CN104523442A - Phenylethyl resorcinol lipid nanoparticle as well as preparation method and use thereof - Google Patents

Phenylethyl resorcinol lipid nanoparticle as well as preparation method and use thereof Download PDF

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CN104523442A
CN104523442A CN201410777603.2A CN201410777603A CN104523442A CN 104523442 A CN104523442 A CN 104523442A CN 201410777603 A CN201410777603 A CN 201410777603A CN 104523442 A CN104523442 A CN 104523442A
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symwhite
lipid nanoparticle
peg
lipid
phenylethyl resorcinol
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CN104523442B (en
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夏强
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SUZHOU NANOHEALTH BIOTECH CO Ltd
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SUZHOU NANOHEALTH BIOTECH CO Ltd
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Abstract

The invention provides a phenylethyl resorcinol lipid nanoparticle as well as a preparation method and use thereof. The phenylethyl resorcinol lipid nanoparticle is composed of an active component phenylethyl resorcinol, lipid, an emulsifier, a co-emulsifier and a stabilizer; the phenylethyl resorcinol lipid nanoparticle is faint yellow and semi-transparent and has high light stability; the phenylethyl resorcinol lipid nanoparticle is transparent and blueing after being dispersed by hot water; the colour of the phenylethyl resorcinol lipid nanoparticle still cannot be changed after being illuminated for a month; the phenylethyl resorcinol lipid nanoparticle can be freely matched with cosmetic formulae; the preparation method of the phenylethyl resorcinol lipid nanoparticle is simple, controllable and good in repeatability; and in addition, after being applied to cosmetic formulae, the phenylethyl resorcinol lipid nanoparticle has the effects of whitening skin, improving skin touch and moisturizing.

Description

Symwhite-337 lipid nanoparticle and its production and use
Technical field
The present invention relates to the technical field of the carrier system in cosmetics technology of preparing, more specifically relate to Symwhite-337 lipid nanoparticle and its production and use.
Background technology
Symwhite-337 is 4-(1-phenethyl)-1,3-resorcinol by name entirely, and be white crystalline solid, molecular formula is C 14h 14o 2, molecular weight: 214.27g/mol, fusing point: 78-82 DEG C.Symwhite-337 has excellent skin whitening effects, and its Main Function suppresses rate-limiting enzyme tryrosinase, and being has one of tyrosinase inhibitor that the activity of report is the highest.In the melanocytic analysis design mothod of B16V, Symwhite-337 is the most effective in check melanin synthesis in all test compounds, its IC 50value (50% inhibition concentration) is 2uM; Confirm in the MTT test that B16V cell carries out, the white-skinned face function of Symwhite-337 does not come from cytotoxicity; In the 3D epidermis model of dyeing, the Symwhite-337 of 0.1% almost completely inhibit melanic synthesis after the cultivation of 14 days; The in vivo test carried out in the tested crowd in Asia proves, Symwhite-337 can whitening effect human body skin under the consumption level of 0.5%.It is crucial that whitening speed is fast, begs for consumer and likes, gradually obtain the license of every country at present, progressively in cosmetics.It can improve colour of skin inequality, reduces the dye that ultraviolet radiation skin causes, and is a outstanding antioxidant simultaneously and has wrinkling resistance.Two benzene ring structures of Symwhite-337 uniqueness are more conducive to the affinity to skin, and suitable molecular size makes it to be absorbed by the skin utilization rapidly simultaneously, and this makes Symwhite-337 have the incomparable advantage of other whitening compounds and market potential.
But Symwhite-337 also exists following problem in the application: 1. the dissolubility of Symwhite-337 in water is lower, and when using in cosmetic formulations, its content is too low, is difficult to play white-skinned face function; 2. Symwhite-337 has photo-labile, ecru can be gradually become from white rapidly under illumination condition, finally become pink, cause Symwhite-337 content to decline rapidly, affect the outward appearance of cosmetics and the bioavailability of Symwhite-337.
The a lot of novel feature of nano medicament carrying system is that cosmetic industry provides much new opportunity to develop.Carrier technique can improve the dissolubility of active substance in water and stability, improve load capacity and the bioavailability of active substance, increase targeting and controlled-release function, improve biological oxidation resistance and mutation ability, and its compatibility in formula can be improved, cosmetics skinfeel can also be made to improve, moisture of skin can be prevented simultaneously to a certain extent to scatter and disappear, play moisture-keeping function.Symwhite-337 some shortcomings in application process can be weakened by nano-carrier technology, thus make it move towards commercialization process better.
Because Symwhite-337 is not soluble in water, there is auroral poles unstability simultaneously, use nano medicament carrying system to wrap up composite whitening agent, can be good at overcoming the above problems, skinfeel can also be improved and increase moistening effect.The present invention comes therefrom.
Summary of the invention
For solving the problems of the technologies described above, the invention provides a kind of Symwhite-337 lipid nanoparticle and its production and use, its objective is and produce a kind of Symwhite-337 emulsion be applied in cosmetics, solve under light conditions, the Symwhite-337 poor stability in cosmetics and the problem how effectively to be absorbed by skin.
For achieving the above object, technical scheme of the present invention is as follows:
A kind of Symwhite-337 lipid nanoparticle, comprise active component Symwhite-337, lipid, emulsifying agent, co-emulsifier and stabilizing agent, wherein each constituent mass percentage ratio is as follows:
All the other are water;
Wherein the mean diameter of Symwhite-337 lipid nanoparticle is 50-400nm.
Wherein, described lipid is selected from the mixing of the compound of following at least two kinds: caprylic/capric triglyceride, glyceryl monostearate, molecule distillating monoglyceride, acetylation monoglyceride, Vitamin E acetate, butyl capryl alcohol salicylate, glycerin polyether-26.
Wherein, described emulsifying agent is selected from the mixing of following at least three kinds of compounds: PEG-8 caprylic/capric glyceride type, the smooth olive oil acid esters of Pyrusussuriensis, laureth-23, PEG-40 stearate, stereth-21, the mixture of palmityl alcohol and PEG-75 stearate and glyceryl stearate and stereth-20, Polyoxyethylene Sorbitan Monooleate, the mixture of tristerin and PEG-75 stearate, Coco-Glucoside/cocoanut oil alcohol, poloxamer188, PEG-30 dimerization hydroxy stearic acid ester, C14-22 alcohol and C12-20 alkyl-glucoside, ceteth-25.
Wherein, described co-emulsifier is selected from the compound of following at least one: ethoxydiglycol, PEG-4000, stereth-2,1,3 butylene glycol, ceteth-6.
Wherein, described stabilizing agent is selected from the compound of following at least one: 1,3 butylene glycol, butylated hydroxytoluene, the smooth cetylate of Pyrusussuriensis, the smooth olive oil acid esters of Pyrusussuriensis, Aden's perfume base malonic acid ethylhexyl and caprylic/capric triglyceride, EDETATE SODIUM.
A preparation method for Symwhite-337 lipid nanoparticle, comprises the following steps,
Step (1): using lipid, emulsifying agent, co-emulsifier and stabilizing agent as oil phase, under 50 ~ 80 DEG C of conditions, mix homogeneously forms mixed solution;
Step (2): add Symwhite-337 to the mixed liquor in step (1) and stir, mixing speed is 300 ~ 600rpm, and mixing time is 2 ~ 10min, dissolves completely to Symwhite-337;
Step (3): the aqueous phase adding same tepidarium in the mixed solution of step (2), stir about 5-10min, mixing speed is 300 ~ 600rpm, and cooling obtains faint yellow or white semi-transparent Symwhite-337 lipid nanoparticle.
A purposes for Symwhite-337 lipid nanoparticle, described Symwhite-337 lipid nanoparticle is applied in cosmetic formulations.
Pass through technique scheme, a kind of Symwhite-337 lipid nanoparticle provided by the invention and its production and use, its beneficial effect is, Symwhite-337 lipid nanoparticle stability is high, transparent blueing after hot water dispersion, an illumination still invariant color in month, improves the light stability of Symwhite-337 greatly, in addition can interworking any with cosmetic formulations, compatibility is good; Symwhite-337 lipid nanoparticle preparation method is simply controlled, reproducible; Symwhite-337 lipid nanoparticle is applied in cosmetic formulations can bring good whitening effect, can also improve skinfeel and increase moistening effect.
Detailed description of the invention
Be clearly and completely described to the technical scheme in the embodiment of the present invention below.
Embodiment 1
Take 12g caprylic/capric triglyceride, 5g acetylation monoglyceride, 3g butyl capryl alcohol salicylate, 5g laureth-23, 10g stereth-21, 5gPEG-30 dimerization hydroxy stearic acid ester, 5gPEG-40 stearate, 1g stereth-2, 3g1, 3-butanediol, 1g Aden perfume base malonic acid ethylhexyl and caprylic/capric triglyceride, 0.1gEDTA disodium, stir under 65 DEG C of conditions and form clear solution, add 4g Symwhite-337, mixing speed is 300rpm, mixing time is 6min, add the deionized water of 45.9g with tepidarium, 300rpm/min stirs 8min, rear cooling obtains faint yellow semi-transparent Symwhite-337 lipid nanoparticle solid, this Symwhite-337 lipid nanoparticle solid measures its particle diameter through laser particle analyzer and is about 334nm.
Embodiment 2
Take 5g glyceryl monostearate, 10g butyl capryl alcohol salicylate, 5g caprylic/capric triglyceride, the smooth olive oil acid esters of 5g Pyrusussuriensis, 5g Polyoxyethylene Sorbitan Monooleate, 5gPEG-30 dimerization hydroxy stearic acid ester, 3gC14-22 alcohol and C12-20 alkyl-glucoside, 5g laureth-23, 5gPEG-40 stearate, 4g ethoxydiglycol, 3g1, 3-butanediol, 1g hydroxy-methylbenzene, 0.1gEDTA disodium, stir under 70 DEG C of conditions and form clear solution, add 3g Symwhite-337, mixing speed is 400rpm, mixing time is 6min, add the deionized water of 40.9g with tepidarium, 300rpm/min stirs 8min, rear cooling obtains faint yellow semi-transparent Symwhite-337 lipid nanoparticle solid, this Symwhite-337 lipid nanoparticle solid measures its particle diameter through laser particle analyzer and is about 225nm.
Embodiment 3
Take 12.5g caprylic/capric triglyceride, 2.5g glyceryl monostearate, 3g acetylation monoglyceride, 5g Vitamin E acetate, 8g stereth-21, 5gPEG-30 dimerization hydroxy stearic acid ester, the smooth olive oil acid esters of 2g Pyrusussuriensis, 3g Polyoxyethylene Sorbitan Monooleate, 3g ceteth-25, 4g PEG-8 caprylic/capric glyceride type, 5g PEG-40 stearate, 3g Coco-Glucoside/cocoanut oil alcohol, 3g1, 3-butanediol, 2g ceteth-6, 2g stereth-2, 1g tetrahydrocurcumin, stir under 75 DEG C of conditions and form clear solution, add 5g Symwhite-337, mixing speed is 350rpm, mixing time is 5min, add the deionized water of 31g with tepidarium, 350rpm/min stirs 7min, rear cooling obtains faint yellow semi-transparent Symwhite-337 lipid nanoparticle solid, this Symwhite-337 lipid nanoparticle solid measures its particle diameter through laser particle analyzer and is about 65nm.
A kind of Symwhite-337 lipid nanoparticle provided by the invention and its production and use, its beneficial effect is, Symwhite-337 lipid nanoparticle stability is high, transparent blueing after hot water dispersion, an illumination still invariant color in month, greatly improve the light stability of Symwhite-337, in addition can interworking any with cosmetic formulations, compatibility is good; Symwhite-337 lipid nanoparticle preparation method is simply controlled, reproducible; Symwhite-337 lipid nanoparticle is applied in cosmetic formulations can bring good whitening effect, can also improve skinfeel and increase moistening effect.
The above-mentioned explanation of disclosed embodiment of this invention, enables professional and technical personnel in the field realize or uses the present invention.To be apparent for those skilled in the art to the multiple amendment of these embodiments, General Principle as defined herein can without departing from the spirit or scope of the present invention, realize in other embodiments.Therefore, the present invention can not be restricted to these embodiments shown in this article, but will meet the widest scope consistent with principle disclosed herein and features of novelty.

Claims (7)

1. a Symwhite-337 lipid nanoparticle, is characterized in that, comprises active component Symwhite-337, lipid, emulsifying agent, co-emulsifier and stabilizing agent, and wherein each constituent mass percentage ratio is as follows:
Wherein the mean diameter of Symwhite-337 lipid nanoparticle is 50-400nm.
2. a kind of Symwhite-337 lipid nanoparticle according to claim 1; it is characterized in that, described lipid is selected from the mixing of the compound of following at least two kinds: caprylic/capric triglyceride, glyceryl monostearate, molecule distillating monoglyceride, acetylation monoglyceride, Vitamin E acetate, butyl capryl alcohol salicylate, glycerin polyether-26.
3. a kind of Symwhite-337 lipid nanoparticle according to claim 1, it is characterized in that, described emulsifying agent is selected from the mixing of following at least three kinds of compounds: PEG-8 caprylic/capric glyceride type, the smooth olive oil acid esters of Pyrusussuriensis, laureth-23, PEG-40 stearate, stereth-21, the mixture of palmityl alcohol and PEG-75 stearate and glyceryl stearate and stereth-20, Polyoxyethylene Sorbitan Monooleate, the mixture of tristerin and PEG-75 stearate, Coco-Glucoside/cocoanut oil alcohol, poloxamer188, PEG-30 dimerization hydroxy stearic acid ester, C14-22 alcohol and C12-20 alkyl-glucoside, ceteth-25.
4. a kind of Symwhite-337 lipid nanoparticle according to claim 1, it is characterized in that, described co-emulsifier is selected from the compound of following at least one: ethoxydiglycol, PEG-4000, stereth-2,1,3 butylene glycol, ceteth-6.
5. a kind of Symwhite-337 lipid nanoparticle according to claim 1, it is characterized in that, described stabilizing agent is selected from the compound of following at least one: 1,3-butanediol, butylated hydroxytoluene, the smooth cetylate of Pyrusussuriensis, the smooth olive oil acid esters of Pyrusussuriensis, Aden's perfume base malonic acid ethylhexyl and caprylic/capric triglyceride, EDETATE SODIUM.
6., based on the preparation method of a kind of Symwhite-337 lipid nanoparticle according to claim 1, it is characterized in that, comprise the following steps,
Step (1): using lipid, emulsifying agent, co-emulsifier and stabilizing agent as oil phase, under 50 ~ 80 DEG C of conditions, mix homogeneously forms mixed solution;
Step (2): add Symwhite-337 to the mixed liquor in step (1) and stir, mixing speed is 300 ~ 600rpm, and mixing time is 2 ~ 10min, dissolves completely to Symwhite-337;
Step (3): the aqueous phase adding same tepidarium in the mixed solution of step (2), stir about 5-10min, mixing speed is 300 ~ 600rpm, and cooling obtains faint yellow or white semi-transparent Symwhite-337 lipid nanoparticle.
7. based on the purposes of a kind of Symwhite-337 lipid nanoparticle according to claim 1, it is characterized in that: described Symwhite-337 lipid nanoparticle is applied in cosmetic formulations.
CN201410777603.2A 2014-12-15 2014-12-15 Symwhite-337 lipid nano particle and its production and use Active CN104523442B (en)

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Cited By (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105342866A (en) * 2015-10-21 2016-02-24 苏州纳康生物科技有限公司 Green tea extract nanostructured lipid carrier and preparation method thereof
CN105616176A (en) * 2016-03-21 2016-06-01 东南大学 Phenylethyl resorcinol high-loading lipid nanocapsule and preparation method thereof
CN106580755A (en) * 2017-03-02 2017-04-26 武汉百思凯瑞纳米科技有限公司 Nanometer composition containing skin-moistening and whitening components, and preparation method and application thereof
CN108210360A (en) * 2018-02-06 2018-06-29 德之馨(上海)有限公司 A kind of water solubility whitening formula and its preparation method and application
CN108743430A (en) * 2018-06-28 2018-11-06 武汉百思凯瑞生物科技有限公司 A kind of total conveying nano-composition of Symwhite-337 and its preparation method and application
CN110420125A (en) * 2019-08-26 2019-11-08 屈威翰 A kind of compound resorcinol liposome and preparation method thereof
CN111588643A (en) * 2019-02-21 2020-08-28 苏州纳康生物科技有限公司 Active matter carrier of microcapsule embedding lipid nanoparticles and preparation method thereof
CN114099403A (en) * 2021-11-19 2022-03-01 广东轻工职业技术学院 Skin-feel-improving nanostructured lipid carrier and preparation process and application thereof
WO2023221665A1 (en) * 2022-05-17 2023-11-23 帕潘纳(北京)科技有限公司 Diphenolic compound, and preparation method therefor and use thereof

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CN103860389A (en) * 2012-12-17 2014-06-18 贝侬生化(苏州工业园区)有限公司 Nanostructured lipid carrier loaded with phenylethyl resorcinol, preparation method thereof and cosmetic containing same
CN104027262A (en) * 2013-03-05 2014-09-10 上海复旦张江生物医药股份有限公司 Phenethyl resorcinol nanostructured lipid carrier and preparation method thereof
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Cited By (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105342866A (en) * 2015-10-21 2016-02-24 苏州纳康生物科技有限公司 Green tea extract nanostructured lipid carrier and preparation method thereof
CN105616176A (en) * 2016-03-21 2016-06-01 东南大学 Phenylethyl resorcinol high-loading lipid nanocapsule and preparation method thereof
CN106580755A (en) * 2017-03-02 2017-04-26 武汉百思凯瑞纳米科技有限公司 Nanometer composition containing skin-moistening and whitening components, and preparation method and application thereof
CN108210360A (en) * 2018-02-06 2018-06-29 德之馨(上海)有限公司 A kind of water solubility whitening formula and its preparation method and application
CN108210360B (en) * 2018-02-06 2021-02-12 德之馨(上海)有限公司 Water-soluble whitening formula and preparation method and application thereof
CN108743430A (en) * 2018-06-28 2018-11-06 武汉百思凯瑞生物科技有限公司 A kind of total conveying nano-composition of Symwhite-337 and its preparation method and application
CN111588643A (en) * 2019-02-21 2020-08-28 苏州纳康生物科技有限公司 Active matter carrier of microcapsule embedding lipid nanoparticles and preparation method thereof
CN110420125A (en) * 2019-08-26 2019-11-08 屈威翰 A kind of compound resorcinol liposome and preparation method thereof
CN114099403A (en) * 2021-11-19 2022-03-01 广东轻工职业技术学院 Skin-feel-improving nanostructured lipid carrier and preparation process and application thereof
WO2023221665A1 (en) * 2022-05-17 2023-11-23 帕潘纳(北京)科技有限公司 Diphenolic compound, and preparation method therefor and use thereof

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