CN109453365A - A kind of eye haustra -dsipelling active peptides - Google Patents
A kind of eye haustra -dsipelling active peptides Download PDFInfo
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/07—Tetrapeptides
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- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
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Abstract
The present invention discloses a kind of eye haustra -dsipelling active peptides, the polypeptide is wrapped in nano-encapsulated body with lipid components, nano-encapsulated body further includes polyalcohol, surfactant, pH buffer ingredient, the mass percentage concentration of eye haustra -dsipelling active peptides is 0.0001%-5%, the mass percentage concentration of lipid components is 2%-20%, the mass percentage concentration of polyalcohol is 2%-20%, and the mass percentage concentration of surfactant is 0.1%-10%, and the mass percentage concentration of pH buffer is 0.001%-1%.The stability of eye haustra -dsipelling active peptides of the present invention is good, highly-safe；It is easy to Transdermal absorption；Compared with before nano-encapsulated, the active peptides after nano-encapsulated are higher in the accumulation of skin, and same inventory can achieve superior eye haustra -dsipelling effect.
Description
Technical field
The invention belongs to skin care external drug fields, are related to a kind of eye haustra -dsipelling active peptides.
Background technique
Periocualr skin is very thin, it is easy to come to harm, be also easier to the various problems such as aging occur.Due to the growth at age
Or undesirable living habit, often stay up late, the elastin laminin and collagen of periocualr skin are gradually lost, skin elasticity drop
It is low, it relaxes, the fat in eye circumference fat pad removes, and is gathered in below eye, then will form eye pouch；Furthermore ocular blood follows
Obstacle occurs for ring, and capillary, vasculolymphatic permeability increase, and oedema occurs for connective tissue now, also will form eye pouch.
With the rapid development of society, people's lives pressure is increasing, and becoming for rejuvenation is gradually presented in eye pouch problem
Gesture seriously affects beauty, therefore eye pouch problem is gradually concerned by people, and occurs many skin cares for being used for eye in the market
Product.The active constituent added in the product of eye haustra -dsipelling at present mainly has plant extracts, active peptides class etc., wherein activity is more
Peptide is play in eye haustra -dsipelling product since small with molecular weight, mechanism is clear, good effect, produces the advantages such as controllable to pass
Important role.
However, the problem of often polypeptide moiety is added directly in prescription, thus brings in existing product is polypeptide
Stability is poor in the product, so that originally there is high-efficiency activated eye haustra -dsipelling polypeptide to be unable to give full play its due effect
Fruit, and the catabolite that polypeptide is degraded in the product and generated is possible to potentially hazardous to human body generation.Further, since skin
The presence of skin barrier limits the exchange of inside and outside substance, and the polypeptide in product can not be successfully to be absorbed through skin barrier,
Just it is difficult to the effect of giving full play to its eye haustra -dsipelling.In order to increase Transdermal absorption, gets a desired effect, increase is needed to feed intake
Amount, thus can bring the rising of cost.
In conclusion this field be badly in need of a kind of stability it is good, it is highly-safe, be easy to that Transdermal absorption, inventory are small, effect is excellent
It is different, it can make up for it the external preparation for skin skin-protection product or curable product of prior art defect.
Summary of the invention
Technical problem to be solved by the present invention lies in provide a kind of stability it is good, it is highly-safe, be easy to Transdermal absorption, throw
Doses is small, excellent effect eye haustra -dsipelling active peptides.
For this purpose, the eye haustra -dsipelling active peptides are to be wrapped in receive the present invention provides a kind of eye haustra -dsipelling active peptides
In rice inclusion enclave.
Eye haustra -dsipelling active peptides of the present invention are acetyl group tetrapeptide -5, palmityl tetrapeptide -7, dipeptides -2, palmityl three
Peptide -1, Matrixyl -4, each composition quality percentage concentration are 0.0001%-5%.
Package of the present invention is wrapped up with lipid components.
The lipid components are that soybean lecithin, egg yolk lecithin, phosphatidyl-ethanolamine, lysophosphatidyl choline, gallbladder are solid
Alcohol, lauric acid, myristic acid, palmitinic acid, stearic acid, isopropyl myristate, isopropyl palmitate, oleic acid, linoleic acid
The combination of one or more of ester, vitamin E, each composition quality percentage concentration are 2%-20%.
Nano-encapsulated body of the present invention further includes following component: polyalcohol, surfactant, pH buffer.
The polyalcohol is propylene glycol, glycerol, 1,2- hexylene glycol, the combination of one or more of 1,3-BDO, respectively
Composition quality percentage concentration is 2%-20%.
The surfactant is polysorbas20, polysorbate40, polysorbate60, Tween 80, poloxamer, Tai Luoshamu, each ingredient
Mass percentage concentration is 0.1%-10%.
The pH buffer is the combination of disodium hydrogen phosphate, sodium dihydrogen phosphate, potassium dihydrogen phosphate or dipotassium hydrogen phosphate, respectively at
Dividing mass percentage concentration is 0.001%-1%.
Eye haustra -dsipelling active peptides product form of the present invention include but is not limited to Essence, emulsion, creme, gel,
Dressing.
Eye haustra -dsipelling active peptides of the present invention are mainly the skin-protection product or curable product for preparing external preparation for skin.
The present invention is understood in order to be more advantageous to, and the mechanism of action of above-mentioned eye haustra -dsipelling active peptides is described as follows:
Acetyl group tetrapeptide -5 (Acetyl Tetrapeptide-5, No. CAS: 820959-17-9), one kind having antioedematous
Function and the strong active peptide for being widely used in eye haustra -dsipelling, mechanism of action are to improve by inhibiting angiotensin I converting enzyme
The microcirculation of eye skin, while increasing the activity of superoxide dismutase (Superoxide Dismutase, SOD), inhibit
It is glycosylated, and prevents protein-crosslinking, improves skin elasticity, can also reduce vasopermeability, moisture exudation is reduced, to water resistant
It is swollen, thus eye haustra -dsipelling and black eye.
Palmityl tetrapeptide -7 (Palmitoyl Tetrapeptide-7, No. CAS: 221227-05-0) is white thin by regulating and controlling
The secretion of born of the same parents' interleukin -6 (IL-6) substantially eliminates scytitis, increases skin elasticity, compact degree.In addition, palmityl tetrapeptide -7 is also
It can promote the discharge of skin excessive moisture, there is very strong draining effect, can be used for eliminating oedema, tighten eye flesh
Skin, additionally it is possible to circumference of eyes skin cell is activated, keeps eye circumference skin smoothly compact, it is more full of elasticity, so that eye haustra -dsipelling, desalinates black
Eyelet.
It is living to be able to suppress angiotensin converting enzyme (ACE) for dipeptides -2 (Dipeptide-2, No. CAS: 24587-37-9)
Property.ACE is a kind of exopeptidase, and can be catalyzed angiotensin I converting is Angiotensin II, bradykinin can also be made to inactivate, from
And lead to hypertension.Dipeptides -2 by inhibit ACE activity, anti-hypertension and improve blood circulation, promote ocular cell draining,
Ocular edema is eliminated, thus eye haustra -dsipelling.
Palmityl tripeptides -1 (Palmitoyl Tripeptide-1, Pal-GHK, No. CAS: 147732-56-7), in GHK
Peptide chain N-terminal modify and obtain through palmitinic acid, with better percutaneous abilities, skin can be promoted largely to synthesize collagen, more
Glycan, so that firm skin, can achieve the effect of eye haustra -dsipelling for eye circumference skin.
Matrixyl -4 (Palmitoyl Pentapeptide-4), can excite collagen, glycosaminoglycan
(GAGs) synthesis increases skin thickness, to effectively reverse aging, reduces wrinkle.It can achieve and dispel for eye circumference skin
The effect of eye pouch.
Acquired beneficial effect includes: the present invention compared with the existing technology
(1) nano-encapsulated is carried out to eye haustra -dsipelling active peptides, improves the stability and safety in utilization of polypeptide.
(2) polypeptide increases Transdermal absorption through nano-encapsulated.
(3) eye haustra -dsipelling active peptides are higher in the accumulation of skin after nano-encapsulated, and same inventory can achieve
Better eye haustra -dsipelling effect.
Detailed description of the invention
The transdermal amount of the cumulative in vitro of Fig. 1 polypeptide and accumulation skin hold-up (for 24 hours)
Specific embodiment
For a better understanding of the present invention, invention is described in detail below with reference to embodiment and attached drawing, but not only
It is limited to embodiment below.
Embodiment 1
Prescription
Preparation method:
1, soybean lecithin, cholesterol, propylene glycol, 1, the 2- hexylene glycol in A phase are taken in prescription ratio, in 40 DEG C of fire-bars
Stirring and dissolving under part, it is spare；
2, acetyl group tetrapeptide -5 in B phase, polysorbas20, disodium hydrogen phosphate, sodium dihydrogen phosphate are taken in prescription ratio, and temperature is added
Water (20 DEG C -35 DEG C), stirring and dissolving is spare；
3, A phase and B are mixed, by high speed shear under the conditions of 20000rpm pre-emulsification；
4, high-pressure homogeneous processing under the conditions of 22500psi by above-mentioned mixed liquor recycles 5 times, obtains dispelling for nano-encapsulated
Eye pouch active peptides.
5, the partial size of eye haustra -dsipelling active peptides nano-encapsulated body is detected, obtaining inclusion enclave partial size is 43.1nm.
Embodiment 2
Prescription
Preparation method:
1, soybean lecithin, cholesterol, propylene glycol, 1, the 2- hexylene glycol in A phase are taken in prescription ratio, in 40 DEG C of fire-bars
Stirring and dissolving under part, it is spare；
2, palmityl tetrapeptide -7, polysorbas20, disodium hydrogen phosphate, sodium dihydrogen phosphate in B phase are taken in prescription ratio, temperature is added
Water (20 DEG C -35 DEG C), stirring and dissolving is spare；
3, A phase and B are mixed, by high speed shear under the conditions of 20000rpm pre-emulsification；
4, high-pressure homogeneous processing under the conditions of 22500psi by above-mentioned mixed liquor recycles 5 times, obtains dispelling for nano-encapsulated
Eye pouch active peptides.
5, the partial size of eye haustra -dsipelling active peptides nano-encapsulated body is detected, obtaining inclusion enclave partial size is 47.6nm.
Embodiment 3
Prescription
Preparation method:
1, soybean lecithin, cholesterol, propylene glycol, 1, the 2- hexylene glycol in A phase are taken in prescription ratio, in 40 DEG C of fire-bars
Stirring and dissolving under part, it is spare；
2, dipeptides -2, polysorbas20, disodium hydrogen phosphate, sodium dihydrogen phosphate in B phase are taken in prescription ratio, warm water (20 is added
DEG C -35 DEG C), stirring and dissolving is spare；
3, A phase and B are mixed, by high speed shear under the conditions of 20000rpm pre-emulsification；
4, high-pressure homogeneous processing under the conditions of 22500psi by above-mentioned mixed liquor recycles 5 times, obtains dispelling for nano-encapsulated
Eye pouch active peptides.
5, the partial size of eye haustra -dsipelling active peptides nano-encapsulated body is detected, obtaining inclusion enclave partial size is 41.7nm.
Embodiment 4
Prescription
Preparation method:
1, soybean lecithin, cholesterol, propylene glycol, 1, the 2- hexylene glycol in A phase are taken in prescription ratio, in 40 DEG C of fire-bars
Stirring and dissolving under part, it is spare；
2, palmityl tripeptides -1 in B phase, polysorbas20, disodium hydrogen phosphate, sodium dihydrogen phosphate are taken in prescription ratio, and temperature is added
Water (20 DEG C -35 DEG C), stirring and dissolving is spare；
3, A phase and B are mixed, by high speed shear under the conditions of 20000rpm pre-emulsification；
4, high-pressure homogeneous processing under the conditions of 22500psi by above-mentioned mixed liquor recycles 5 times, obtains dispelling for nano-encapsulated
Eye pouch active peptides.
5, the partial size of eye haustra -dsipelling active peptides nano-encapsulated body is detected, obtaining inclusion enclave partial size is 44.8nm.
Embodiment 5
Prescription
Preparation method:
1, soybean lecithin, cholesterol, propylene glycol, 1, the 2- hexylene glycol in A phase are taken in prescription ratio, in 40 DEG C of fire-bars
Stirring and dissolving under part, it is spare；
2, Matrixyl -4, polysorbas20, disodium hydrogen phosphate, sodium dihydrogen phosphate in B phase are taken in prescription ratio, temperature is added
Water (20 DEG C -35 DEG C), stirring and dissolving is spare；
3, A phase and B are mixed, by high speed shear under the conditions of 20000rpm pre-emulsification；
4, high-pressure homogeneous processing under the conditions of 22500psi by above-mentioned mixed liquor recycles 5 times, obtains dispelling for nano-encapsulated
Eye pouch active peptides.
5, the partial size of eye haustra -dsipelling active peptides nano-encapsulated body is detected, obtaining inclusion enclave partial size is 49.2nm.
Embodiment 6
Prescription
Preparation method:
1, phosphatidyl-ethanolamine, isopropyl myristate, the oleic acid, propylene glycol, 1,3- fourth two in A phase are taken in prescription ratio
Alcohol, the stirring and dissolving under 40 DEG C of heating conditions are spare；
2, acetyl group tetrapeptide -5 in B phase, polysorbas20, disodium hydrogen phosphate, sodium dihydrogen phosphate are taken in prescription ratio, and temperature is added
Water (20 DEG C -35 DEG C), stirring and dissolving is spare；
3, A phase and B are mixed, by high speed shear under the conditions of 20000rpm pre-emulsification；
4, high-pressure homogeneous processing under the conditions of 22500psi by above-mentioned mixed liquor recycles 5 times, obtains dispelling for nano-encapsulated
Eye pouch active peptides.
5, the partial size of eye haustra -dsipelling active peptides nano-encapsulated body is detected, obtaining inclusion enclave partial size is 24.3nm.
Embodiment 7
Prescription
Preparation method:
1, phosphatidyl-ethanolamine, isopropyl myristate, the oleic acid, propylene glycol, 1,3- fourth two in A phase are taken in prescription ratio
Alcohol, the stirring and dissolving under 40 DEG C of heating conditions are spare；
2, palmityl tetrapeptide -7, polysorbas20, disodium hydrogen phosphate, sodium dihydrogen phosphate in B phase are taken in prescription ratio, temperature is added
Water (20 DEG C -35 DEG C), stirring and dissolving is spare；
3, A phase and B are mixed, by high speed shear under the conditions of 20000rpm pre-emulsification；
4, high-pressure homogeneous processing under the conditions of 22500psi by above-mentioned mixed liquor recycles 5 times, obtains dispelling for nano-encapsulated
Eye pouch active peptides.
5, the partial size of eye haustra -dsipelling active peptides nano-encapsulated body is detected, obtaining inclusion enclave partial size is 27.6nm.
Embodiment 8
Prescription
Preparation method:
1, phosphatidyl-ethanolamine, isopropyl myristate, the oleic acid, propylene glycol, 1,3- fourth two in A phase are taken in prescription ratio
Alcohol, the stirring and dissolving under 40 DEG C of heating conditions are spare；
2, dipeptides -2, polysorbas20, disodium hydrogen phosphate, sodium dihydrogen phosphate in B phase are taken in prescription ratio, warm water (20 is added
DEG C -35 DEG C), stirring and dissolving is spare；
3, A phase and B are mixed, by high speed shear under the conditions of 20000rpm pre-emulsification；
4, high-pressure homogeneous processing under the conditions of 22500psi by above-mentioned mixed liquor recycles 5 times, obtains dispelling for nano-encapsulated
Eye pouch active peptides.
5, the partial size of eye haustra -dsipelling active peptides nano-encapsulated body is detected, obtaining inclusion enclave partial size is 23.1nm.
Embodiment 9
Prescription
Preparation method:
1, phosphatidyl-ethanolamine, isopropyl myristate, the oleic acid, propylene glycol, 1,3- fourth two in A phase are taken in prescription ratio
Alcohol, the stirring and dissolving under 40 DEG C of heating conditions are spare；
2, palmityl tripeptides -1 in B phase, polysorbas20, disodium hydrogen phosphate, sodium dihydrogen phosphate are taken in prescription ratio, and temperature is added
Water (20 DEG C -35 DEG C), stirring and dissolving is spare；
3, A phase and B are mixed, by high speed shear under the conditions of 20000rpm pre-emulsification；
4, high-pressure homogeneous processing under the conditions of 22500psi by above-mentioned mixed liquor recycles 5 times, obtains dispelling for nano-encapsulated
Eye pouch active peptides.
5, the partial size of eye haustra -dsipelling active peptides nano-encapsulated body is detected, obtaining inclusion enclave partial size is 26.8nm.
Embodiment 10
Prescription
Preparation method:
1, phosphatidyl-ethanolamine, isopropyl myristate, the oleic acid, propylene glycol, 1,3- fourth two in A phase are taken in prescription ratio
Alcohol, the stirring and dissolving under 40 DEG C of heating conditions are spare；
2, Matrixyl -4, polysorbas20, disodium hydrogen phosphate, sodium dihydrogen phosphate in B phase are taken in prescription ratio, temperature is added
Water (20 DEG C -35 DEG C), stirring and dissolving is spare；
3, A phase and B are mixed, by high speed shear under the conditions of 20000rpm pre-emulsification；
4, high-pressure homogeneous processing under the conditions of 22500psi by above-mentioned mixed liquor recycles 5 times, obtains dispelling for nano-encapsulated
Eye pouch active peptides.
5, the partial size of eye haustra -dsipelling active peptides nano-encapsulated body is detected, obtaining inclusion enclave partial size is 28.4nm.
Embodiment 11
Prescription
Preparation method:
1, soybean lecithin, cholesterol, propylene glycol, 1, the 2- hexylene glycol in A phase are taken in prescription ratio, in 40 DEG C of fire-bars
Stirring and dissolving under part, it is spare；
2, acetyl group tetrapeptide -5 in B phase, polysorbas20, disodium hydrogen phosphate, sodium dihydrogen phosphate are taken in prescription ratio, and temperature is added
Water (20 DEG C -35 DEG C), stirring and dissolving is spare；
3, A phase and B are mixed, by high speed shear under the conditions of 20000rpm pre-emulsification；
4, high-pressure homogeneous processing under the conditions of 22500psi by above-mentioned mixed liquor recycles 5 times, obtains dispelling for nano-encapsulated
Eye pouch active peptides.
5, the partial size of eye haustra -dsipelling active peptides nano-encapsulated body is detected, obtaining inclusion enclave partial size is 45.7nm.
Comparative example 1
Prescription (1 kilogram of Essence)
Preparation method:
The Sodium Hyaluronate of formula ratio is added to the water, stirring makes to be uniformly mixed, and is then heated to 80~85 DEG C, heat preservation
Stirring makes it be uniformly dispersed.Temperature drops to 40 DEG C hereinafter, glycerol, Aloe Vera Gel, acetyl group tetrapeptide -5, Cer NP, Xin Gan is added
Pure and mild 1,2- hexylene glycol, stirs evenly.With the pH value of 15% triethanolamine tune solution to 5.5 or so.
Comparative example 2
According to the prescription and preparation method of comparative example 1, the Essence of blank is prepared.By embodiment 11 and blank
Essence is compounded according to mass ratio 1:1, is uniformly mixed, is obtained -5 essence of nano-encapsulated acetyl group tetrapeptide containing about 0.1%
Liquid.
The stability test of 12 eye haustra -dsipelling active peptides nano-encapsulated body of embodiment
The eye haustra -dsipelling active peptides nano-encapsulated body that embodiment 1-11 is obtained at room temperature, in closed container
It places 30 days, the character and partial size of test sample, experimental result are shown in Table 1.
The stability test result of 1 eye haustra -dsipelling active peptides nano-encapsulated body of table
By result in table 1 it is found that embodiment 1-11 eye haustra -dsipelling active peptides nano-encapsulated body does not go out after placing 30 days
Now to assemble, precipitates, lamination, significant changes also do not occur for partial size, and it is with good stability, it can be realized to active peptides
Nano-encapsulated.
The eye haustra -dsipelling active peptides of 13 nano-encapsulated of embodiment and its compounding stability test
13.1 instruments
Climatic chamber, high performance liquid chromatograph (HPLC)
13.2 test specimens
1 nano-encapsulated acetyl group tetrapeptide -5 of embodiment, common -5 Essence of acetyl group tetrapeptide of comparative example 1, comparison are real
Apply -5 Essence of 2 nano-encapsulated acetyl group tetrapeptide of example.
13.3 test basis
" Chinese Pharmacopoeia " four 9001 bulk pharmaceutical chemicals of general rule of version in 2015 and preparation stability test direction principle
13.4 experimental conditions and inspection project
Accelerated test: 40 DEG C ± 2 DEG C of climatic chamber, RH75% ± 5% passed through HPLC respectively at the 1st, 2,3,6 month
The content of polypeptide in each sample is detected, to evaluate its stability.
Long term test: 25 DEG C ± 2 DEG C of climatic chamber, RH60% ± 10%, respectively at the 3rd, 6,9,12,18,24,36
The moon detects the content of polypeptide in each sample by HPLC, to evaluate its stability.
13.5 stability test result
1 nano-encapsulated acetyl group tetrapeptide -5 of embodiment, common -5 Essence of acetyl group tetrapeptide of comparative example 1, comparison are real
Apply -5 Essence of 2 nano-encapsulated acetyl group tetrapeptide of example sample placed 6 months under the conditions of accelerated test after, stability data is shown in
The following table 2:
Table 2 accelerates 6 months stability test data
1 nano-encapsulated acetyl group tetrapeptide -5 of embodiment, common -5 Essence of acetyl group tetrapeptide of comparative example 1, comparison are real
Apply -5 Essence of 2 nano-encapsulated acetyl group tetrapeptide of example sample placed 6 months under the conditions of long term test after, stability data is shown in
The following table 3:
The long-term 6 months stability test data of table 3
By result in table 2 and table 3 it is found that 1 nano-encapsulated acetyl group tetrapeptide -5 of embodiment, 2 nano-encapsulated of comparative example
In accelerated test and after long term test 6 months, -5 content of acetyl group tetrapeptide in product does not go out -5 Essence of acetyl group tetrapeptide
, there is not water-oil separating phenomenon in existing significant changes, illustrate polypeptide after nano-encapsulated and by the polypeptide and base of nano-encapsulated
After matter compounding, good stability is all had.In contrast, common -5 Essence of acetyl group tetrapeptide of comparative example 1 is accelerating 6
A month and it is 6 months long-term under the conditions of, there is different degrees of decline in -5 content of acetyl group tetrapeptide in product, content of peptides
Reduce the decline for necessarily leading to its effect, in some instances it may even be possible to generate harmful catabolite, there is potential hazard to human body.Therefore,
Its stability and safety can be improved in active peptides after nano-encapsulated, can obtain in the case where identical inventory more excellent
Different eye haustra -dsipelling effect.
The transdermal amount of 14 cumulative in vitro of embodiment and accumulation skin hold-up test
14.1 instruments
Intellectual drug percutaneous dispersion test instrument, high performance liquid chromatograph (HPLC)
14.2 test specimens
1 nano-encapsulated acetyl group tetrapeptide -5 of embodiment, common -5 Essence of acetyl group tetrapeptide of comparative example 1, comparison are real
Apply -5 Essence of 2 nano-encapsulated acetyl group tetrapeptide of example.
14.3 test methods
Using the percutaneous abilities of rectilinear Franz diffusion cell method evaluation sample.The isolated skin of SD rat abdomen is fixed
Between diffusion cell receiving chamber and supply chamber, take 1g sample in the skin surface of supply chamber, effective diffusion area 3.14cm2, connect
Physiological saline is added in receives pond as receiving liquid, emptying bubble completely attaches to corium side and receiving liquid, 32 DEG C, 300r/min
Stirring diffusion.Respectively at 4h, 8h, 12h, 16h, 20h, receiving liquid 0.5mL is taken for 24 hours, and the reception of equivalent constant temperature blank is replenished in time
Liquid.Concentration through polypeptide in HPLC measurement receiving liquid, the polypeptide units area accumulation for calculating different time as follows are transdermal
Amount:
Wherein: QnTo accumulate transdermal amount；CnPeptide concentration in receiving liquid when for the sub-sampling；V is physiological saline in reception tank
Volume；CiPeptide concentration in receiving liquid when for the 1st time to previous sample；ViFor each sample volume；A is effective diffusion area.
After for 24 hours, skin is removed, ultrapure water shreds after washing away sample raffinate, addition ultrapure water homogenized, ultrasonic 5min,
10000r/min is centrifuged 10min, and supernatant is taken to detect through HPLC method, calculates polypeptide units areas of skin as follows and is detained
Amount:
Qs=Cs×V/A
Wherein, QsTo accumulate hold-up；CsPeptide masses concentration in the skin samples liquid measured for sampling time point；V is upper
Supernatant volume；A is effective diffusion area.
14.4 test results
1 nano-encapsulated acetyl group tetrapeptide -5 of embodiment, common -5 Essence of acetyl group tetrapeptide of comparative example 1, comparison are real
- 5 Essence of 2 nano-encapsulated acetyl group tetrapeptide of example is applied after percutaneous dispersion test for 24 hours, the cumulative in vitro of polypeptide is transdermal in sample
Amount and accumulation skin hold-up are as shown in Figure 1.
Fig. 1 the results show that 1 nano-encapsulated acetyl group tetrapeptide -5 of embodiment through the transdermal amount of accumulation for 24 hours be 69.36 μ g/
cm2, accumulation skin hold-up is 47.54 μ g/cm2, the accumulation of common -5 Essence of acetyl group tetrapeptide of comparative example 1 for 24 hours is transdermal
Amount is 38.43 μ g/cm2, accumulation skin hold-up is 11.70 μ g/cm2, -5 essence of 2 nano-encapsulated acetyl group tetrapeptide of comparative example
The transdermal amount of the accumulation of magnificent liquid is 69.12 μ g/cm2, accumulation skin hold-up is 47.28 μ g/cm2.It follows that polypeptide is in nanometer
Before package, due to the limitation of skin barrier, transdermal amount and skin hold-up are lower, and after nano-encapsulated, polypeptide
Transdermal amount and skin hold-up be significantly increased, especially skin hold-up improve it is more obvious, show polypeptide in nanometer packet
Transdermal absorption can be enhanced after wrapping up in, and accumulate in skin, more efficiently play its eye haustra -dsipelling effect in skin.
The polypeptide of nano-encapsulated has no effect on the Transdermal absorption of polypeptide and skin in product and is detained after compounding with matrix, still have biggish
Skin hold-up is accumulated, is conducive to enhance its eye haustra -dsipelling effect.
Embodiment 15 improves eye microcirculation
15.1 volunteer's situation
Between 25-40 years old, there are different degrees of eye pouch at 120 volunteers, age, are randomly divided into 4 groups, every group 30
People.
15.2 test specimens
1 nano-encapsulated acetyl group tetrapeptide -5 of embodiment, common -5 Essence of acetyl group tetrapeptide of comparative example 1, comparison are real
- 5 Essence of 2 nano-encapsulated acetyl group tetrapeptide of example is applied, using placebo as blank control.
15.3 test equipments
II type laser-Doppler perfusion weighted imaging instrument of PERIMED company, Sweden PeriScan PIM, the laser wave used
A length of 670nm.
15.4 test operations
Before test, keep room temperature at 25 DEG C ± 2 DEG C, volunteer lies low the 20min that reposes, and records periocualr skin blood flow, note
Start to test after the completion of record.Each group volunteer uses placebo, embodiment 1, comparative example 1, comparative example 2 to smear respectively
Eye pouch records the blood flow of 30min, 60min after each group administration respectively.
15.5 data are analyzed
The blood flow average value in periocualr skin unit area is analyzed, each time point blood flow variation is indicated with change rate, different
Time point administration group is analyzed compared between placebo with t inspection.
15.6 test results
The change rate that the blood flow of each group administration 30min, 60min are respectively relative to blood flow before it is tested is shown in Table 4.
4 each group periocualr skin blood flow change rate of table
Note: * indicates that administration group has statistical difference, p < 0.05 compared with placebo.* indicates administration group and placebo
Group compares significant difference, p < 0.01.
By result in table it is found that compared with placebo, acetyl group tetrapeptide -5 can improve eye circumference blood microcirculation, especially
Be improve after nano-encapsulated microcirculation effect it is more significant, and the polypeptide of nano-encapsulated is after being administered 60min,
Its effect for improving microcirculation does not weaken, and common -5 Essence of acetyl group tetrapeptide is after being administered 60min, when with 30min
It compares, the effect for improving microcirculation is decreased obviously.This shows polypeptide after nano-encapsulated, due to higher
Skin amount and skin hold-up, active peptides can form storage cavern, slow release, continuous action in skin, to have long-acting
Improvement blood microcirculation, to antioedematous, the effect of eye haustra -dsipelling.
16 periocualr skin flexibility test of embodiment
16.1 subjects
120 30-50 years old healthy womens, are randomly divided into 4 groups, average every group of 30 people.
16.2 test specimens
1 nano-encapsulated acetyl group tetrapeptide -5 of embodiment, common -5 Essence of acetyl group tetrapeptide of comparative example 1, comparison are real
- 5 Essence of 2 nano-encapsulated acetyl group tetrapeptide of example is applied, using placebo as blank control.
16.3 test equipments
The skin elasticity Cotometer MPA580 master of German Courage+Khazaka company (German CK company) manufacture
Machine, used probe are Reviscometer RV600 elastic fibrous tissue test probes.
16.4 test operations
Blank R2, R5, R7 value of 30min after first measurement periocular area is cleaned,
Wherein R2=Ua/Uf, R5=Ur/Ue, R7=Ur/Uf,
Ua: the recovery value of skin when from cancellation negative pressure to follow-on test skin surface repressurization next time；
Uf: skin maximum amount of tension when having negative pressure；
Ur: after cancelling negative pressure 0.1s, the recovery value and visco-elastic portions value or plastic value of skin；
Ue: after constant negative pressure is added on skin, the amount of tension of skin, positioning elastic part amount of tension when 0.1s；
Then sample is spread evenly across eye pouch position, twice a day, adhere to sooner or later using, must not use other makeup
Product are used continuously 4 weeks, skin R2, R5, R7 value after distinguishing test record test area before administration.The same subject's
Test is completed by the same survey crew.
16.5 test results
Improve effect of periocualr skin elasticity by comparing skin R2, R5, R7 value variation of administration front and back to assess product,
The variation of R2, R5, R7 value is as shown in table 5 below:
The situation of change of 5 each group of table administration front and back skin R2, R5, R7 value
Note: for R2, R5, R7 value closer to 1, skin elasticity is better.
From the data in the table, relative to placebo, after being used 4 weeks in the identical situation of activity component concentration, respectively
R2, R5, R7 value that test group measures significantly improve, wherein real using 1 nano-encapsulated acetyl group tetrapeptide -5 of embodiment and comparison
- 5 Essence of 2 nano-encapsulated acetyl group tetrapeptide of example is applied after 4 weeks, skin R2, R5, R7 value measured is than the common second of comparative example 1
The value that -5 Essence of acyl group tetrapeptide measures is higher, and the change rate of rear R2, R5, R7 value is bigger before testing, shows polypeptide through nanometer
Skin elasticity can be significantly improved after package, and there is better eye haustra -dsipelling effect.
17 eye haustra -dsipelling clinical test of embodiment
17.1 volunteer's situation
120 30-50 years old healthy volunteers have long-term eye pouch problem, are randomly divided into 4 groups, average every group of 30 people.
17.2 test specimens
1 nano-encapsulated acetyl group tetrapeptide -5 of embodiment, common -5 Essence of acetyl group tetrapeptide of comparative example 1, comparison are real
- 5 Essence of 2 nano-encapsulated acetyl group tetrapeptide of example is applied, using placebo as blank control.
17.3 test methods
Respectively using placebo, the sample of embodiment 1, comparative example 1, comparative example 2, smears twice, hold daily
It is 8 weeks continuous.
Before use, using be respectively adopted after 8 weeks Fringe Projection technology carry out eye pouch cubing, eye pouch
The 3D rendering in region is obtained by FaceScanner and Optocat software is used to handle.
17.4 curative effect determinate standards
Eye haustra -dsipelling effect assessment standard is as follows:
(1) effective: eye pouch volume is obviously reduced, and volume reduces more than 50% (containing)；
(2) effectively: eye pouch volume reduced for 25% (containing) -50%；
(3) invalid: the reduction of eye pouch volume is unobvious, does not reach above-mentioned requirements or does not reduce.
Total effective rate=(effective number of cases+effective number of cases)/total number of cases × 100%
17.5 test results
After being administered 8 weeks, compares the total effective rate situation of each group, the results are shown in Table 6.
Therapeutic evaluation situation after 6 each group volunteer medication of table 8 weeks
From the data in the table, the total effective rate of placebo is 3.33%, and the total effective rate of 1 administration group of embodiment is
70.00%, the total effective rate of 1 administration group of comparative example is 40.00%, and the total effective rate of 2 administration group of comparative example is
66.67%.The result shows that administration 8 weeks after, each administration group can effective eye haustra -dsipelling, relative to the common acetyl of comparative example 1
- 5 Essence of base tetrapeptide, active peptides are after nano-encapsulated, in the case where active peptides concentration is constant, can play more preferable
Eye haustra -dsipelling effect.
The above content is the further details of explanations for combining specific preferred embodiment to be the present invention, but not
Indicate that specific implementation of the invention is limited to these explanations.For those skilled in the art,
Under the premise of not departing from present inventive concept, several simple deductions or replacement can also be made, is regarded as belonging to of the invention
Protection scope.
Claims (10)
1. a kind of eye haustra -dsipelling active peptides, which is characterized in that the eye haustra -dsipelling active peptides are to be wrapped in nano-encapsulated body
In.
2. by eye haustra -dsipelling active peptides described in claim 1, which is characterized in that the eye haustra -dsipelling active peptides are acetyl group
Tetrapeptide -5, palmityl tetrapeptide -7, dipeptides -2, palmityl tripeptides -1, Matrixyl -4, each composition quality percentage concentration are
0.0001%-5%.
3. by eye haustra -dsipelling active peptides described in claim 1, which is characterized in that the package is wrapped with lipid components
It wraps up in.
4. by eye haustra -dsipelling active peptides described in claim 3, which is characterized in that the lipid components are soybean lecithin, egg
Yellow lecithin, phosphatidyl-ethanolamine, lysophosphatidyl choline, cholesterol, lauric acid, myristic acid, palmitinic acid, stearic acid, meat
The combination of one or more of isopropyl myristate, isopropyl palmitate, oleic acid, glyceryl linoleate, vitamin E, respectively at
Dividing mass percentage concentration is 2%-20%.
5. by eye haustra -dsipelling active peptides described in claim 1, which is characterized in that the nano-encapsulated body further include it is following at
Point: polyalcohol, surfactant, pH buffer.
6. by eye haustra -dsipelling active peptides described in claim 5, which is characterized in that the polyalcohol is propylene glycol, glycerol, 1,2-
Hexylene glycol, the combination of one or more of 1,3-BDO, each composition quality percentage concentration are 2%-20%.
7. by eye haustra -dsipelling active peptides described in claim 5, which is characterized in that the surfactant is polysorbas20, tween
40, polysorbate60, Tween 80, poloxamer, Tai Luoshamu, each composition quality percentage concentration are 0.1%-10%.
8. by eye haustra -dsipelling active peptides described in claim 5, which is characterized in that the pH buffer is disodium hydrogen phosphate, phosphorus
The combination of acid dihydride sodium, potassium dihydrogen phosphate or dipotassium hydrogen phosphate, each composition quality percentage concentration are 0.001%-1%.
9. by eye haustra -dsipelling active peptides described in claim 1-8 any claim, which is characterized in that the eye haustra -dsipelling is living
Property polypeptide products form includes but is not limited to Essence, emulsion, creme, gel, dressing.
10. by eye haustra -dsipelling active peptides described in claim 1-8 any claim, which is characterized in that the eye haustra -dsipelling
Active peptides are mainly the skin-protection product or curable product for preparing external preparation for skin.
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN112603862A (en) * | 2020-12-09 | 2021-04-06 | 珠海为你而美丽化妆品有限公司 | Composition for removing eye bags and eye mask containing composition |
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|---|---|---|---|---|
| WO2009095456A1 (en) * | 2008-01-30 | 2009-08-06 | Diverdrugs S.L. | Peptide derivatives useful in the treatment, care or cleansing of the skin, mucosae, scalp or nails |
| CN106726668A (en) * | 2016-11-19 | 2017-05-31 | 诺斯贝尔化妆品股份有限公司 | A kind of many peptidoliposome raw materials used in cosmetics |
| CN107260569A (en) * | 2017-05-25 | 2017-10-20 | 珀莱雅化妆品股份有限公司 | A kind of preparation method of eye-care compositions liposome |
| CN108338934A (en) * | 2017-01-23 | 2018-07-31 | 珠海联邦制药股份有限公司 | A kind of peptide composition and its application for eye-care |
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2019
- 2019-01-22 CN CN201910057497.3A patent/CN109453365A/en active Pending
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2009095456A1 (en) * | 2008-01-30 | 2009-08-06 | Diverdrugs S.L. | Peptide derivatives useful in the treatment, care or cleansing of the skin, mucosae, scalp or nails |
| CN106726668A (en) * | 2016-11-19 | 2017-05-31 | 诺斯贝尔化妆品股份有限公司 | A kind of many peptidoliposome raw materials used in cosmetics |
| CN108338934A (en) * | 2017-01-23 | 2018-07-31 | 珠海联邦制药股份有限公司 | A kind of peptide composition and its application for eye-care |
| CN107260569A (en) * | 2017-05-25 | 2017-10-20 | 珀莱雅化妆品股份有限公司 | A kind of preparation method of eye-care compositions liposome |
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| CN112603862A (en) * | 2020-12-09 | 2021-04-06 | 珠海为你而美丽化妆品有限公司 | Composition for removing eye bags and eye mask containing composition |
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