CN105496801A - Nanostructured solid lipid carrier coating vitamin A palmitate and preparation method thereof - Google Patents
Nanostructured solid lipid carrier coating vitamin A palmitate and preparation method thereof Download PDFInfo
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
- A61K8/14—Liposomes; Vesicles
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/55—Phosphorus compounds
- A61K8/553—Phospholipids, e.g. lecithin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/67—Vitamins
- A61K8/671—Vitamin A; Derivatives thereof, e.g. ester of vitamin A acid, ester of retinol, retinol, retinal
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
- A61K2800/10—General cosmetic use
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Abstract
The invention provides a nanostructured solid lipid carrier coating vitamin A palmitate and a preparation method. The nanostructured solid lipid carrier coating vitamin A palmitate comprises 1-15% of vitamin A palmitate, 0.5-5% of phospholipid, 3-30% of solid emulsifier, 2-15% of solid lipid, 2-10% of liquid lipid, 0.02-1% of inorganic salt, 0.01-0.8% of preservative and the balance of deionized water by weight. The preparation method comprises the following steps: melting and uniformly dispersing vitamin A palmitate, phospholipid, the solid emulsifier, solid lipid and liquid lipid to obtain an oil phase, mixing and heating the inorganic salt and the deionized water to obtain a water phase, adding the oil phase under stirring and adding the preservative after ultrasonic treatment and cooling in sequence, thus obtaining the nanostructured solid lipid carrier coating vitamin A palmitate. The stability and dispersibility of vitamin A palmitate are improved and permeation of vitamin A palmitate on skins is promoted by adopting the nanostructured solid lipid carrier.
Description
Technical field
The present invention relates to nano-solid lipid carrier of a kind of coated vitamin A palmitate and preparation method thereof, belong to chemical field.
Background technology
Innate efficacy ingredients Vitamin A cetylate is the product after vitamin A and Palmic acid esterification.It has possessed the function of vitamin, may be used for the treatment of vitro skin disease, as Niu Pi Xian, acne, photoaging and epithelial cancer etc.Compared with natural vitamin A, relatively improve stability.But be still easily destroyed after esterification, water insoluble, ethanol etc., to air, light and humidity sensitive, fusing point is 28 ~ 29 DEG C.Therefore for unstable during preparation, easily at storage and use procedure mesometamorphism.Meanwhile, there is certain zest, as Hong Xian can be caused, and peels off decortication and sees the burning sensation after light.It is impelled better to disperse often through emulsifying, the technology such as coated.
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.
At present about coated vitamin A palmitate technology, the coated vitamin A of fibrous membrane (CN104846555A) that useful gelatin is formed; Also the coated vitamin A of microcapsule structure (CN104661656A) of useful arabic gum formation; And microcapsule structure is under certain shearing force, structure is easy to destroy, and is not suitable for being applied in cosmetic product system.And the nano-solid lipid carrier of coated vitamin A has not yet to see report.
Summary of the invention
One of the object of the invention be in order to solve above-mentioned vitamin A palmitate to be applied in cosmetics unstable, dispersive property is poor, the not easily technical problem such as infiltration and provide a kind of nano-solid lipid carrier of coated vitamin A palmitate on skin.The nano-solid lipid carrier of this coated vitamin A palmitate makes vitamin A palmitate stablize, and in aqueous medium, dispersive property is good, is conducive to the advantages such as the infiltration on skin simultaneously.
Two of object of the present invention is the preparation method of the nano-solid lipid carrier providing above-mentioned a kind of coated vitamin A palmitate.
Technical scheme of the present invention
A nano-solid lipid carrier for coated vitamin A palmitate, counts by weight percentage, its raw material composition and content as follows:
Described phospholipid to be phosphatidylcholine (hereinafter referred to as PC) content be 50% ~ 95% soybean lecithin, Ovum Gallus domesticus Flavus lecithin, one or more combination in 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 or 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 inorganic salt is sodium chloride, potassium chloride or calcium chloride;
Described antiseptic is alcohols, parabens, germall class, sorbic acid, Kazon, 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, 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, alcohols is o-p-Cymene-5-alcohol, polyquaternary ammonium salt-73/ pentanediol, pentanediol, 1,3-butylene glycol, methyl propanediol or phenoxyethanol;
Parabens methyl hydroxybenzoate, ethyl hydroxybenzoate, propylparaben or butoben;
Germall class is imidazolidinyl urea or two imidazolidinyl urea.
The preparation method of the nano-solid lipid carrier of above-mentioned coated vitamin A palmitate, specifically comprises the steps:
(1), join in container by vitamin A palmitate, phospholipid, solid lipid, liquid fatty, solid state emulsifying agent, control temperature is melting at 70 ~ 85 DEG C, and is uniformly dispersed, and obtains oil phase;
(2), by inorganic salt and deionized water join in another container, be heated to 70 ~ 85 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 vitamin A palmitate.
Beneficial effect of the present invention
The nano-solid lipid carrier of a kind of coated vitamin A palmitate of the present invention, because vitamin A palmitate is coated in nano-solid lipid carrier structure, avoids the direct irradiation of light, therefore improves the stability of vitamin A palmitate;
Further, the nano-solid lipid carrier of a kind of coated vitamin A palmitate 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 vitamin A palmitate nano-solid lipid carrier structure on skin, therefore, the permeability of vitamin A palmitate is facilitated;
Further, the nano-solid lipid carrier of a kind of coated vitamin A palmitate of the present invention, because vitamin A palmitate is coated in nano-solid lipid carrier structure, form water slurry, be conducive to being dispersed in aqueous medium, vitamin A palmitate is present in carrier structure with molecular structure; Carrier structure facilitates the infiltration of active component simultaneously, and therefore vitamin A palmitate utilization rate is high.
Further, the nano-solid lipid carrier of a kind of coated vitamin A palmitate 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 vitamin A palmitate of the present invention, effectively can control the particle diameter of the nano-solid liposome of coated vitamin A palmitate at 50 ~ 200nm, horny layer is adhered to be more conducive to it, facilitate the infiltration of active component vitamin A palmitate on horny layer, thus improve the utilization rate of vitamin A palmitate.
Accompanying drawing explanation
The scanning electron microscope (SEM) photograph of the nano-solid lipid carrier of the coated vitamin A palmitate of Fig. 1, embodiment 6 gained.
Detailed description of the invention
Also by reference to the accompanying drawings the present invention is described further below by instantiation, 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, vitamin A Palmic acid, phospholipid, solid state emulsifying agent and polyhydric alcohol, inorganic salt etc., except specified otherwise, is conventional raw material in cosmetics, for commercially available.
It is as follows that the nano-solid lipid carrier of coated vitamin A palmitate containing phospholipid of embodiments of the invention 3 gained and the nano-solid lipid carrier not containing the coated vitamin A palmitate of phospholipid of the comparative examples gained of embodiment 3 carry out vitamin A palmitate permeability data assay method:
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 vitamin A palmitate containing phospholipid of gained in 1mL embodiment to be measured is pipetted with the pipet of 2mL in 10mL volumetric flask, 10mL is settled to deionized water, rock evenly, by the nano-lipid carrier that raw sample dilution is 0.8% vitamin A palmitate, reserve liquid 1; Pipette the nano-solid lipid carrier not containing the coated vitamin A palmitate of phospholipid of the comparative examples gained of 2mL embodiment 3 simultaneously, do same process, be 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 vitamin A palmitate in filtrate by efficient liquid phase.
Experimental result:
Wherein receiving liquid drug concentration during the Cn: the n-th sub-sampling, μ g/mL;
V: receiving liquid volume in receiving chamber, 7mL;
Receiving liquid drug concentration during the Ci: 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 vitamin A palmitate, by the total of 100g, its raw material composition and content as follows:
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 inorganic salt is sodium chloride;
Described antiseptic is attached most importance to azanyl urea.
The nano-solid lipid carrier of above-mentioned coated vitamin A palmitate, specifically comprises the steps:
(1), join in container by vitamin A palmitate, phospholipid, solid lipid, liquid fatty, solid state emulsifying agent, control temperature is melting at 70 ~ 85 DEG C, and is uniformly dispersed, and obtains oil phase;
(2), by inorganic salt and deionized water join in another container, be heated to 70 ~ 85 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 vitamin A palmitate.
embodiment 2
A nano-solid lipid carrier for coated vitamin A palmitate, by the total of 100g, its raw material composition and content as follows:
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 inorganic salt is potassium chloride;
Described antiseptic is methyl hydroxybenzoate.
The preparation method of the nano-solid lipid carrier of above-mentioned coated vitamin A palmitate, with embodiment 1.
embodiment 3
A nano-solid lipid carrier for coated vitamin A palmitate, namely containing the nano-solid lipid carrier of coated vitamin A palmitate of phospholipid, by the total of 100g, its raw material composition and content as follows:
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 inorganic salt is potassium chloride;
Described antiseptic is propylene glycol-bis-imidazolidinyl urea.
The nano-solid lipid carrier of above-mentioned coated vitamin A palmitate, namely containing the preparation method of the nano-solid lipid carrier of the coated vitamin A palmitate of phospholipid, with embodiment 1.
Embodiment 3 case of comparative examples
A nano-solid lipid carrier for coated vitamin A palmitate, namely not containing the nano-solid lipid carrier of coated vitamin A palmitate of phospholipid, by the total of 100g, its raw material composition and content as follows:
Described solid state emulsifying agent is cetearyl glucoside;
Described solid lipid is castor oil hydrogenated;
Described liquid fatty is isopropyl palmitate;
Described inorganic salt is potassium chloride;
Described antiseptic is propylene glycol-bis-imidazolidinyl urea.
Above-mentioned not containing the preparation method of the nano-solid lipid carrier of the coated vitamin A palmitate of phospholipid, specifically comprise the steps:
(1), join in container by vitamin A palmitate, solid lipid, liquid fatty, solid state emulsifying agent, control temperature is melting at 70 ~ 85 DEG C, and is uniformly dispersed, and obtains oil phase;
(2), by inorganic salt and deionized water join in another container, be heated to 70 ~ 85 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, obtain the nano-solid lipid carrier of coated vitamin A palmitate, be not containing the nano-solid lipid carrier of the coated vitamin A palmitate of phospholipid.
Carrying out permeability data mensuration to carrying out vitamin A palmitate in the nano-solid lipid carrier of coated vitamin A palmitate containing phospholipid of above-described embodiment 3 gained and the nano-solid lipid carrier not containing the coated vitamin A palmitate of phospholipid of the comparative examples gained of embodiment 3, the results are shown in following table:
The adhesive capacity not containing the coated vitamin A palmitate of solid lipid carrier structure of phospholipid of gained in the comparative examples of embodiment 3 is greater than as can be seen from the above table containing the adhesive capacity of vitamin A palmitate on artificial skin that the solid lipid carrier structure of phospholipid is coated, high adhesive capacity is conducive to promoting that vitamin A palmitate permeates in horny layer, and the vitamin A palmitate indicated thus containing the solid lipid carrier structure of phospholipid is coated is more conducive to the infiltration on skin.
embodiment 4
A nano-solid lipid carrier for coated vitamin A palmitate, by the total of 100g, its raw material composition and content as follows:
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 inorganic salt is calcium 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 vitamin A palmitate, with embodiment 1.
embodiment 5
A nano-solid lipid carrier for coated vitamin A palmitate, by the total of 100g, its raw material composition and content as follows:
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 inorganic salt is calcium chloride;
Described antiseptic is methyl hydroxybenzoate.
The preparation method of the nano-solid lipid carrier of above-mentioned coated vitamin A palmitate, with embodiment 1.
embodiment 6
A nano-solid lipid carrier for coated vitamin A palmitate, by the total of 100g, its raw material composition and content as follows:
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 inorganic salt is sodium chloride;
Described antiseptic is two imidazolidinyl urea.
The preparation method of the nano-solid lipid carrier of above-mentioned coated vitamin A palmitate, 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 vitamin A palmitate 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 vitamin A palmitate.
In sum, the nano-solid lipid carrier of a kind of coated vitamin A palmitate 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 vitamin A palmitate 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 vitamin A palmitate, is characterized in that the nano-solid lipid carrier of described coated vitamin A palmitate counts by weight percentage, its raw material composition and content as follows:
Described phospholipid to be phosphatidylcholine content be 50% ~ 95% soybean lecithin, Ovum Gallus domesticus Flavus lecithin, one or more combination in hydrolecithin and deoiled phosphatides;
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 or 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 be 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 inorganic salt is sodium chloride, potassium chloride or calcium chloride;
Described antiseptic is alcohols, parabens, germall class, sorbic acid, Kazon, 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, 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, described alcohols is o-p-Cymene-5-alcohol, polyquaternary ammonium salt-73/ pentanediol, pentanediol, 1,3-butylene glycol, methyl propanediol or phenoxyethanol;
Described parabens methyl hydroxybenzoate, ethyl hydroxybenzoate, propylparaben or butoben;
Germall class is imidazolidinyl urea or two imidazolidinyl urea.
2. the nano-solid lipid carrier of a kind of coated vitamin A palmitate 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 vitamin A palmitate 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 inorganic salt is sodium chloride;
Described antiseptic is attached most importance to azanyl urea.
4. the nano-solid lipid carrier of a kind of coated vitamin A palmitate 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 inorganic salt is potassium chloride;
Described antiseptic is methyl hydroxybenzoate.
5. the nano-solid lipid carrier of a kind of coated vitamin A palmitate 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 inorganic salt is potassium chloride;
Described antiseptic is propylene glycol-bis-imidazolidinyl urea.
6. the nano-solid lipid carrier of a kind of coated vitamin A palmitate 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 inorganic salt is calcium 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 vitamin A palmitate 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 inorganic salt is calcium chloride;
Described antiseptic is methyl hydroxybenzoate.
8. the nano-solid lipid carrier of a kind of coated vitamin A palmitate 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 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 vitamin A palmitate as described in as arbitrary in claim 1-8, is characterized in that specifically comprising the steps:
(1), join in container by vitamin A palmitate, phospholipid, solid lipid, liquid fatty, solid state emulsifying agent, control temperature is melting at 70 ~ 85 DEG C, and is uniformly dispersed, and obtains oil phase;
(2), by inorganic salt and deionized water join in another container, be heated to 70 ~ 85 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 vitamin A palmitate.
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Cited By (7)
Publication number | Priority date | Publication date | Assignee | Title |
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US10493009B2 (en) | 2016-12-13 | 2019-12-03 | The Procter & Gamble Company | Stable personal care compositions containing a retinoid |
CN107549801A (en) * | 2017-08-24 | 2018-01-09 | 福格森(武汉)生物科技股份有限公司 | A kind of multilayer embeds solid lipid calcium particulate |
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CN108451787A (en) * | 2018-05-23 | 2018-08-28 | 上海格兰化妆品有限公司 | A kind of nano-lipid carrier and preparation method thereof of embedding vitamin A alcohol |
CN108451787B (en) * | 2018-05-23 | 2020-01-07 | 上海格兰化妆品有限公司 | Vitamin A alcohol-embedded nano lipid carrier and preparation method thereof |
CN113164368A (en) * | 2018-12-04 | 2021-07-23 | 株式会社Lg生活健康 | High-content and sustained-release retinoid capsule and wrinkle-improving composition containing same |
EP4282281A3 (en) * | 2019-12-04 | 2024-03-06 | Alesco S.r.l. | Solid form formulation comprising chromium or copper or a vitamin, compositions and uses thereof |
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