阅读说明：本技术 一种油包水体系祛皱多肽组合物 (Water-in-oil wrinkle-removing polypeptide composition ) 是由 丁文锋 彭晏 黄春青 于 2019-12-19 设计创作，主要内容包括：本发明公开一种油包水体系祛皱多肽组合物,属于美容多肽技术领域,所述祛皱多肽组合物包含具有类肉毒作用的多肽,所述具有类肉毒作用的多肽存在于水相当中,各多肽质量百分浓度为0.0001％-5％,所述水相与油相形成油包水体系。所述油相包含表面活性剂、油性润肤剂。与水基体系相比,本发明所述祛皱多肽组合物采用油包水体系,多肽成分溶于少量水相,使得油包水体系中局部多肽浓度更高,更易于透皮吸收,在皮肤的蓄积量更高,同样的投料量可以达到更优异的祛皱效果,而且稳定性好、安全性高、制备工艺简单、成本低廉、适于工业化大生产。(The invention discloses a water-in-oil system wrinkle-removing polypeptide composition, which belongs to the technical field of beauty polypeptide, and comprises polypeptides with a botulinus-like effect, wherein the polypeptides with the botulinus-like effect exist in a water phase, the mass percentage concentration of each polypeptide is 0.0001-5%, and the water phase and an oil phase form a water-in-oil system. The oil phase comprises a surfactant and an oily emollient. Compared with a water-based system, the wrinkle-removing polypeptide composition adopts a water-in-oil system, polypeptide components are dissolved in a small amount of water phase, so that the concentration of local polypeptide in the water-in-oil system is higher, the transdermal absorption is easier, the accumulation amount on skin is higher, the same feeding amount can achieve a more excellent wrinkle-removing effect, and the wrinkle-removing polypeptide composition is good in stability, high in safety, simple in preparation process, low in cost and suitable for industrial mass production.)

1. The water-in-oil system wrinkle-removing polypeptide composition is characterized by comprising a polypeptide with a botulinum-like effect, wherein the polypeptide is selected from one or more of the following polypeptides, including but not limited to acetyl hexapeptide-8, acetyl octapeptide-3, pentapeptide-18, pentapeptide-3, dipeptide diaminobutyryl benzylamide diacetate, β -alanyl hydroxy prolyl diaminobutyryl benzylamide and conopeptide, the polypeptide with the botulinum-like effect exists in an aqueous phase, the mass percent concentration of each polypeptide is 0.0001-5%, and the aqueous phase and an oil phase form a water-in-oil system.

2. The water-in-oil system wrinkle-removing polypeptide composition according to claim 1, wherein said oil phase comprises a surfactant, an oily emollient.

3. The water-in-oil system wrinkle-removing polypeptide composition as claimed in claim 2, wherein the surfactant is one or more of PEG-20 triisostearin, PEG-7 glyceryl cocoate, PEG-6 caprylic/capric glycerides, polyglycerol-2 isostearate and polyglycerol-4 laurate, and the mass percentage concentration of each component is 1-10%.

4. The water-in-oil system wrinkle-removing polypeptide composition according to claim 2, wherein said oily emollient is one or a combination of hydrogenated polyisobutene, caprylic/capric triglyceride, isononyl isononanoate, and the concentration of said oily emollient is 70% -90% by weight.

5. The water-in-oil system wrinkle-removing polypeptide composition according to claim 4, wherein said oily emollient further comprises vegetable oil, said vegetable oil being camellia oil, jojoba oil, nut oil, sunflower oil.

6. The water-in-oil wrinkle-removing polypeptide composition according to claim 1, wherein the water-in-oil wrinkle-removing polypeptide composition is mainly used for preparing skin care products or medical products for external application to the skin.

Technical Field

The invention belongs to the technical field of beauty polypeptide, and relates to a water-in-oil wrinkle-removing polypeptide composition.

Background

Wrinkles are the result of skin aging, which not only directly affects the normal structure and physiology of skin tissues, but also indirectly affects the stabilization of the internal and external environment of the body, resulting in various degrees of imbalance in metabolism, and even possibly promoting and accelerating aging and death of the body. The normal course of muscle contraction is: nerve impulse-acetylcholine (Ach) -endplate potential-muscle action potential-muscle contraction. Excessive muscle tension and contraction are one of the causes of wrinkle formation.

Botulinum toxin type A (Botox) causes muscle paralysis by specifically blocking the release of acetylcholine at the neuro-muscular junction. Research and development of small molecular polypeptide simulating the action of botulinum toxin A can achieve the effect of improving wrinkles. The wrinkle-removing polypeptide composition can achieve the effect of regulating muscle contraction by regulating the release of neurotransmitter, thereby removing wrinkles. These active polypeptides are water soluble, and thus the composition product is also water-based, with the polypeptide dissolved therein.

However, polypeptides are easily degraded in aqueous solution, and polypeptide components are directly added into water-based products, so that the stability of polypeptides in products is poor, the original wrinkle-removing polypeptides with high-efficiency activity cannot fully exert the due effect, and degradation products generated by degradation of polypeptides in products may possibly generate potential harm to human bodies. In addition, water-soluble substances are difficult to be absorbed through the skin barrier, and thus it is difficult to sufficiently exert their wrinkle-removing effects. In order to increase the transdermal absorption and achieve the desired effect, the amount of the feed needs to be increased, which leads to an increase in cost.

Therefore, a wrinkle-removing product which has good stability, high safety, easy transdermal absorption, low cost, simple preparation process, suitability for industrial mass production, excellent effect and capability of overcoming the defects of the prior art is urgently needed in the field.

Disclosure of Invention

The technical problem to be solved by the invention is to provide the wrinkle-removing polypeptide composition which has the advantages of good stability, high safety, easy transdermal absorption, low cost, simple preparation process, suitability for industrial mass production and excellent effect.

Through experimental research, the inventor finds that polypeptide components are dispersed in an oil phase to form a water-in-oil system, a small amount of water phase in the system can reduce the contact of the polypeptide and water, so that the polypeptide is concentrated in the water phase, the stability of the polypeptide is improved, and the polypeptide with a larger local concentration is favorable for exerting a better wrinkle removing effect; the external oil phase can enable the polypeptide components to better penetrate through skin barriers and promote absorption, thereby endowing the product with more excellent wrinkle-removing effect, and forming the invention.

The invention provides a water-in-oil system wrinkle-removing polypeptide composition, which comprises a polypeptide with a botulinum-like effect, wherein the polypeptide is selected from one or more of the following polypeptides, including but not limited to acetyl hexapeptide-8, acetyl octapeptide-3, pentapeptide-18, pentapeptide-3, dipeptide diaminobutyryl benzylamide diacetate, β -alanyl hydroxy prolyl diaminobutyryl benzylamide and conopeptide, the polypeptide with the botulinum-like effect exists in an aqueous phase, the mass percent concentration of each polypeptide is 0.0001-5%, and the aqueous phase and an oil phase form a water-in-oil system.

The oil phase comprises a surfactant and an oily emollient.

The surfactant is one or a combination of more of PEG-20 triisostearin, PEG-7 glyceryl cocoate, PEG-6 caprylic/capric glycerides, polyglycerol-2 isostearate and polyglycerol-4 laurate, and the mass percentage concentration of each component is 1-10%.

The oily emollient is one or a combination of hydrogenated polyisobutene, caprylic/capric triglyceride and isononyl isononanoate, and the mass percentage concentration of the oily emollient is 70-90%.

The oily emollient may also comprise vegetable oil, which is camellia seed oil, jojoba seed oil, nut oil, sunflower seed oil.

The water-in-oil wrinkle-removing polypeptide composition is mainly used for preparing skin care products or medical products for external application of skin.

To further facilitate understanding of the present invention, the mechanism of wrinkle formation and removal, and the mechanism of action of the wrinkle-removing polypeptide described above, are illustrated as follows:

1. wrinkle formation and wrinkle removal mechanism

Excessive muscle tension and contraction are one of the causes of wrinkle formation. Wrinkle generation can be reduced by regulating muscle contraction. Muscle contraction is caused by the release of the neurotransmitter acetylcholine in the pre-synaptic membrane vesicles of the nerve-muscle junction, acting on the post-synaptic membrane. Vesicles need to fuse with presynaptic membranes before the exocytosis process can be completed. Membrane fusion is mediated by the SNARE complex, which is a ternary complex formed by synaptic Vesicle Associated Membrane Protein (VAMP), Syntaxin (Syntaxin) and synaptosome associated protein 25(SNAP-25), wherein VAMP is located on the vesicle membrane and Syntaxin and SNAP-25 are located on the presynaptic membrane. Through specific recognition and interaction between the two, the vesicle and the presynaptic membrane are promoted to fuse, acetylcholine is released, and muscle contraction is caused. The formation of ternary complexes of VAMP, Syntaxin and SNAP-25 depends on the calcium ion inflow in synaptic cleft, and the calcium ion entering into presynaptic membrane can start the formation process of the ternary complex, promote the fusion of vesicle and presynaptic membrane, and release acetylcholine. After acetylcholine is released, it needs to bind to the muscle-type nicotinic acetylcholine receptor (m-nAChR) of the postsynaptic membrane, and sodium ions flow in to generate action potential, so that muscle contraction can finally occur.

Therefore, starting from the mechanism of muscle contraction, calcium ion influx in synaptic gaps is inhibited by interfering the formation of SNARE ternary complex, the muscle-type nicotinic acetylcholine receptor (m-nAChR) of postsynaptic membrane is competitively antagonized, and sodium ion influx is prevented, so that nerve signal conduction can be blocked, muscle contraction is inhibited, and wrinkles are lightened.

2. Mechanism of action of wrinkle-removing polypeptide

Acetyl Hexapeptide-8 (Acetyl Hexapeptide-8, CAS number: 616204-22-9) is a neurotransmitter inhibitory polypeptide, participates in competing for SyNaptosomal Associated Protein 25(SNAP-25) at the binding site of the vesicle, thereby influencing the formation of ternary complex, enabling the vesicle not to effectively release neurotransmitter acetylcholine, further weakening muscle contraction, preventing the formation of wrinkles, and remarkably removing dynamic lines such as crow's feet, raised head lines, and slubby lines.

Acetyl Octapeptide-3 (Acetyl Octapeptide-3, CAS number: 868844-74-0), which is designed by simulating the N-terminal sequence of the peptide chain of SNAP-25, is an extended analogue of Acetyl hexapeptide-8, and is combined with the relevant sites of the vesicle to prevent the combination of SNAP-25 and the sites, further influence the formation of ternary complex, interfere the release of acetylcholine, block nerve signal conduction, weaken muscle contraction and play a role in removing wrinkles.

Pentapeptide-18 (Pentapeptide-18, CAS number: 64963-01-5), a modified enkephalin, can bind to enkephalin receptors outside nerve cells, and regulates calcium ion channels through G protein, so that the calcium ion channels are closed, and vesicles cannot be fused with presynaptic membranes, thereby inhibiting the release of neurotransmitter acetylcholine, inhibiting muscle contraction and preventing fine lines and wrinkles from generating.

Pentapeptide-3 (Pentapeptide-3, CAS number: 135679-88-8), has botulinum-like effects, and can exert anti-wrinkle and skin-smoothing effects.

Dipeptide diaminobutyrylbenzylamide diacetate (CAS number: 823202-99-9) has a botulinum-like effect, acts on a postsynaptic membrane, is a muscle-type nicotinic acetylcholine receptor (m-nAChR) antagonist, and reversibly binds to a muscle-type nicotinic acetylcholine receptor (m-nAChR) to block the binding of acetylcholine to the receptor, so that the receptor is blocked.

β -alanyl hydroxy prolyl diamino butyryl benzyl amide (Beta-alanyl hydroxy propyl diamino butyryl benzyl amide), a novel polypeptide raw material developed by the inventor independently, a botulism, is a muscle type nicotinic acetylcholine receptor (m-nAChR) antagonist, and blocks the combination of neurotransmitter acetylcholine and the receptor through the firm combination of the m-nAChR, so that excitation transmission is weakened, muscles are relaxed, and the obvious wrinkle removing effect is achieved.

Conotoxin (Conopeptide) simulates natural mu-conotoxin, is composed of 22 amino acids, has a mu-conotoxin disulfide bond framework, has three pairs of disulfide bond linkage modes in a molecule of C3-C15, C4-C21 and C10-C22, and has strong penetration capability through high folding of the structure. After the action signal reaches the motor nerve ending, through a series of physiological activities, the presynaptic membrane releases acetylcholine, the acetylcholine is combined with the receptor m-nAChR of the postsynaptic membrane, sodium ions flow in, so that action potential is generated, and the muscle contracts. The conopeptide can specifically block a voltage-gated sodium ion channel, so that the sodium ion inflow is blocked, a muscle action potential cannot be formed, and expression muscles are relaxed, thereby effectively preventing and reducing wrinkles. Is known as the botulinum toxin which can be smeared and can quickly remove wrinkles in time.

The invention starts from the mechanisms of wrinkle formation and wrinkle removal, utilizes different action targets of the polypeptide, and obtains the water-in-oil system wrinkle removal polypeptide composition by dispersing the polypeptide in an oil phase system. Compared with the prior art, the invention has the advantages that:

(1) the polypeptide is dissolved in a small amount of water phase and dispersed in the oil phase to form a water-in-oil system, so that the stability and the use safety of the polypeptide are improved.

(2) The polypeptide is concentrated in the water phase, so that the concentration of local active ingredients is increased, and the excellent wrinkle removing effect is favorably achieved.

(3) The oil phase in the system can promote the transdermal absorption of the water-soluble polypeptide, and the same dosage can achieve better wrinkle-removing effect.

(4) The invention can achieve better wrinkle-removing effect with lower cost, and the preparation process is simple and suitable for industrial mass production.

Drawings

FIG. 1 microscopic image (40X 10 times) of water-in-oil system of polypeptide composition

FIG. 2 in vitro cumulative transdermal and cumulative skin Retention of the polypeptide (24h)

Detailed Description

For a better understanding of the present invention, the following detailed description is given in conjunction with the following examples and drawings, but is not limited to the following examples.