CN108938456A - A kind of composition and preparation method and application - Google Patents
A kind of composition and preparation method and application Download PDFInfo
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- CN108938456A CN108938456A CN201811172233.4A CN201811172233A CN108938456A CN 108938456 A CN108938456 A CN 108938456A CN 201811172233 A CN201811172233 A CN 201811172233A CN 108938456 A CN108938456 A CN 108938456A
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- Prior art keywords
- composition
- preparation
- alcohol
- alcohol plastid
- gel
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- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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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
- A61K8/60—Sugars; Derivatives thereof
- A61K8/606—Nucleosides; Nucleotides; Nucleic acids
-
- 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
- A61K8/04—Dispersions; Emulsions
- A61K8/042—Gels
-
- 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
-
- 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
-
- 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
- A61K8/63—Steroids; Derivatives thereof
-
- 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
- A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
- A61K8/73—Polysaccharides
-
- 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
- A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
- A61K8/81—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds obtained by reactions involving only carbon-to-carbon unsaturated bonds
- A61K8/8141—Compositions of homopolymers or copolymers of compounds having one or more unsaturated aliphatic radicals, each having only one carbon-to-carbon double bond, and at least one being terminated by only one carboxyl radical, or of salts, anhydrides, esters, amides, imides or nitriles thereof; Compositions of derivatives of such polymers
- A61K8/8147—Homopolymers or copolymers of acids; Metal or ammonium salts thereof, e.g. crotonic acid, (meth)acrylic acid; Compositions of derivatives of such polymers
-
- 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
-
- 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
- A61K2800/80—Process related aspects concerning the preparation of the cosmetic composition or the storage or application thereof
- A61K2800/82—Preparation or application process involves sonication or ultrasonication
Abstract
The present invention provides a kind of compositions and preparation method and application, it is related to technical field of skin care, it is mostly ball-type or subsphaeroidal multilamellar vesicles structure that the obtained KGM modified phospholipid load transdermal alcohol plastid of NADH, which is the novel form of one kind, it is more stable with thermodynamics, partial size is smaller, and encapsulation rate is high, have percutaneous abilities faster, it is stronger, skin-tolerant can be good, the features such as dosage is less, reduces the incidence of adverse reaction, improves safety.And, the preparation process for preparing gel composite skin care product using the alcohol plastid is simple, NADH alcohol plastid can be obtained using stirring, homogeneous, ultrasound, filtering, alcohol plastid and penetrating agent are uniformly mixed with the gel-type vehicle being swollen again after mixing can obtain Ethosomal gel.
Description
Technical field
A kind of composition for referring in particular to can be used for improve looks the present invention relates to technical field of skin care and its preparation side
Method and application.
Background technique
In the prior art, alcohol plastid has hypotoxicity, hypoimmunity, good cell compatibility, can load water simultaneously
The advantages that dissolubility, fat-soluble macromolecular drug, thus received significant attention in drug delivery especially cutaneous penetration field.Alcohol
Plastid contains the ethyl alcohol of relatively high volume fraction, makes it have imitated vesicle structure, and form is mostly subsphaeroidal or spherical, shape circle
Whole smooth, the presence of ethyl alcohol improves lipophilicity and amphiphilic species in the phospholipid bilayer of vesica and the dissolution at aqueous center
Degree.Alcohol plastid carries drug first and penetrates cuticula arrival deep skin through intercellular pathways, then discharges drug, makes drug to skin
Skin deep layer is distributed and promotes percutaneous drug absorption.Its detailed process are as follows: 1. ethyl alcohol changes the close-packed arrays of lipid between horn cell,
Enhance its mobility, permeability enhancing;2. alcohol plastid is using its flexible and morphotropism, by between disorganized horn cell
Lipid carries drug and reaches deep skin;Enter in the cell of deep skin 3. alcohol plastid carries drug, plays locally targeting
Effect;4. the cell membrane fusion of alcohol plastid and deep skin, release drug, are distributed drug to deep skin, and promote its warp
Skin absorbs.Alcohol plastid may also promote drug to deep skin distribution and percutaneous absorbtion through hair follicle and sebaceous glands approach.Therefore, alcohol
Plastid film is flexible preferably, and when passing through skin barrier, deformability increases, and is more suitable for passing through horn cell gap, is to take
Carry the ideal carrier of macromolecular.
Currently, common transdermal drug delivery system, refers to and be administered in skin surface, drug is each through skin with certain speed
Layer, enters Whole Body blood circulation by capillary and reaches effective blood drug concentration, realizes whole body or local therapeutic effects
Novel form.Compared to administration modes such as oral, intravenous injections, cutaneous penetration has the first pass effect for avoiding liver and stomach and intestine, drop
The fluctuation of low blood concentration, avoid drug to the stimulation of gastrointestinal tract, administration hurtless measure, compliance is strong the advantages that, and directly from
Skin surface administration, to the effect in terms of skin care and beauty, becomes apparent.
NADH is the reduction-state of nicotinamide adenine dinucleotide, for the citric acid in glycolysis and cellular respiration
Circulation.There are in each living cells of human body, they react NADH with oxygen, generation energy, and thousands of kinds intracorporal to people
Physiological metabolism reaction all plays a crucial role.How much closely bound up with many diseases the content of NADH is in human body cell,
Such as alzheimer's disease, Parkinson, muscular atrophy.Scientist is the study found that cancer is because intracellular DNA is by carcinogenic
After the attack of substance, by damage without caused by time repairing.NADH can be activated DNA repair enzyme (PARP), fast
Speed repairs the DNA of damage, it is prevented to evolve into cancer.Moreover, NADH or superpower antioxidant, can remove internal freedom
Base prevents the process of cancer.We can supplement NADH by diet for body, but the amount absorbed is very low.NADH is non-
It is often unstable, easily degrade.And cannot be smoothly absorbed after oral NADH because NADH have the characteristics that it is acid nonfast, from
When by human stomach, the influence that will receive gastric acid causes to lose activity the NADH of outside intake, and absorptivity is generally relatively low,
Most of ingredient is just oxidized and degrades before reaching blood, keeps its application limited.NADH can be by skin action pathway to machine
External source is continuously replenished in vivo, the generation with delay skin aging process can be effectively prevented.According to clinical verification with prolonged application table
The effects of bright NADH not only has crease-resistant, nti-freckle to dispel outside the remarkable efficacies such as pigment, and there are also anti-inflammatory, sun-proof, health cares, anti-aging.But
Since stability is poor at normal temperature, biological half-life is short, is easily digested and had the shortcomings that immunogenicity, and it is latent to limit it
It is applying.
Currently, there are many administration modes, such as oral, injection by NADH, but due to the property of drug itself, inevitably
Lead to this disadvantage of frequent drug administration.In order to improve the compliance of patient, while increasing the bioavilability of NADH, and remains constant
Effective blood drug concentration, exploitation can be spaced the long period administration NADH alcohol plastid have great meaning.
Summary of the invention
The technical problems to be solved by the present invention are: the administration problem of above-mentioned mentioned NADH.
In order to solve the above-mentioned technical problem, the invention discloses a kind of compositions, according to weight content meter, the composition
Composition are as follows:
In parts by weight, the composition of the alcohol plastid are as follows:
Further, the particle size range of vesica is 35-85nm in the alcohol plastid.
Further, the composition is in gel, and the gel-type vehicle is carbomer.
In addition, also disclosing a kind of preparation method of composition, specifically comprise the following steps:
Gel-type vehicle is weighed, is sufficiently swollen with distilled water at room temperature;
Moisturizer, preservative, permeation enhancers are added thereto;
It is slowly added to pH adjusting agent under stirring condition and adjusts it to neutrality;
It is sufficiently mixed uniformly up to colorless and transparent Blank gel;
Blank gel is mixed with alcohol plastid, is developed uniformly up to Ethosomal gel composition.
Further, the preparation of the alcohol plastid includes the following steps:
KGM, phosphatide, cholesterol, stabilizer, antioxidant is weighed to be added to the container;
Low-molecular-weight alcohol is added, stirs and makes it completely dissolved;
NADH is added, after mixing, water is added and stirs;
Homogeneous, ultrasonic treatment are carried out again, are filtered up to alcohol plastid filtrate.
Further, in the preparation of the alcohol plastid, low mass molecule alcohol be added is dehydrated alcohol, isopropanol or propylene glycol
One of or several, magnetic agitation, water-bath, whipping temp be 10-40 DEG C, make it completely dissolved.
Further, it in the preparation of the alcohol plastid, is added water to using injection method, in the forming of the alcohol plastid
The total weight 100% of water is meter, and the injection rate of the distilled water is that 2-10% is per minute.
Further, in the preparation of the alcohol plastid, whole grain, homogenizing time 0- are carried out using high speed dispersion homogenizer
20min, homogeneous speed are 0-8000r/min.
Further, in the preparation of the alcohol plastid, the time of the ultrasonic treatment is 0-45min;The filtering uses
0.22 μm or 0.45 μm of filter membrane progress.
Finally, also disclosing a kind of application of composition, the composition can be used among cosmetics and skincare product.
KGM modified phospholipid that the present invention obtains carries the transdermal alcohol plastid of NADH, be a kind of novel form is mostly ball-type or close
Spherical multilamellar vesicles structure has thermodynamics more stable, and partial size is smaller, and encapsulation rate is high, have percutaneous abilities faster, it is stronger,
The features such as skin-tolerant can be good, and dosage is less, reduces the incidence of adverse reaction, improves safety.And utilize the alcohol matter
The preparation process that body prepares gel skin care item is simple, NADH alcohol plastid can be obtained using stirring, homogeneous, ultrasound, filtering, by alcohol
Plastid and penetrating agent are uniformly mixed with the gel-type vehicle being swollen again after mixing can obtain Ethosomal gel.
Detailed description of the invention
Concrete scheme of the invention is described in detail with reference to the accompanying drawing
Fig. 1 is the TEM image of vesica in alcohol plastid;
Fig. 2 is the histogram of particle size distribution of vesica in alcohol plastid;
Fig. 3 is the grading curve figure of vesica in alcohol plastid;
Fig. 4 is the vitro cumulative release profiles of alcohol plastid transdermal experiment;
Fig. 5 is the dermal penetration rate release profiles of alcohol plastid.
Specific embodiment
To explain the technical content, the achieved purpose and the effect of the present invention in detail, below in conjunction with embodiment and cooperate attached
Figure is explained in detail.
Embodiment 1
The preparation of alcohol plastid:
The lecithin of precise, cholesterol, vitamin E, QKGM, 4%wtPEG-4000 solution are sequentially added into taper
In bottle, dehydrated alcohol is added into conical flask and carries out magnetic agitation, stirring in water bath temperature is 37 DEG C, is made it completely dissolved.Sufficiently
After dissolution, NADH is added thereto, after mixing, water is added using injection method and is distilled into the forming of the alcohol plastid
The total weight 100% of water be meter, the injection rate of the distilled water is 10% minute.Gained mixed solution is stirred into 60min,
Above-mentioned solution is subjected to high speed dispersion homogenizer and carries out whole grain, homogenizing time 15min, homogeneous speed is 8000r/min, will be equal
Solution after matter carries out ultrasound procedure, ultrasonic time 20min, finally with 0.22 μm or 0.45 μm of membrane filtration to get to alcohol
Plastid filtrate.
Embodiment 2
The preparation of alcohol plastid:
The lecithin of precise, cholesterol, vitamin E, QKGM are sequentially added in conical flask, are added into conical flask
Dehydrated alcohol carries out magnetic agitation, and whipping temp is 25 DEG C, makes it completely dissolved.After completely dissolution, NADH is added thereto, mixes
After closing uniformly, distilled water is added using injection method, is to count with the total weight 100% of the water in the forming of the alcohol plastid, institute
The injection rate for stating distilled water is 10% minute.Gained mixed solution is stirred into 60min, it is equal that above-mentioned solution is carried out high speed dispersion
Matter machine carries out whole grain, homogenizing time 20min, and homogeneous speed is 6000r/min, and the solution after homogeneous is carried out ultrasound procedure,
Ultrasonic time is 20min, finally with 0.45 μ membrane filtration to get arrive alcohol plastid filtrate.
Embodiment 3
The preparation of NADH Ethosomal gel composition
Weigh 1g carbomer gel matrix, be sufficiently swollen with 15g distilled water under room temperature, by 1.5:1 (triethanolamine:
Carbomer: w/w) pH adjusting agent triethanolamine is added dropwise, carbomer gel matrix is obtained after mixing evenly, and ethyl alcohol is added, and (ethyl alcohol contains
Measure identical as ethanol content in alcohol plastid) and moisturizer, preservative, permeation enhancers are added, three second are slowly added under stirring condition
Hydramine adjusts it to neutrality, is sufficiently mixed uniformly up to colorless and transparent Blank gel.By the weight such as NADH alcohol plastid and Blank gel
Part mixing is measured to develop uniformly to get fine and smooth flaxen NADH Ethosomal gel composition.
Experimental example
1, images of transmissive electron microscope test is carried out to alcohol plastid, test results are shown in figure 1, and it will be seen from figure 1 that alcohol
Plastid is formed with the spherical vesica to differ in size.
2, alcohol plastid vesica partial size is tested, test result is as shown in Figure 2 and Figure 3, of the invention according to attached drawing
The average grain diameter of alcohol plastid vesica is 57.1nm, and most of vesica particle diameter distribution is within the scope of 35-85nm.
3, the transdermal test of rats in vitro is carried out, vitro cumulative release profiles as shown in Figure 4 are obtained, and adds up within 24 hours to release
It is unconventional and unrestrained to 30%.And dermal penetration rate release profiles as shown in Figure 5, meet transdermal kinetic theory, osmotic engine
Learning equation is Q=59.34t-20.91 wherein steady-state permeation rate Js=59.34 μ gxh-1·cm-2.By to rats in vitro
It is transdermal research shows that prepared NADH Ethosomal gel preparation of the invention has certain controlled-release function, NADH is steady in for 24 hours
State percutaneous rate is 1331.24 μ g/cm2, accumulation transmitance is 28.6%.
The above description is only an embodiment of the present invention, is not intended to limit the scope of the invention, all to utilize this hair
Equivalent process transformation made by bright specification and accompanying drawing content is applied directly or indirectly in other relevant technical fields,
Similarly it is included within the scope of the present invention.
Claims (10)
1. a kind of composition, which is characterized in that according to weight content meter, the composition of the composition are as follows:
In parts by weight, the composition of the alcohol plastid are as follows:
2. composition as described in claim 1, it is characterised in that: the particle size range of vesica is 35-85nm in the alcohol plastid.
3. composition as described in claim 1, it is characterised in that: the composition is in gel, and the gel-type vehicle is card
Wave nurse.
4. a kind of preparation method of the composition as described in claim any one of 1-3, which comprises the steps of:
Gel-type vehicle is weighed, is sufficiently swollen with distilled water at room temperature;
Moisturizer, preservative, permeation enhancers are added thereto;
It is slowly added to pH adjusting agent under stirring condition and adjusts it to neutrality;
It is sufficiently mixed uniformly up to colorless and transparent Blank gel;
Blank gel is mixed with alcohol plastid, is developed uniformly up to Ethosomal gel composition.
5. the preparation method of composition as claimed in claim 4, which is characterized in that the preparation of the alcohol plastid includes following step
It is rapid:
KGM, phosphatide, cholesterol, stabilizer, antioxidant is weighed to be added to the container;
Low-molecular-weight alcohol is added, stirs and makes it completely dissolved;
NADH is added, after mixing, water is added and stirs;
Homogeneous, ultrasonic treatment are carried out again, are filtered up to alcohol plastid filtrate.
6. the preparation method of composition as claimed in claim 5, it is characterised in that: in the preparation of the alcohol plastid, be added low
Molecule alcohol is one or more of dehydrated alcohol, isopropanol or propylene glycol, magnetic agitation, water-bath, whipping temp 10-40
DEG C, it makes it completely dissolved.
7. the preparation method of composition as claimed in claim 5, it is characterised in that: in the preparation of the alcohol plastid, using injection
Method adds water to, and is to count with the total weight 100% of the water in the forming of the alcohol plastid, and the injection rate of the distilled water is 2-
10% per minute.
8. the preparation method of composition as claimed in claim 5, it is characterised in that: in the preparation of the alcohol plastid, using high speed
Homogeneous dispersion machine carries out whole grain, homogenizing time 0-20min, and homogeneous speed is 0-8000r/min.
9. the preparation method of composition as claimed in claim 5, it is characterised in that: in the preparation of the alcohol plastid, the ultrasound
The time of processing is 0-45min;The filtering is carried out using 0.22 μm or 0.45 μm of filter membrane.
10. the application of composition as described in any one of claims 1-3, it is characterised in that: the composition is used for beauty
Skin care item.
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Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
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US20210338594A1 (en) * | 2018-12-07 | 2021-11-04 | Binotec Co., Ltd. | Nano-lipid carrier for encapsulation of bioactive material, and method for producing same |
Citations (3)
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CN102552147A (en) * | 2011-02-11 | 2012-07-11 | 舒泰神(北京)生物制药股份有限公司 | Bullatacin ethosome gel and preparation method thereof |
CN102579323A (en) * | 2011-02-21 | 2012-07-18 | 舒泰神(北京)生物制药股份有限公司 | Paclitaxel ethosome gel and preparation method thereof |
CN106011163A (en) * | 2016-05-19 | 2016-10-12 | 武汉华美生物工程有限公司 | Method for cell-free expression of signal protein and expression system |
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2018
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Patent Citations (3)
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CN102552147A (en) * | 2011-02-11 | 2012-07-11 | 舒泰神(北京)生物制药股份有限公司 | Bullatacin ethosome gel and preparation method thereof |
CN102579323A (en) * | 2011-02-21 | 2012-07-18 | 舒泰神(北京)生物制药股份有限公司 | Paclitaxel ethosome gel and preparation method thereof |
CN106011163A (en) * | 2016-05-19 | 2016-10-12 | 武汉华美生物工程有限公司 | Method for cell-free expression of signal protein and expression system |
Non-Patent Citations (1)
Title |
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张姗姗等: ""NADH和NADPH代谢和功能的研究进展"", 《第二军医大学学报》 * |
Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US20210338594A1 (en) * | 2018-12-07 | 2021-11-04 | Binotec Co., Ltd. | Nano-lipid carrier for encapsulation of bioactive material, and method for producing same |
US11826474B2 (en) * | 2018-12-07 | 2023-11-28 | Binotec Co., Ltd. | Nano-lipid carrier for encapsulation of bioactive material, and method for producing same |
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Application publication date: 20181207 |