above results fully demonstrate that the four core components in this technical solution constitute an inseparable and mutually reinforcing organic whole. The absence or substitution of any component will disrupt this synergistic balance, resulting in a significant decrease in the final overall efficacy.

[0058] Finally, it should be noted that the above embodiments are used to illustrate the technical solutions of the present invention and not to limit the scope of protection of the present invention. Although the present invention has been described in detail with reference to preferred embodiments, those skilled in the art should understand that modifications or equivalent substitutions can be made to the technical solutions of the present invention without departing from the essence and scope of the technical solutions of the present invention.

Claims

1. A composition having antioxidant and brightening effects and inhibiting lipofuscin levels, characterized in that, The composition comprises the following components in parts by weight: 0.0001-5 parts tetrahydrocurcumin, 0.0001-5 parts glycyrrhizic acid, 0.0001-5 parts stearyl glycyrrhetinic acid ester, and 0.0001-5 parts peony root bark extract.

2. The composition according to claim 1, characterized in that, The composition comprises the following components in parts by weight: 0.001-0.1 parts tetrahydrocurcumin, 0.001-0.1 parts glycyrrhizic acid, 0.001-0.1 parts stearyl glycyrrhetinic acid ester, and 0.01-1 parts peony root bark extract.

3. The composition according to claim 1 or 2, characterized in that, The composition also includes the following components in parts by weight: 0.001-0.5 parts of palm wood extract.

4. The composition according to claim 3, characterized in that, The composition also includes the following components in parts by weight: 0.01-0.2 parts of palm wood extract.

5. The method for preparing the composition according to any one of claims 1-4, characterized in that, Includes the following steps: Mix all components thoroughly to obtain the composition.

6. The use of the composition according to any one of claims 1-4 in the preparation of cosmetics.

7. The application as described in claim 6, characterized in that, The cosmetics include at least one of serums, lotions, creams, masks, eye creams, and gels.

8. A cosmetic product with antioxidant and brightening effects and inhibition of lipofuscin levels, characterized in that, The cosmetic product includes the composition according to any one of claims 1-4.

9. The cosmetic product as described in claim 8, characterized in that, The composition has a mass percentage of 0.01-5% in cosmetics.

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