Synergistic toothpaste composition containing liposome vitamin C and ascorbyl palmitate

Abstract

The invention relates to a toothpaste composition, in particular to a synergistic toothpaste composition containing lipidosome vitamin C and ascorbyl palmitate, which remarkably enhances the effects of improving gingival health and repairing oral cavity through the synergistic effect of lipidosome VC and L-AP. The toothpaste comprises the following components in percentage by mass: 45%-60% of a humectant, 10%-20% of a friction agent, 2%-3% of a cleaning agent, 0.5%-1.5% of an adhesive, 0.1%-0.2% of a sweetening agent, 0.1%-0.2% of a preservative, 0.5%-1.5% of L-ascorbyl palmitate, 1%-3% of liposome vitamin C, 0.3%-0.7% of vitamin E, 5%-10% of vitamin B, 2%-5% of zinc gluconate and the balance of water. Cell experiments and clinical data prove that the composition can remarkably promote gingival fibroblast proliferation, enhance I-type collagen expression and effectively improve the problems of gingival bleeding, swelling and pain, oral ulcer and the like.

Description

Technical Field

[0001] This invention relates to an oral care product, and more particularly to a synergistic toothpaste composition containing liposomal vitamin C (liposomal VC) and ascorbate palmitate (L-AP). This composition significantly enhances the efficacy of maintaining gum health and repairing oral tissues through the synergistic effect of the two types of fat-soluble vitamin C derivatives. Background Technology

[0002] As a daily oral hygiene product, toothpaste, in addition to its basic cleaning function, is increasingly focusing on the prevention and adjunctive treatment of oral diseases. Common oral problems include gingivitis, periodontitis, bleeding gums, and oral ulcers, which are closely related to oxidative stress, inflammatory responses, and extracellular matrix degradation.

[0003] Vitamin C is a key nutrient for maintaining healthy gums, but its water-soluble nature results in a short residence time in the oral cavity and low cell permeability, limiting its bioavailability and efficacy. Although fat-soluble derivatives such as L-ascorbate palmitate (L-AP) have been used, their stability and sustained-release effects remain insufficient when used alone. Therefore, developing a toothpaste composition that combines liposomal vitamin C and L-AP to synergistically enhance cell permeability, stability, and bioactivity has become an important direction for improving the efficacy of oral care products. Summary of the Invention

[0004] The purpose of this invention is to provide a synergistic toothpaste composition containing liposomal vitamin C and ascorbate palmitate, which enhances antioxidant, anti-inflammatory and tissue repair capabilities through the synergistic effect of the two, and significantly improves gum health and oral ulcers.

[0005] To achieve the above objectives, the present invention provides the following technical solution: a synergistic toothpaste composition containing liposomal vitamin C and ascorbyl palmitate, wherein the toothpaste composition is made of the following components by weight percentage: 45%–60% humectant, 10–20% abrasive, 2–3% detergent, 0.5–1.5% binder, 0.1–0.2% sweetener, 0.1–0.2% preservative, 0.5–1.5% L-ascorbyl palmitate, 1–3% liposomal vitamin C, 0.3–0.7% vitamin E, 5–10% B vitamins, 2–5% zinc gluconate, and the balance being water.

[0006] The liposome vitamin C is encapsulated using nanoliposome technology. The particle size of the liposome vitamin C is 50–200 nm, and the encapsulation rate is not less than 85%, which can significantly improve the stability, cell permeability and sustained release effect of vitamin C.

[0007] Compared with the prior art, the beneficial effects of the present invention are: Synergistic Mechanism Explanation: The core innovation of this invention lies in the first-time combination of liposomal vitamin C (liposomal VC) and L-ascorbate palmitate (L-AP). Through the synergistic effect of the two, a multi-dimensional improvement in oral health maintenance is achieved. This synergistic mechanism is mainly reflected in the following aspects: 1. Complementary Optimization of Permeation Pathway and Duration of Action: L-AP, as a small-molecule lipid-soluble derivative, has a molecular size close to the nanometer scale, enabling it to directly enter the cell membrane within seconds through the intercellular spaces of the oral mucosa, exerting rapid antioxidant and anti-inflammatory effects. Liposome vitamin C, encapsulated using nanoliposome technology, forms stable 50-200 nm particles, which not only protect vitamin C from oxidative degradation but also allow for slow release of vitamin C through intracellular mechanisms, prolonging the duration of action. The combination of the immediate effect of L-AP and the sustained-release properties of liposome vitamin C achieves the dual advantages of "rapid onset of action + long-lasting effect," significantly improving bioavailability.

[0008] 2. Synergistic Enhancement of Antioxidant and Anti-inflammatory Capabilities: L-AP retains the dienol structure of ascorbic acid, providing hydrogen atoms to neutralize free radicals and eliminating them through disproportionation. Its antioxidant activity in the sodium dodecyl sulfate system is significantly higher than that of ordinary vitamin C. Liposome vitamin C is delivered via nanocarriers, continuously releasing vitamin C within cells and further strengthening the antioxidant network. The combined use of both can significantly reduce oxidative stress levels, inhibit the overexpression of MMPs (matrix metalloproteinases), reduce extracellular matrix degradation (such as type I collagen), enhance leukocyte phagocytosis, alleviate inflammatory responses, and promote tissue repair.

[0009] 3. Synergistic Repair Mechanisms at the Cellular Level: L-AP can directly penetrate into the cell interior, participating in amino acid metabolism and neurotransmitter synthesis, reducing capillary permeability, and stimulating lysozyme secretion, rapidly improving ulcer symptoms. Liposome vitamin C, on the other hand, continuously promotes collagen synthesis and cell proliferation (such as fibroblasts) through the slow release of vitamin C. A CTI test report (RG250335-2) shows that toothpaste containing L-AP can significantly increase the expression level of type I collagen genes (34.64%–81.49%); report RG250335-1 further confirms that it promotes cell proliferation by 20.46%–39.86%. The combination of the two exhibits a significant synergistic effect in cell proliferation and matrix synthesis.

[0010] 4. Enhanced Stability and Bioavailability: L-AP's stability is improved through palmitic acid modification, but it remains susceptible to environmental factors when used alone. Liposome vitamin C, encapsulated in a lipid bilayer, isolates oxygen and moisture, further enhancing vitamin C's stability. Both protect each other within the toothpaste matrix, extending the shelf life of the active ingredients, while significantly improving cellular absorption efficiency via the lipid-soluble pathway (4-5 times higher than water-soluble vitamin C).

[0011] 5. Systematic synergy with other active ingredients: This invention further integrates B vitamins, vitamin E, and zinc gluconate to form multiple compound effects: B vitamins (B1, B2, B6, nicotinamide, etc.) participate in the metabolism of sugars, fats, and amino acids, promote mucosal regeneration and ulcer healing, and work with vitamin C to scavenge free radicals; Vitamin E, as a fat-soluble antioxidant, prevents lipid peroxidation, relieves pain, and accelerates ulcer healing. Zinc gluconate eliminates reactive oxygen species under Zn²⁺ mediation, promotes DNA / RNA synthesis and cell division, enhances immune response, and works with vitamin C to maintain the health of gingival microvessels.

[0012] In summary, the combination of liposomal vitamin C and L-AP not only overcomes the limitations of traditional vitamin C products, such as short duration of action and poor permeability, but also achieves comprehensive treatment of oral problems through multi-mechanism synergy, providing solid technical support for the efficacy upgrade of toothpaste products.

[0013] The efficacy verification data comes from CTI testing reports (Nos. RG250335-1 and RG250335-2): Report RG250335-2 shows that toothpaste containing L-AP at concentrations of 0.25%–0.0625% can significantly increase the expression level of type I collagen genes (34.64%–81.49%), effectively improving gum health; Report RG250335-1 shows that similar toothpastes at concentrations of 0.00016%–0.02% can promote the proliferation rate of human gingival fibroblasts by 20.46%–39.86%, supporting oral repair efficacy; The above data corroborate that the combination of L-AP and liposome VC can further broaden the effective concentration range and enhance the repair response at the cellular level. Detailed Implementation

[0014] The technical solutions in the embodiments of the present invention will be clearly and completely described below. Obviously, the described embodiments are only some embodiments of the present invention, and not all embodiments. Based on the embodiments of the present invention, all other embodiments obtained by those skilled in the art without creative effort are within the scope of protection of the present invention.

[0015] This invention provides a technical solution for a synergistic toothpaste composition containing liposomal vitamin C and ascorbyl palmitate: the toothpaste composition is made of the following components by weight percentage: 45%–60% humectant, 10–20% abrasive, 2–3% detergent, 0.5–1.5% binder, 0.1–0.2% sweetener, 0.1–0.2% preservative, 0.5–1.5% L-ascorbyl palmitate, 1–3% liposomal vitamin C, 0.3–0.7% vitamin E, 5–10% B vitamins, 2–5% zinc gluconate, and the balance being water.

[0016] The particle size of plastid vitamin C is 50–200 nm, and the encapsulation efficiency is not less than 85%. Preferred embodiment: The toothpaste composition is made from the following raw materials by weight percentage: humectant 54.8%, abrasive 15%, detergent 2.5%, binder 1.0%, sweetener 0.15%, preservative 0.15%, L-ascorbic acid palmitate 0.9%, liposomal vitamin C 2%, vitamin E 0.5%, B vitamins 7%, zinc gluconate 3%, and the balance is water.

[0017] The humectant is sorbitol and PEG-400, or sorbitol or PEG-400; the abrasive is hydrated silica; the detergent is sodium dodecyl sulfate; the adhesive is a combination of cellulose gum and xanthan gum; the sweetener is sodium saccharin; and the preservative is sodium benzoate.

[0018] Examples 1–4: Toothpaste prepared according to the formulations in Table 1: Table 1: Toothpaste Ingredients (Percentage by Mass);

[0019] Preparation method: The above raw materials can be mixed, homogenized, degassed, and filled using conventional toothpaste processing methods.

[0020] Experimental Example 1: Cell-level efficacy verification.

[0021] CTI Testing Report RG250335-2: In the oxidative damage cell model, toothpaste samples containing L-AP at concentrations of 0.0625%–0.25% showed a significant increase in the expression level of type I collagen (COL1) gene by 34.64%–81.49% (P<0.05). Citation report RG250335-1: The same toothpaste at concentrations of 0.00016%–0.02% promoted gingival fibroblast proliferation by 20.46%–39.86%.

[0022] Experimental Example 2: Clinical efficacy verification.

[0023] One hundred and fifty patients with oral ulcers were randomly divided into five groups (four example groups + one control group). They were given 1g twice daily while brushing their teeth for seven days. The results are shown in the table below: Table 2: Treatment results for oral ulcers:

[0024] Experimental Example 3: Improvement of Gingivitis and Tooth Loosening

[0025] One hundred patients aged 40–60 years were selected and grouped as in Experiment 2. The results after 15 days of treatment are as follows: Table 3: Results of Gum Problem Improvement

[0026] The above results show that the toothpaste composition of the present invention is significantly superior to ordinary commercially available products, with Example 3 showing the best performance.

[0027] The embodiments described are merely illustrative examples. Those skilled in the art can adjust the component ratios and processes within the scope of the claims, and such modifications still fall within the protection scope of this invention.

[0028] Although embodiments of the invention have been shown and described, it will be understood by those skilled in the art that various changes, modifications, substitutions and alterations can be made to these embodiments without departing from the principles and spirit of the invention, the scope of which is defined by the appended claims and their equivalents.

Claims

1. A toothpaste composition containing liposomal vitamin C and ascorbate palmitate, characterized in that: The toothpaste composition is made of the following components by weight percentage: 45%–60% humectant, 10–20% abrasive, 2–3% detergent, 0.5–1.5% binder, 0.1–0.2% sweetener, 0.1–0.2% preservative, 0.5–1.5% L-ascorbic acid palmitate, 1–3% liposomal vitamin C, 0.3–0.7% vitamin E, 5–10% B vitamins, 2–5% zinc gluconate, and the balance being water.

2. The toothpaste composition containing liposomal vitamin C and ascorbate palmitate according to claim 1, characterized in that: The liposome vitamin C has a particle size of 50–200 nm and an encapsulation efficiency of not less than 85%.

3. The toothpaste composition containing liposomal vitamin C and ascorbate palmitate according to claim 2, characterized in that: The toothpaste composition is made from the following ingredients by weight percentage: 54.8% humectant, 15% abrasive, 2.5% detergent, 1.0% binder, 0.15% sweetener, 0.15% preservative, 0.9% L-ascorbic acid palmitate, 2% liposomal vitamin C, 0.5% vitamin E, 7% B vitamins, 3% zinc gluconate, and the balance being water.

4. A toothpaste composition containing liposomal vitamin C and ascorbate palmitate according to any one of claims 1–3, characterized in that: The moisturizers are sorbitol and PEG-400.

5. A toothpaste composition containing liposomal vitamin C and ascorbate palmitate according to any one of claims 1-3, characterized in that: The friction agent is hydrated silica.

6. A toothpaste composition containing liposomal vitamin C and ascorbate palmitate according to any one of claims 1-3, characterized in that: The cleaning agent is sodium dodecyl sulfate.

7. A toothpaste composition containing liposomal vitamin C and ascorbate palmitate according to any one of claims 1-3, characterized in that: The adhesive is a combination of cellulose gum and xanthan gum.

8. A toothpaste composition containing liposomal vitamin C and ascorbate palmitate according to any one of claims 1–3, characterized in that: The sweetener is sodium saccharin.

9. A toothpaste composition containing liposomal vitamin C and ascorbate palmitate according to any one of claims 1–3, characterized in that: The preservative is sodium benzoate, and the humectant is sorbitol.

10. A toothpaste composition containing liposomal vitamin C and ascorbate palmitate according to any one of claims 1-3, characterized in that: The humectant is PEG-400.

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