CN105534724A - Resveratrol-coated nano solid lipid carrier and preparation method thereof - Google Patents

Resveratrol-coated nano solid lipid carrier and preparation method thereof Download PDF

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CN105534724A
CN105534724A CN201610034448.4A CN201610034448A CN105534724A CN 105534724 A CN105534724 A CN 105534724A CN 201610034448 A CN201610034448 A CN 201610034448A CN 105534724 A CN105534724 A CN 105534724A
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resveratrol
solid lipid
oil
peg
ester
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张婉萍
梁小智
秦钰波
朱海洋
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Shanghai Institute of Technology
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/02Cosmetics or similar toiletry preparations characterised by special physical form
    • A61K8/14Liposomes; Vesicles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/34Alcohols
    • A61K8/347Phenols
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/55Phosphorus compounds
    • A61K8/553Phospholipids, e.g. lecithin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/92Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/92Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof
    • A61K8/922Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof of vegetable origin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • A61Q19/02Preparations for care of the skin for chemically bleaching or whitening the skin

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
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  • Chemical & Material Sciences (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Emergency Medicine (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Dermatology (AREA)
  • Cosmetics (AREA)
  • Medicinal Preparation (AREA)

Abstract

The invention discloses a resveratrol-coated nano solid lipid carrier and a preparation method thereof. The resveratrol-coated nano solid lipid carrier comprises the following components in percentage by weight: 0.1 to 15 percent of resveratrol, 0.5 to 5 percent of phospholipid, 3 to 30 percent of a solid emulsifier, 2 to 15 percent of solid lipid, 3 to 18 percent of liquid lipid, 5 to 20 percent of polyhydric alcohol, 0.02 to 1 percent of inorganic salt, 0.01 to 0.8 percent of a preservative, and the balance of deionized water. The preparation method comprises the following steps: melting an oil phase consisting of the resveratrol, the phospholipid, the solid emulsifier, the solid lipid and the liquid lipid, and dispersing the molten oil phase uniformly; meanwhile, heating a water phase consisting of the polyhydric alcohol, the inorganic salt and the deionized water; stirring the water phase; adding the oil phase into the water phase; mixing and performing ultrasonic treatment; stirring, cooling and adding the preservative to form the resveratrol-coated nano solid lipid carrier. The resveratrol-coated nano solid lipid carrier has the particle size of 50 to 200 nm, and can penetrate into a cuticle effectively.

Description

Nano-solid lipid carrier of a kind of coated resveratrol and preparation method thereof
Technical field
The present invention relates to nano-solid lipid carrier of a kind of coated resveratrol and preparation method thereof, belong to chemical field.
Background technology
Innate efficacy composition resveratrol, also known as resvertrol, is colorless needle crystals, is insoluble in water, is soluble in ethanol, acetone and other organic solvent.Its fusing point is at 253 ~ 255 DEG C, and namely 261 DEG C distil, and its structural formula is as the non-flavonoid polyphenolic substance of one, some general character of existing plant polyphenol, the again biological activity of its uniqueness of tool, research finds that polyphenol substance has the effect of significant antioxidation, free radical resisting mostly.
Research shows, resveratrol is applied to having good whitening effect in cosmetics.But resveratrol is insoluble in water, be only soluble in ethanol, acetone and other organic solvent, acetone can not be directly used in cosmetics, and ethanol easily causes skin allergy.Poor biocompatibility simultaneously, not easily through skin; On the other hand, resveratrol is unstable to light and heat, only stable under neutral pH environment under lucifuge condition.These factors all limit the application of resveratrol in cosmetics.
Nano-solid lipid carrier (NLC) is the solid grease solid particle that solidification and crystallization are formed in cooling or phase separation.As a kind of novel carrier, nano-solid lipid carrier possesses that physiological compatibility is good, biodegradable, Drug loading capacity is strong, physical chemistry stable storage, cost are low, be beneficial to the advantages such as large-scale production.Act in cosmetics, can enhanced activity composition permeability, improve closure function and hydration, the stability of active component can be improved as coated carrier simultaneously.
And for the nano-solid lipid carrier preparation research of coated resveratrol more be high pressure homogenization method and common emulsion process.The advantage of high pressure homogenization method is that the nanoparticle particle diameter prepared is little, and shortcoming is complicated operation, easily destroys structure.And common emulsion process is simple to operate, but the sample prepared can disperse heterogeneity, and particle diameter is large, is unfavorable for the infiltration of active component.
Patent CN102614091A (date of publication on August 01st, 2012), the nano structured lipid carrier of disclosed coated resveratrol, because emulsifying agent is wherein mainly tween, fatty alcohol-polyoxyethylene ether series, belong to the nonionic surfactant containing polyoxyethylene block, diox can be brought in cosmetics due to the nonionic surfactant containing polyoxyethylene block by the nano structured lipid carrier of the coated resveratrol obtained like this, and then skin permeation and cause insecurity.
Further, the nanometer liposome of the disclosed coated resveratrol of patent CN103040754A (date of publication on April 17th, 2013), because the solvent adopted in preparation process is ethanol, methanol, chloroform, ether, petroleum ether etc., therefore, the nanometer liposome of this coated resveratrol is owing to also having solvent in system, these solvents all belong to forbidding, limit the use of raw material in cosmetics, and this coating technology is applied in cosmetics and also has certain insecurity.
Patent CN101874763A (date of publication on November 03rd, 2011) is mainly through film evaporation method and add organic solvent and obtain resveratrol liposomal systems, this technology has residual solvent to exist equally, cannot directly be applied in cosmetic product system as cosmetic material coated carrier.
In sum, all there is the safety issue directly applied in cosmetics in the nano structured lipid carrier of coated resveratrol of the prior art.And the present invention proposes to solve this technical problem just.
Summary of the invention
An object of the present invention is unstable in order to solve above-mentioned resveratrol, poor permeability, technical problems such as utilization rate is low and a kind of nano-solid lipid carrier using phospholipid as wherein a kind of coated resveratrol of lipid feedstocks is provided, in the nano-solid lipid carrier of this coated resveratrol, resveratrol is stablized, good penetrability, improves its utilization rate simultaneously.
Two of object of the present invention is to provide the preparation method of the nano-solid lipid carrier of above-mentioned a kind of coated resveratrol.
Technical scheme of the present invention
A nano-solid lipid carrier for coated resveratrol, its particle diameter, at 50 ~ 200nm, counts by weight percentage, its raw material composition and content as follows:
Surplus is deionized water;
Wherein, described phospholipid to be phosphatidylcholine (hereinafter referred to as PC) content the be soybean lecithin of 50% ~ 95%, one or more the combination in Ovum Gallus domesticus Flavus lecithin and hydrolecithin; Be preferably that phosphatidylcholine content is the soybean lecithin of 50%-90%, phosphatidylcholine content be 70% Ovum Gallus domesticus Flavus lecithin or phosphatidylcholine content be the hydrolecithin of 95%;
Described solid state emulsifying agent is ceteareth class, PEG esters, portugal glycoside, polyglycereol-3 methyl distearate, hard ester acyl sodium glutamate, Gemini emulsifying agent or polyglycereol-6 pairs of stearates;
Wherein stereth class is ceteareth-25, ceteareth-6, ceteareth-12, ceteareth-20, ceteareth-30, stereth-2, stereth-21 or three cetearyl alcohol ether-4 phosphoric acid;
PEG esters is PEG-20 tri-Glyceryl Behenate, PEG-8 dioleic acid ester, PEG-8 two stearate, PEG-4 laurate, PEG-8 oleate, PEG-8 stearate, PEG-8 Cera Flava, PEG-20 stearate, PEG-32 stearate, Cremophor RH40, PEG-20 octadecanol ether, PEG-15 cetostearyl alcohol ether, PEG-2 hexadecanol ether, PEG-10 hexadecanol ether or PEG-4 laurate;
Portugal glycoside is cetearyl glucoside, hydroxystearyl alcohol and hydroxy stearate glucosides, sucrose ester, arachidic alcohol glucoside, behenyl alcohol glucoside, cetearyl glucoside, cetearyl alcohol glucoside, Coco-Glucoside, PEG-20 methyl glucoside sesqui-stearate or methyl glucoside sesqui-stearate;
Described solid lipid is saturated fat acids, steroid, glyceride type, waxiness class, alcohols, castor oil hydrogenated, cetearyl alcohol, hard ester alcohol or pentaerythritol stearic acid ester 2;
Wherein saturated fat acids is stearic acid, Palmic acid, capric acid or behenic acid;
Steroid is cholesterol;
Glyceride type is tristerin, cetearyl alcohol caprylate, glyceryl monostearate, cetin, glyceryl tristearate or trilaurin;
Waxiness class is tetramethylolmethane four mountain Yu's acid esters, tetramethylolmethane four caprylic/capric ester, tetramethylolmethane four oleate, pentaerythritol tetrastearate, myristyl myristate ester, cetyl lactate, cetyl riconoleate, myristyl myristate, cetyl palmitate, stearic acid octadecyl ester, spermol cetylate or dipentaerythritol six caprylic/capric ester;
Alcohols is hexadecanol, octadecanol, two Lauryl Alcohols or cetostearyl alcohol;
Described liquid fatty is one or more combination of Vegetable oil lipoprotein, mineral grease and synthetic ester oil;
Wherein Vegetable oil lipoprotein is Jojoba oil, macadimia nut oil, olive oil, Semen pruni armeniacae oil, Oleum Vitis viniferae, American Avocado Tree oil, Testa oryzae oil, safflower oil, Oleum Cocois, Oleum Ricini, the young oil of Helianthi, Semen Tritici aestivi germ oil or lavandula angustifolia wet goods;
Mineral grease is white oil;
Synthetic ester oil is isopropyl myristate, IPIS, stearic acid 13 ester, tristerin, isononyl isononanoate, isomery hexadecane hydrocarbon, iso-octyl palmitate, isopropyl palmitate, caprylic/capric triglyceride, myristyl myristate, squalane, ethyl oleate, stearic acid 13 ester or the different monooctyl ester of isostearic acid;
Described polyhydric alcohol is glycerol, sorbitol, propylene glycol and 1, one or more the combination in 3 butanediols;
Described inorganic salt is the mixture of one or more compositions in sodium chloride, potassium chloride or calcium chloride;
Described antiseptic is benzoic acids, Pyrusussuriensis acids, parabens, germall class, Kazon class, dihydroxymethyl glycolylurea, 1, 2-benzisothiazole-3-ketone, essence of Niobe, Methylisothiazolinone, trichloro-symmetrical diphenyl urea, the bromo-2-nitro of 2--1.3-propylene glycol (Bronopol), glyceryl monolaurate, diazonium ureine, bromo-5 nitros-1 of propylene glycol-5-, 3-bis-Evil alkane, dehydroacetic acid, bromo-5 nitros-1 of propylene glycol-5-, 3-bis-Evil alkane, propylene glycol-bis-imidazolidinyl urea, two imidazolidinyl urea/methyl hydroxybenzoate/propylene glycol, one or more combination in iodo propinyl butyl carbamate,
Described parabens is preferably methyl hydroxybenzoate;
Germall class is imidazolidinyl urea, two imidazolidinyl urea.
The preparation method of the nano-solid lipid carrier of above-mentioned a kind of coated resveratrol, comprises the steps:
(1), join in container by phospholipid, resveratrol, solid lipid, liquid fatty, solid state emulsifying agent, control temperature is melting at 85 ~ 100 DEG C, and is uniformly dispersed, and obtains oil phase;
(2), by polyhydric alcohol, inorganic salt and deionized water join in another container, be heated to 85 ~ 100 DEG C, with 800rpm speed homogenizing, obtain aqueous phase;
(3), the oil phase of step (1) gained is joined in the aqueous phase of step (2) homogenizing, continue the speed homogenizing 3 ~ 6min with 800rpm, obtain emulsification system;
(4), by step (3) gained emulsification system with the power ultrasonic 4 ~ 20min of 80 ~ 800W, then cool while stirring with the speed of 200 ~ 800r/min, when temperature is down to 40 ~ 60 DEG C, add antiseptic and stir, cool to room temperature subsequently, obtains the nano-solid lipid carrier of coated resveratrol.
Beneficial effect of the present invention:
The nano-solid lipid carrier of a kind of coated resveratrol of the present invention, because resveratrol is coated in nano-solid lipid carrier structure, avoids the direct irradiation of light, therefore improves the stability of resveratrol;
Further, the nano-solid lipid carrier of a kind of coated resveratrol of the present invention, owing to containing phospholipid in this nano-solid lipid carrier structure, the similarity of structure of phospholipid and skin lipid structure, improve the adhesiveness of coated resveratrol nano-solid lipid carrier structure on skin, therefore, the permeability of resveratrol is facilitated;
Further, because resveratrol is coated in nano-solid lipid carrier structure, form water slurry, be conducive to being dispersed in aqueous medium, resveratrol is present in carrier structure with molecular structure; Carrier structure facilitates the infiltration of active component simultaneously, and therefore resveratrol utilization rate is high.
Further, the nano-solid lipid carrier of a kind of coated resveratrol of the present invention, be applied in solid lipid carrier structure owing to have employed liposome main material phospholipid, on the basis of solid lipid carrier structure advantage, add the feature of liposome and skin good affinity, and avoid the shortcoming of liposome and solid lipid carrier single structure, as liposome structure is very easily subject to the destruction of surfactant, and solid lipid particulate carrier is because of the deficiency with the aspect such as skin affinity is inadequate, in conjunction with the preparation method of the nano-solid lipid carrier of coated resveratrol of the present invention, effectively can control the particle diameter of the nano-solid liposome of coated resveratrol at 50 ~ 200nm, horny layer is adhered to be more conducive to it, facilitate the infiltration of active component resveratrol on horny layer, thus improve the utilization rate of resveratrol.
Accompanying drawing explanation
The scanning electron microscope (SEM) photograph of the nano-solid lipid carrier of the coated resveratrol of Fig. 1, embodiment 6 gained.
Detailed description of the invention
Below in conjunction with instantiation, the present invention is described further, but protection scope of the present invention is not limited in this.
Raw material used in various embodiments of the present invention, as solid lipid, liquid fatty, resveratrol, phospholipid, solid state emulsifying agent and polyhydric alcohol, inorganic salt etc., except specified otherwise, is conventional raw material in cosmetics, for commercially available.
The nano-solid lipid carrier of coated resveratrol containing phospholipid of embodiments of the invention 3 gained and the nano-solid lipid carrier not containing the coated resveratrol of phospholipid of the comparative examples gained of embodiment 3 carry out resveratrol permeability data.
Assay method is as follows:
1, instrument: Agilent1260 high performance liquid chromatograph, HS-02 horizontal transdermal scattering and permeating instrument.
2, operating procedure:
(1) receiving liquid is configured: the dehydrated alcohol of the PBS buffer solution+60% of 40%.
(2) external osmotic deffusion experiment
1. the nano-solid lipid carrier of the coated resveratrol containing phospholipid of 2mL embodiment to be measured 3 gained is pipetted with the pipet of 2mL in 10mL volumetric flask, 10mL is settled to deionized water, rocking evenly, is the nano-lipid carrier of 0.8% resveratrol by raw sample dilution, reserve liquid 1; Pipette 2mL simultaneously embodiment the comparative examples of 3the nano-solid lipid carrier not containing the coated resveratrol of phospholipid of gained, does same process, is settled to 10mL with deionized water, shake up, reserve liquid 2;
2. in reception tank, load stirrer, and fill receiving liquid, artificial skin to be fixed between the supply pool of diffusion cell and reception tank (bright face supply pool, dark face is towards reception tank), to make skin be immersed in solution;
3. in supply pool, fill the reserve liquid 1 supply liquid in (1), in another supply pool, fill reserve liquid 2, supply liquid simultaneously, contrast the permeability of two samples simultaneously;
4. keep the temperature of recirculated water to be 37 DEG C, under certain rotating speed, extract 1mL receiving liquid when 1h, 2h, 4h, 6h, 8h, 10h, 12h, 24h, 36h with 1mL medical aseptic syringe respectively, supplement the fresh receiving liquid of same volume simultaneously.Sample, after 0.22 μm of filter membrane filters, surveys the concentration of resveratrol in filtrate by efficient liquid phase.
Q = [ C n × V + Σ i = 1 n - 1 C i × 1.0 ] / S
Experimental result:
Wherein C n: receiving liquid drug concentration during the n-th sub-sampling, μ g/mL;
V: receiving liquid volume in receiving chamber, 7mL;
C i: receiving liquid drug concentration during the i-th sub-sampling, μ g/mL;
1.0: each sample volume, mL;
S: effectively infiltrating area, 1cm 2;
Q: permeability, μ g/cm 2.
embodiment 1
A nano-solid lipid carrier for coated resveratrol, by the total of 100g, its raw material composition and content as follows:
Surplus is deionized water;
Described phospholipid to be PC content be 50% soybean lecithin, the food grade products that Beijing Merya's Lecithin Co., Ltd. produces;
Described solid state emulsifying agent is ceteareth-20;
Described solid lipid is glyceryl monostearate;
Described liquid fatty is macadimia nut oil;
Described polyhydric alcohol is propylene glycol;
Described inorganic salt is potassium chloride;
Described antiseptic is attached most importance to azanyl urea.
The nano-solid lipid carrier of above-mentioned coated resveratrol, is characterized in that specifically comprising the steps:
(1), join in container by phospholipid, resveratrol, solid lipid, liquid fatty, solid state emulsifying agent, control temperature is melting at 85 ~ 100 DEG C, and is uniformly dispersed, and obtains oil phase;
(2), by polyhydric alcohol, inorganic salt and deionized water join in another container, be heated to 85 ~ 100 DEG C, with 800rpm speed homogenizing, obtain aqueous phase;
(3), the oil phase of step (1) gained is joined in the aqueous phase of step (2) homogenizing, continue the speed homogenizing 3 ~ 6min with 800rpm, obtain emulsification system;
(4), by step (3) gained emulsification system with the power ultrasonic 4 ~ 20min of 80 ~ 800W, then cool while stirring with the speed of 200 ~ 800r/min, when temperature is down to 40 ~ 60 DEG C, add antiseptic and stir, cool to room temperature subsequently, obtains the nano-solid lipid carrier of coated resveratrol.
embodiment 2
A nano-solid lipid carrier for coated resveratrol, by the total of 100g, its raw material composition and content as follows:
Surplus is deionized water;
Described phospholipid to be PC content be 70% Ovum Gallus domesticus Flavus lecithin, the food grade products that Beijing Merya's Lecithin Co., Ltd. produces;
Described solid state emulsifying agent is PEG-8 dioleic acid ester;
Described solid lipid is hexadecanol;
Described liquid fatty is stearic acid 13 ester;
Described polyhydric alcohol is glycerol;
Described inorganic salt is sodium chloride;
Described antiseptic is methyl hydroxybenzoate.
The preparation method of the nano-solid lipid carrier of above-mentioned coated resveratrol, with embodiment 1.
embodiment 3
A nano-solid lipid carrier for coated resveratrol, namely containing the nano-solid lipid carrier of coated resveratrol of phospholipid, by the total of 100g, its raw material composition and content as follows:
Surplus is deionized water;
Described phospholipid to be PC content be 70% soybean lecithin, the food grade products that Shanxi Sen Fu natural product company limited produces;
Described solid state emulsifying agent is cetearyl glucoside;
Described solid lipid is castor oil hydrogenated;
Described liquid fatty is isopropyl palmitate;
Described polyhydric alcohol is 1,3 butylene glycol;
Described inorganic salt is calcium chloride;
Described antiseptic is propylene glycol-bis-imidazolidinyl urea.
The nano-solid lipid carrier of above-mentioned coated resveratrol, namely containing the preparation method of the nano-solid lipid carrier of the coated resveratrol of phospholipid, with embodiment 1.
the comparative examples of embodiment 3
A nano-solid lipid carrier for coated resveratrol, by the total of 100g, its raw material composition and content as follows:
Surplus is deionized water;
Described solid state emulsifying agent is cetearyl glucoside;
Described solid lipid is castor oil hydrogenated;
Described liquid fatty is isopropyl palmitate;
Described polyhydric alcohol is 1,3 butylene glycol;
Described inorganic salt is calcium chloride;
Described antiseptic is propylene glycol-bis-imidazolidinyl urea.
The nano-solid lipid carrier of above-mentioned coated resveratrol, specifically comprises the steps:
(1), join in container by resveratrol, solid lipid, liquid fatty, solid state emulsifying agent, control temperature is melting at 85 ~ 100 DEG C, and is uniformly dispersed, and obtains oil phase;
(2), by polyhydric alcohol, inorganic salt and deionized water join in another container, be heated to 85 ~ 100 DEG C, with 800rpm speed homogenizing, obtain aqueous phase;
(3), the oil phase of step (1) gained is joined in the aqueous phase of step (2) homogenizing, continue the speed homogenizing 3 ~ 6min with 800rpm, obtain emulsification system;
(4), by step (3) gained emulsification system with the power ultrasonic 4 ~ 20min of 80 ~ 800W, then cool while stirring with the speed of 200 ~ 800r/min, when temperature is down to 40 ~ 60 DEG C, add antiseptic and stir, cool to room temperature subsequently, obtains not containing the nano-solid lipid carrier of the coated resveratrol of phospholipid.
Carry out resveratrol permeability data mensuration in the nano-solid lipid carrier of coated resveratrol containing phospholipid of above-described embodiment 3 gained and the nano-solid lipid carrier not containing the coated resveratrol of phospholipid of the comparative examples gained of embodiment 3, the results are shown in following table:
In the nano-solid lipid carrier structure of the coated resveratrol containing phospholipid of embodiment 3 gained as can be seen from the above table the coated adhesive capacity of resveratrol on artificial skin be greater than gained in the comparative examples of embodiment 3 not containing the adhesive capacity of resveratrol coated in the solid lipid carrier structure of phospholipid, high adhesive capacity is conducive to promoting that resveratrol permeates in horny layer, indicates resveratrol coated in the solid lipid carrier structure containing phospholipid thus and is more conducive to the infiltration on skin.
embodiment 4
A nano-solid lipid carrier for coated resveratrol, by the total of 100g, its raw material composition and content as follows:
Surplus is deionized water;
Described phospholipid to be PC content be 80% soybean lecithin, the food grade products that Shanxi Sen Fu natural product company limited produces;
Described solid state emulsifying agent is polyglycereol-6 pairs of stearates;
Described solid lipid is behenic acid;
Described liquid fatty is Semen Tritici aestivi germ oil;
Described polyhydric alcohol is propylene glycol;
Described inorganic salt is potassium chloride;
Described antiseptic is the bromo-2-nitro of 2--1.3-propylene glycol.
The preparation method of the nano-solid lipid carrier of above-mentioned coated resveratrol, with embodiment 1.
embodiment 5
A nano-solid lipid carrier for coated resveratrol, by the total of 100g, its raw material composition and content as follows:
Surplus is deionized water
Described phospholipid to be PC content be 90% soybean lecithin, the pharma grade product that Shanxi Sen Fu natural product company limited produces;
Described solid state emulsifying agent is sucrose ester;
Described solid lipid is Palmic acid;
Described liquid fatty is isopropyl myristate;
Described polyhydric alcohol is sorbitol;
Described inorganic salt is potassium chloride;
Described antiseptic is methyl hydroxybenzoate.
The preparation method of the nano-solid lipid carrier of above-mentioned coated resveratrol, with embodiment 1.
embodiment 6
A nano-solid lipid carrier for coated resveratrol, by the total of 100g, its raw material composition and content as follows:
Surplus is deionized water;
Described phospholipid to be PC content be 95% hydrolecithin, the pharma grade product that base bio tech ltd, Shanghai one provides;
Described solid state emulsifying agent is Gemini emulsifying agent;
Described solid lipid is dipentaerythritol six caprylic/capric ester;
Described liquid fatty is caprylic/capric triglyceride;
Described polyhydric alcohol is 1,3 butylene glycol;
Described inorganic salt is sodium chloride;
Described antiseptic is two imidazolidinyl urea.
The preparation method of the nano-solid lipid carrier of above-mentioned coated resveratrol, with embodiment 1.
Use Quanta200F type scanning electron microscope (FEIcompany, Quanta200FEG, Holland, accelerating potential 5 ~ 30kv) the appearance form of the nano-solid lipid carrier of the coated resveratrol of above-mentioned gained is scanned, the microscopic appearance figure of gained is as shown in Figure 1.As can be seen from Figure 1 the arrangement of nano-solid lipid particles closely, and uniform particles, has good coating function to resveratrol.
In sum, the nano-solid lipid carrier of a kind of coated resveratrol of the present invention, because introducing phospholipid in carrier structure, improves the adhesiveness of carrier structure on skin, and then is conducive to the infiltration of resveratrol on skin.
The above is only the citing of embodiments of the present invention; it should be pointed out that for those skilled in the art, under the prerequisite not departing from the technology of the present invention principle; can also make some improvement and modification, these improve and modification also should be considered as protection scope of the present invention.

Claims (9)

1. a nano-solid lipid carrier for coated resveratrol, it is characterized in that the nano-solid lipid carrier of described coated resveratrol, its particle diameter is 50 ~ 200nm, counts by weight percentage, its raw material composition and content as follows:
Described phospholipid to be phosphatidylcholine content the be soybean lecithin of 50% ~ 95%, one or more the combination in Ovum Gallus domesticus Flavus lecithin and hydrolecithin;
Described solid state emulsifying agent is ceteareth class, PEG esters, portugal glycoside, polyglycereol-3 methyl distearate, the two stearate of hard ester acyl sodium glutamate, Gemini emulsifying agent or polyglycereol 6-;
Wherein stereth class is ceteareth-25, ceteareth-6, ceteareth-12, ceteareth-20, ceteareth-30, stereth-2, stereth-21 or three cetearyl alcohol ether-4 phosphoric acid;
PEG esters is PEG-20 tri-Glyceryl Behenate, PEG-8 dioleic acid ester, PEG-8 two stearate, PEG-4 laurate, PEG-8 oleate, PEG-8 stearate, PEG-8 Cera Flava, PEG-20 stearate, PEG-32 stearate, Cremophor RH40, PEG-20 octadecanol ether, PEG-15 cetostearyl alcohol ether, PEG-2 hexadecanol ether, PEG-10 hexadecanol ether or PEG-4 laurate;
Portugal glycoside is cetearyl glucoside, hydroxystearyl alcohol and hydroxy stearate glucosides, sucrose ester, arachidic alcohol glucoside, behenyl alcohol glucoside, cetearyl glucoside, cetearyl alcohol glucoside, Coco-Glucoside, PEG-20 methyl glucoside sesqui-stearate or methyl glucoside sesqui-stearate;
Described solid lipid is saturated fat acids, steroid, glyceride type, waxiness class, alcohols, castor oil hydrogenated, cetearyl alcohol, hard ester alcohol or pentaerythritol stearic acid ester 2;
Wherein saturated fat acids is stearic acid, Palmic acid, capric acid or behenic acid;
Steroid is cholesterol;
Glyceride type is tristerin, cetearyl alcohol caprylate, glyceryl monostearate, cetin, glyceryl tristearate or trilaurin;
Waxiness class is tetramethylolmethane four mountain Yu's acid esters, tetramethylolmethane four caprylic/capric ester, tetramethylolmethane four oleate, pentaerythritol tetrastearate, myristyl myristate ester, cetyl lactate, cetyl riconoleate, myristyl myristate, cetyl palmitate, stearic acid octadecyl ester, spermol cetylate or dipentaerythritol six caprylic/capric ester;
Alcohols is hexadecanol, octadecanol, two Lauryl Alcohols or cetostearyl alcohol;
Described liquid fatty is one or more the combination in Vegetable oil lipoprotein, mineral grease and synthetic ester oil;
Wherein Vegetable oil lipoprotein is Jojoba oil, macadimia nut oil, olive oil, Semen pruni armeniacae oil, Oleum Vitis viniferae, American Avocado Tree oil, Testa oryzae oil, safflower oil, Oleum Cocois, Oleum Ricini, the young oil of Helianthi, Semen Tritici aestivi germ oil or Oleum lavandula angustifolia;
Mineral grease is white oil;
Synthetic ester oil is isopropyl myristate, IPIS, stearic acid 13 ester, tristerin, isononyl isononanoate, isomery hexadecane hydrocarbon, iso-octyl palmitate, isopropyl palmitate, caprylic/capric triglyceride, myristyl myristate, squalane, ethyl oleate, stearic acid 13 ester or the different monooctyl ester of isostearic acid;
Described polyhydric alcohol is one or more the combination in glycerol, sorbitol, propylene glycol and 1,3 butylene glycol;
Described inorganic salt is the mixture of one or more compositions in sodium chloride, potassium chloride and calcium chloride;
Described antiseptic is benzoic acids, Pyrusussuriensis acids, parabens, germall class, Kazon class, dihydroxymethyl glycolylurea, 1, 2-benzisothiazole-3-ketone, essence of Niobe, Methylisothiazolinone, trichloro-symmetrical diphenyl urea, the bromo-2-nitro of 2--1.3-propylene glycol (Bronopol), glyceryl monolaurate, diazonium ureine, bromo-5 nitros-1 of propylene glycol-5-, 3-bis-Evil alkane, dehydroacetic acid, bromo-5 nitros-1 of propylene glycol-5-, 3-bis-Evil alkane, propylene glycol-bis-imidazolidinyl urea, two imidazolidinyl urea/methyl hydroxybenzoate/propylene glycol, one or more combination in iodo propinyl butyl carbamate,
Wherein parabens is methyl hydroxybenzoate;
Germall class is imidazolidinyl urea or two imidazolidinyl urea.
2. the nano-solid lipid carrier of a kind of coated resveratrol as claimed in claim 1, is characterized in that:
The soybean lecithin of described phospholipid to be phosphatidylcholine content be 50%-90%, phosphatidylcholine content be 70% Ovum Gallus domesticus Flavus lecithin or phosphatidylcholine content be the hydrolecithin of 95%;
Described solid state emulsifying agent is ceteareth class, PEG esters, portugal glycoside, Gemini emulsifying agent or polyglycereol-6 pairs of stearates;
Wherein stereth class is ceteareth-20;
PEG esters is PEG-8 dioleic acid ester;
Portugal glycoside is cetearyl glucoside or sucrose ester;
Described solid lipid is saturated fat acids, glyceride type, waxiness class, alcohols or castor oil hydrogenated;
Wherein saturated fat acids is Palmic acid or behenic acid;
Glyceride type is glyceryl monostearate;
Waxiness class is dipentaerythritol six caprylic/capric ester;
Alcohols is hexadecanol;
Described liquid fatty is Vegetable oil lipoprotein or synthetic ester oil;
Wherein Vegetable oil lipoprotein is macadimia nut oil or Semen Tritici aestivi germ oil;
Synthetic ester oil is isopropyl myristate, stearic acid 13 ester, isopropyl palmitate or caprylic/capric triglyceride;
Described antiseptic is parabens, germall class, 2-bromo-2-nitro-1.3-propylene glycol, diazonium ureine or propylene glycol-bis-imidazolidinyl urea;
Wherein parabens is methyl hydroxybenzoate;
Germall class is two imidazolidinyl urea.
3. the nano-solid lipid carrier of a kind of coated resveratrol as claimed in claim 2, is characterized in that counting by weight percentage, its raw material composition and content as follows:
Described phospholipid to be phosphatidylcholine content be 50% soybean lecithin;
Described solid state emulsifying agent is ceteareth-20;
Described solid lipid is glyceryl monostearate;
Described liquid fatty is macadimia nut oil;
Described polyhydric alcohol is propylene glycol;
Described inorganic salt is potassium chloride;
Described antiseptic is attached most importance to azanyl urea.
4. the nano-solid lipid carrier of a kind of coated resveratrol as claimed in claim 2, is characterized in that counting by weight percentage, its raw material composition and content as follows:
Described phospholipid to be phosphatidylcholine content be 70% Ovum Gallus domesticus Flavus lecithin;
Described solid state emulsifying agent is PEG-8 dioleic acid ester;
Described solid lipid is hexadecanol;
Described liquid fatty is stearic acid 13 ester;
Described polyhydric alcohol is glycerol;
Described inorganic salt is sodium chloride;
Described antiseptic is methyl hydroxybenzoate.
5. the nano-solid lipid carrier of a kind of coated resveratrol as claimed in claim 2, is characterized in that counting by weight percentage, its raw material composition and content as follows:
Described phospholipid to be phosphatidylcholine content be 70% soybean lecithin;
Described solid state emulsifying agent is cetearyl glucoside;
Described solid lipid is castor oil hydrogenated;
Described liquid fatty is isopropyl palmitate;
Described polyhydric alcohol is 1,3 butylene glycol;
Described inorganic salt is calcium chloride;
Described antiseptic is propylene glycol-bis-imidazolidinyl urea.
6. the nano-solid lipid carrier of a kind of coated resveratrol as claimed in claim 2, is characterized in that counting by weight percentage, its raw material composition and content as follows:
Described phospholipid to be phosphatidylcholine content be 80% soybean lecithin;
Described solid state emulsifying agent is polyglycereol-6 pairs of stearates;
Described solid lipid is behenic acid;
Described liquid fatty is Semen Tritici aestivi germ oil;
Described polyhydric alcohol is propylene glycol;
Described inorganic salt is potassium chloride;
Described antiseptic is the bromo-2-nitro of 2--1.3-propylene glycol.
7. the nano-solid lipid carrier of a kind of coated resveratrol as claimed in claim 2, is characterized in that counting by weight percentage, its raw material composition and content as follows:
Described phospholipid to be phosphatidylcholine content be 90% soybean lecithin;
Described solid state emulsifying agent is sucrose ester;
Described solid lipid is Palmic acid;
Described liquid fatty is isopropyl myristate;
Described polyhydric alcohol is sorbitol;
Described inorganic salt is potassium chloride;
Described antiseptic is methyl hydroxybenzoate.
8. the nano-solid lipid carrier of a kind of coated resveratrol as claimed in claim 2, is characterized in that counting by weight percentage, its raw material composition and content as follows:
Described phospholipid to be phosphatidylcholine content be 95% hydrolecithin;
Described solid state emulsifying agent is Gemini emulsifying agent;
Described solid lipid is dipentaerythritol six caprylic/capric ester;
Described liquid fatty is caprylic/capric triglyceride;
Described polyhydric alcohol is 1,3 butylene glycol;
Described inorganic salt is sodium chloride;
Described antiseptic is two imidazolidinyl urea.
9. the preparation method of the nano-solid lipid carrier of a kind of coated resveratrol as described in as arbitrary in claim 1-8, is characterized in that specifically comprising the steps:
(1), join in container by phospholipid, resveratrol, solid lipid, liquid fatty, solid state emulsifying agent, control temperature is melting at 85 ~ 100 DEG C, and is uniformly dispersed, and obtains oil phase;
(2), by polyhydric alcohol, inorganic salt and deionized water join in another container, be heated to 85 ~ 100 DEG C, with 800rpm speed homogenizing, obtain aqueous phase;
(3), the oil phase of step (1) gained is joined in the aqueous phase of step (2) homogenizing, continue the speed homogenizing 3 ~ 6min with 800rpm, obtain emulsification system;
(4), by step (3) gained emulsification system with the power ultrasonic 4 ~ 20min of 80 ~ 800W, then cool while stirring with the speed of 200 ~ 800r/min, when temperature is down to 40 ~ 60 DEG C, add antiseptic and stir, cool to room temperature subsequently, obtains the nano-solid lipid carrier of coated resveratrol.
CN201610034448.4A 2016-01-19 2016-01-19 Resveratrol-coated nano solid lipid carrier and preparation method thereof Pending CN105534724A (en)

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CN107997979B (en) * 2018-01-08 2021-02-05 苏州纳康生物科技有限公司 Preparation method of thermosensitive liposome with whitening effect
CN107997979A (en) * 2018-01-08 2018-05-08 苏州纳康生物科技有限公司 A kind of preparation method of the temperature sensitive liposome with white-skinned face function
CN108065396A (en) * 2018-01-15 2018-05-25 中鸿纳米纤维技术丹阳有限公司 A kind of preparation method of the oxidation resistant nutrient containing nanometer pelelith powder
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CN110200829A (en) * 2019-05-17 2019-09-06 湖南人文科技学院 A kind of resveratrol nanometer alcohol plastid and the preparation method and application thereof
CN110200829B (en) * 2019-05-17 2022-04-01 湖南人文科技学院 Resveratrol nano ethosome and preparation method and application thereof
CN110812267A (en) * 2019-11-15 2020-02-21 上海应用技术大学 Soybean isoflavone liposome and preparation method thereof
CN112336649A (en) * 2020-11-09 2021-02-09 江南大学 Preparation method and product of skin co-permeation carrier of ceramide and fat-soluble active substance
CN112336649B (en) * 2020-11-09 2021-10-22 江南大学 Preparation method and product of skin co-permeation carrier of ceramide and fat-soluble active substance
CN114028272A (en) * 2021-11-30 2022-02-11 江苏瑞霆生物科技有限公司 Liquid crystal nano emulsion of high-permeability vegetable oil and preparation method and application thereof
WO2023154479A1 (en) * 2022-02-10 2023-08-17 Dyve Biosciences, Inc. Formulations for transdermal administration of active agents

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