CN106236596A - A kind of nanoscale solid state lipid drug-loading system and preparation method thereof - Google Patents
A kind of nanoscale solid state lipid drug-loading system and preparation method thereof Download PDFInfo
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Abstract
The present invention provides a kind of nanoscale solid state lipid drug-loading system, and this drug-loading system is to mix as raw material liquid fatty and solid lipid to prepare a kind of drug-loading system being embedded with 4 n-butyl resorcinols;Especially, this drug-loading system is that a kind of oil is wrapped in fat and is wrapped in the composite nano lipid drug-loading system of water (O/F/W), has high embedding rate, high drug load, high stability, hypotoxicity and good drug release characteristics;The present invention also provides for the application that drug-loading system is applied to prepare the formula of cosmetics, contributes to skin whitening, removes skin dark stain, freckle and suppression melanin generation.
Description
Technical field
The invention belongs to chemical field, particularly relate to a kind of nanoscale solid state fat embedding 4-n-n-butyl resorcinol
Matter drug-loading system.
Background technology
4-n-n-butyl resorcinol (1,3-Dihydroxy-4-n-butylbenzene, i.e. Lucin)
It is effective skin lightener, is commonly called as Kopcinol.Owing to Kopcinol has antagonism chloasma and effect of anti-saccharifying, because of
This is for H2O2The DNA damage of induction has the strongest protective effect.Furthermore, on the premise of causing any cytotoxicity,
Kopcinol has more suppression effect of tyrosinase activity, and also can suppress the synthesis of tryrosinase.But, due to
Kopcinol can absorb ultraviolet light, and therefore its many effect being had (such as whitening) can reduce because of the effect of light.This
Outward, the Lucin of high dose also has stimulation for skin.
Not yet it is related to the report of the drug-loading system of 4-n-n-butyl resorcinol embedding at present.The most how to prepare bag
The drug-loading system burying 4-n-n-butyl resorcinol is the task of top priority, and wherein the carrier of drug-loading system is chosen as key problem in technology.
Owing to the basic recipe of drug-loading system is wax kind, oil kind, interfacial agent kind and concentration;But, due to
Commercially available wax, oil, interfacial agent of a great variety, should use which kind of wax, oil, interfacial agent kind and concentration is important pass
Key, which kind of wax, oil can constitute with the formula combination of interfacial agent and possesses the lipid carrier of high embedding rate and high stability just
The present invention has been become to desire most ardently problem and the technique direction of solution.Test the most hard through present inventor, finally researched and developed
A kind of nanoscale solid state lipid drug-loading system of the present invention.
Summary of the invention
Finding in present inventor's research, Kopcinol is not only soluble in organic solvent, can be dissolved among oils and fats yet, because of
This, a kind of nanoscale solid state lipid drug-loading system is just born, and it can be used for embedding Kopcinol (4-n-normal-butyl isophthalic two
Phenol).
Described drug-loading system can form a kind of oil and be wrapped in the ideal structure that fat is wrapped in the drug-loading system of water (O/F/W).This
Bright proposed nanoscale solid state lipid drug-loading system is that a kind of oil is wrapped in fat and is wrapped in the composite nano lipid of water (O/F/W) and carries
Body, its ideal structure comprises the oil droplet (liquid fatty substance) of innermost layer, the wax (Solid lipid) of embedding oil droplet and embedding wax
Water.The composite nano lipid carrier of the present invention is primarily adapted for use in embedding active substance, particularly relates to have skin to have function people
The Kopcinol of property effect (have another name called for 4-n-n-butyl resorcinol, 1,3-Dihydroxy-4-n-butylbenzene).
In order to solve above-mentioned technical problem, the invention provides a kind of nanoscale solid state lipid drug-loading system, by active drug
Thing, liquid fatty substance, Solid lipid, polyhydric alcohol, phospholipid, interfacial agent and water composition, wherein, according to mass fraction, described work
Property medicine is 2%-5%, and described liquid fatty substance is 8%-14%, and described Solid lipid is 6%-12%, and described polyhydric alcohol is
1%-3%, described phospholipid is 0.5%-1%, and described interfacial agent is 8%-14%, and remaining is water, described drug-loading system
Particle diameter is 110nm-6040nm.
Described active medicine preferred 4-n-n-butyl resorcinol, mass fraction is 3%.
This drug-loading system is that a kind of oil is wrapped in fat and is wrapped in the drug-loading system of water (O/F/W), has high embedding rate, high medicine carrying
Amount, high stability, hypotoxicity and good drug release characteristics.Further, O/F/W fat provided by the present invention is utilized
Matter carrier embedding drug-loading system obtained by 4-n-n-butyl resorcinol, it is possible to as a kind of functional benefiting human body skin
Skin care products, contributes to skin whitening, removes the pigementation such as skin dark stain, freckle and suppress melanic generation.
Further, inventor carries out organizing experiment more and comparing related experiment result, thus obtains various optimal preparation ginseng
Number, has the nanoscale solid state lipid drug-loading system of high embedding rate and high stability with preparation.As shown in table 1 below, experiment is first
The one-tenth listing nanoscale solid state lipid drug-loading system is grouped into
The composition of table 1 nanoscale solid state lipid drug-loading system
Then, it is most suitable for preparing the oil component of described drug-loading system, wax composition and interfacial agent to determine, invention
Several conventional oil, wax and interfacial agent are set as the Factors of experiment by people, and arrangement is listed among lower list 2.Table 2
Described in Poloxamer 188 be PLURONICS F87,ATO 888 is Glyceryl Behenate,For caprylic/capric triglyceride, Tween 80 is the Tween-80 being commonly called as,900K refers to
Glyceryl monostearate (Glycerol Monostearate).
Table 2 nanoscale solid state lipid drug-loading system
Further, we obtain 16 kinds of nanoscale solid state according to the Factors of table 24 groups of different conditional combinations of arranging in pairs or groups again
The sample of lipid drug-loading system, and these 16 kinds of samples are arranged and in table 3.
The synthesis condition of table 3 drug-loading system
The drug-loading system of embedding Lucin (Kopcinol) is stored under room temperature (25 DEG C) and lasts 60 days,
And by the mean diameter data compilation of the 1st day to the 60th day among lower list 4.By table 4, it appeared that 16 kinds of samples deposit 60
After it, mean diameter system is between 117.2nm to 4843nm, and the average coefficient of dispersion, about between 0.23-1, belongs to moderate dispersion
System and polydisperse system it.
The particle diameter distribution of table 4 drug-loading system
Then, phase boundary potential analysis is carried out for 16 kinds of samples, data compilation under be classified as table 5.The measurement of phase boundary potential
The physical stability of lipid carrier can be assessed, generally belong to stable shape when phase boundary potential | 30 | mV this colloid indicated above that exists
State, represents that its particle accumulation situation is relatively low.Relatively, when phase boundary potential exists, | 15 | mV-| 30 | are between mV, represent that this colloid body is
There is the possibility of cohesion.Additionally, when phase boundary potential is higher than | 60 | more than mV, and this colloid has high stability.
By table 5, it appeared that the distribution of the phase boundary potential of 16 kinds of samples is between | 25.1 | mV extremely | 70.9 | between mV;And
And, present inventor finds the most in an experiment, and the example interface current potential of this drug-loading system is within the 1st day, to start the highest in storage
Being higher than | 60 | mV in | 30 | mV, the even phase boundary potential of some sample, it is stable that this represents that the colloid of this drug-loading system is belonging to
State.Further, along with the increase (to the 60th day) of resting period, the phase boundary potential of each sample all maintain stable or high surely
State qualitatively.
The phase boundary potential of each sample of table 5 drug-loading system
It is then used by differential scanning calorimeter (Differential scanning calorimetry, DSC) to 16 kinds of samples
Product carry out the analysis of degree of crystallinity, and correlation analysis data compilation is table 6.In table 6 it appeared that the degree of crystallinity of 16 kinds of samples about
Between 0.7% to 36.5%;Additionally, learn that by table 6 16 kinds of samples have the active matter medicine carrying energy of 63.5%-99.3%
Power, and wherein to use the Cera Flava drug-loading system as Solid lipid can have the Drug loading capacity of maximum, there are about 90.0%-
The Drug loading capacity of 99.3%.It addition, to use the palm wax drug-loading system as Solid lipid can have medium Drug loading capacity, and
To use ATO888 or the spermaceti lipid carrier as Solid lipid can have the Drug loading capacity of minimum.
The degree of crystallinity of table 6 drug-loading system each sample
After confirming degree of crystallinity and the Drug loading capacity of 16 kinds of samples, then with ultraviolet light/visible spectrometer to 16
Plant sample and carry out the analysis of embedding rate, and correlation analysis data compilation is in lower list 7.As shown in table 7,16 kinds of drug-loading systems
The embedding rate system of sample, between 90.15%-92.03%, belongs to the system of high embedding rate, and the embedding rate of individual samples is also
Without significant difference.
In order to how verify drug-loading system embedding Lucin effect, we use high-performance liquid chromatograph to enter
The analysis of row embedding rate.Respectively with concentration 1,10,25,50,100ppm, 300ppm produce detection curve, R2It is 0.999, table
Show that its calibration curve is to be referred to.The straight line returning gained is formula (1), and high-performance liquid chromatograph detects the area of sample,
Try to achieve out sample area and bring the X value of calibration curve into, obtain its concentration, then carry out the calculating of embedding rate with formula (1).Its embedding rate value
Between 90-92%, represent that each group of embedding rate change is little, i.e. operating condition is limited on the impact of embedding rate.Additionally, result is also
The display present invention carries out embedding and has high embedding characteristic Lucin.
High-performance liquid chromatograph is analyzed
Detector: ultraviolet detector, detects wavelength: 280nm, tubing string: ODS (C18) post 4.6nm*25cm, 5um
C18, flow phase: methanol: deionized water=80: 20+0.1% glacial acetic acid, injection volume: 20 μ l, flow velocity: 0.42ml/
min。
The embedding rate of table 7 drug-loading system
Further, in order to confirm the optimum grain-diameter of this drug-loading system, optimal phase boundary potential and degree of crystallinity, therefore to this
The sample of drug-loading system has carried out S/N ratio (signal noise ratio) Effects of Factors effect analysis, and analysis result system arranges in following
Among table 8, table 9 and table 10.Wherein, table 8 is the S/N specific factor influential effect analytical table of particle size parameters, and table 9 is joined for phase boundary potential
The S/N specific factor influential effect analytical table of number, and the S/N specific factor influential effect analytical table that table 10 is degree of crystallinity
Table 8 particle size parameters S/N specific factor influential effect analytical table
Table 9 phase boundary potential parameter S/N specific factor influential effect analytical table
Table 10 degree of crystallinity S/N specific factor influential effect analytical table
After completing various S/N specific factor influential effect analytical table, apply for just particle diameter, phase boundary potential and degree of crystallinity
The figure of merit arranges among lower list 11.
Table 11
Further, by the relevant experimental data of the S/N specific factor influential effect analysis of table 8-11, applicant can obtain
To following experimental result:
(1) through field mouth method analyze after, be appreciated that impact embedding Kopcinol drug-loading system particle size parameters condition because of
The importance of son obtains sequencing and is: C (component ratio) > B (wax kind) > D (interfacial agent kind) > (interfacial agent is dense for E
Degree) > A (kind of oil);Wherein, refering to table 2 and table 3, optimum operation condition is:B2 (Cera Flava), C3
(oil 12wt%+ wax 8wt%), D3 (Poloxamer 188), E4 (Poloxamer 188 14wt%).
(2) after field mouth method is analyzed, it is appreciated that the bar of the phase boundary potential parameter of impact embedding Kopcinol drug-loading system
The importance of the part factor obtains sequencing: D (interfacial agent kind) > B (wax kind) > E (surfactant concentration) > A (oil
Kind) > C (component ratio);Wherein, refering to table 2 and table 3, optimum operation condition is: A3 (Ribes nigrum L. oil), B2 (Cera Flava), C4
(oil 14wt%+ wax 6wt%), D1 (decyl glucoside), E4 (decyl glucoside 14wt%).
(3) after field mouth method is analyzed, it is appreciated that the condition of the degree of crystallinity parameter of impact embedding Kopcinol drug-loading system
The importance of the factor obtains sequencing: B (wax kind circle) > C (component ratio) > A (oil kind) > E (surfactant concentration) >
D (interfacial agent kind);Wherein, refering to table 2 and table 3, optimum operation condition is: A4 (oily),C1 (oil 8%, wax 12%),E2(10%).
(4) and, by above-mentioned (1), the conclusion of (2) and (3), more can learn further, affect the main of particle diameter
The factor is oil wax ratio, affects the kind that the main factor is interfacial agent of phase boundary potential, and affects degree of crystallinity size
The main factor is the kind of wax.
Present invention also offers a kind of drug-loading system, wherein, described liquid fatty substance is selected from least one compound following:
Hawaii Oleum Glycines, Ribes nigrum L. oil, Miglyol 812N or blueweed oil.
Present invention also offers a kind of drug-loading system, wherein, described Solid lipid is palm wax, Apis cerana Fabricius, behenic acid glycerol
Ester or spermaceti.
Present invention also offers a kind of drug-loading system, wherein, described polyhydric alcohol is pentanediol, and mass fraction is 2%.
Present invention also offers a kind of drug-loading system, wherein, described phospholipid is lecithin, and mass fraction is 0.5%.
Present invention also offers a kind of drug-loading system, wherein, described interfacial agent is selected from least one compound following:
Decyl glucoside, PLURONICS F87, Tween-80 or glyceryl monostearate.
Present invention also offers a kind of drug-loading system, wherein, the interface charge of described drug-loading system is | 25.1 | mV-|
70.9 | mV, degree of crystallinity is 0.7%-36.5%.
Present invention also offers the preparation method of a kind of drug-loading system, wherein, following steps be prepared from: employ height
Pressure homogenizer device, thermal high homogenizer device contains frozen water machine, is mainly used for cooling down high pressure homogenizer, high pressure homogenize
Machine, feed well, the port of export, motor, high-pressure pump, pressurizing valve (first paragraph and second segment pressurizing valve), heater, coil pipe etc..High pressure
Homogenizer makes sectional area in pipe reduce by the shuttle promotion of high-pressure pump to pressurizing valve pressurization, make liquid pass through one the most several
The slit of individual micron, liquid, under unexpected puffing and high speed impact collide dual function, is internally formed the strongest turbulent flow
And vortex pot, fluid also can produce impulsive force and shearing force etc., make particle reach the effect of debulk and homogenizing.
1) opening the cooling water of high pressure homogenizer, the heater opening high pressure homogenizer is heated to 80-90 DEG C;Start high pressure
Homogenizer, in keeping circulation to make machine, line temperature maintains 80-90 DEG C;The amount all medicines of scale respectively, by liquid fatty substance, solid-state
Lipid and active medicine mixing heated at constant temperature, to 80-90 DEG C, obtain oil phase;
2) by water, interfacial agent, polyhydric alcohol and phospholipid mixing heated at constant temperature to 80-90 DEG C, aqueous phase is obtained;
3) by step 1) in oil phase add to step 2) in aqueous phase, constant temperature, in 80-90 DEG C, obtains mixed phase;
4) by step 3) in mixed phase put into high pressure homogenizer and carry out front emulsifying, rotating speed 7000-9000rpm, time 80-
200 seconds, form mixed phase emulsion, it is thus achieved that sample;
5) by step 4) the mixed phase samples of latex that completes of front emulsifying feeds in high pressure homogenizer, waits that air is arranged completely
Remove;
6) after air is got rid of completely, start the program that homogenizes, obtain described drug-loading system.
Wherein temperature the most preferably 85 DEG C, the preferred 8000rpm of rotating speed, preferably 180 seconds time.
So, described above is the clearest, introduce the drug-loading system of the present invention in detail;Further, it is appreciated that via above-mentioned
The present invention has with purgation advantage:
(1) in the present invention, mainly liquid fatty and solid lipid are mixed and be just embedded with 4-n-as raw material to prepare
A kind of drug-loading system of butyl resorcinol;Especially, this drug-loading system is that a kind of oil is wrapped in fat and is wrapped in the medicine carrying of water (O/F/W)
System, has high embedding rate, high drug load, high stability, hypotoxicity and good drug release characteristics.
(2) doctor utilizing O/F/W lipid carrier embedding 4-n-n-butyl resorcinol provided by the present invention obtained is beautiful
Purposes compositions, it is possible to as benefiting a kind of functional skin care products of human body skin, contributes to skin whitening, removes skin dark stain, passeris montani saturati
Pigementations such as speckle and suppress melanic generation.
The nanoscale solid state lipid drug-loading system of the application commercially has no report.
Above-mentioned drug-loading system is prepared as cosmetics such as skin whitener, had already obtained good using effect, and had
Well safety and stability.
Detailed description of the invention
Experimental example is used for further illustrating the present invention but is not limited to the present invention below.All real based on foregoing of the present invention institute
Existing technology belongs to the scope of the invention.
Embodiment 1
1) according to preparation method involved in summary of the invention, i.e. following methods
1) opening the cooling water of high pressure homogenizer, the heater opening high pressure homogenizer is heated to 85 DEG C;Start high pressure equal
Matter machine, in keeping circulation to make machine, line temperature maintains 85 DEG C;The amount all medicines of scale respectively, by liquid fatty substance, Solid lipid
And active medicine mixing heated at constant temperature is to 85 DEG C, obtains oil phase;
2) by water, interfacial agent, polyhydric alcohol and phospholipid mixing heated at constant temperature to 85 DEG C, aqueous phase is obtained;
3) by step 1) in oil phase add to step 2) in aqueous phase, constant temperature, in 85 DEG C, obtains mixed phase;
4) by step 3) in mixed phase put into high pressure homogenizer and carry out front emulsifying, rotating speed 8000rpm, 180 seconds time, formed
Mixed phase emulsion, it is thus achieved that sample;
5) by step 4) the mixed phase samples of latex that completes of front emulsifying feeds in high pressure homogenizer, waits that air is arranged completely
Remove;
6) after air is got rid of completely, start the program that homogenizes, obtain described drug-loading system.
Wherein liquid fatty substance is the Hawaii Oleum Glycines of 8%, and Solid lipid is the palm wax of 12%, and the active medicine of 3% is
4-n-n-butyl resorcinol, the interfacial agent of 8% is decyl glucoside, and the polyhydric alcohol of 2% is pentanediol, 0.5%
Phospholipid is lecithin, and remaining is water, and above mark refers both to mass fraction.Obtain Q1.
Measuring particle diameter, be shown in Table 4Q1 row, phase boundary potential is shown in Table 5Q1, and degree of crystallinity is shown in Table in 6 the 13.7% of Q1, and embedding degree is shown in Table
In 7 the 90.68% of Q1.
Embodiment 2
Preparation method is same as in Example 1,
Wherein liquid fatty substance is the Hawaii Oleum Glycines of 10%, and Solid lipid is the Cera Flava of 10%, and the active medicine of 3% is 4-
N-n-butyl resorcinol, the interfacial agent of 10% is Tween 80, and the polyhydric alcohol of 2% is pentanediol, and the phospholipid of 0.5% is
Lecithin, remaining is water, and above mark refers both to mass fraction.Obtain Q2.
Measuring particle diameter, be shown in Table 4Q2 row, phase boundary potential is shown in Table 5Q2, and degree of crystallinity is shown in Table in 6 the 0.7% of Q2, and embedding degree is shown in Table 7
The 91.94% of middle Q2.
Embodiment 3
Preparation method is same as in Example 1,
Wherein liquid fatty substance is the Hawaii Oleum Glycines of 12%, and Solid lipid is 8%ATO 888,3%
Active medicine is 4-n-n-butyl resorcinol, and the interfacial agent of 12% is Poloxamer 188, and the polyhydric alcohol of 2% is penta
Glycol, the phospholipid of 0.5% is lecithin, and remaining is water, and above mark refers both to mass fraction.Obtain Q3.
Measuring particle diameter, be shown in Table 4Q3 row, phase boundary potential is shown in Table 5Q3, and degree of crystallinity is shown in Table in 6 the 14.4% of Q3, and embedding degree is shown in Table
In 7 the 91.24% of Q3.
Embodiment 4
Preparation method is same as in Example 1,
Wherein liquid fatty substance is the Hawaii Oleum Glycines of 14%, and Solid lipid is the spermaceti of 6%, and the active medicine of 3% is 4-
N-n-butyl resorcinol, the interfacial agent of 14% is900K, the polyhydric alcohol of 2% is pentanediol, the phosphorus of 0.5%
Fat is lecithin, and remaining is water, and above mark refers both to mass fraction.Obtain Q4.
Measuring particle diameter, be shown in Table 4Q4 row, phase boundary potential is shown in Table 5Q4, and degree of crystallinity is shown in Table in 6 the 7.6% of Q4, and embedding degree is shown in Table 7
The 91.84% of middle Q4.
Embodiment 5
Preparation method is same as in Example 1,
Wherein liquid fatty substance is 12%Solid lipid is the Cera Flava of 8%, and the active medicine of 3% is 4-
N-n-butyl resorcinol, the interfacial agent of 14% is Poloxamer 188, and the polyhydric alcohol of 2% is pentanediol, 0.5%
Phospholipid is lecithin, and remaining is water, and above mark refers both to mass fraction.Obtaining Q17, particle diameter is 79.4nm.
Embodiment 6
Preparation method is same as in Example 1,
Wherein liquid fatty substance is the Ribes nigrum L. oil of 14%, and Solid lipid is the Cera Flava of 6%, and the active medicine of 3% is 4-n-
N-butyl resorcinol, the interfacial agent of 14% is decyl glucoside, and the polyhydric alcohol of 2% is pentanediol, the phospholipid of 0.5%
For lecithin, remaining is water, and above mark refers both to mass fraction.Obtain Q18, phase boundary potential-71.8mV.
Embodiment 7
Preparation method is same as in Example 1,
Wherein liquid fatty substance is the blueweed oil of 8%, and Solid lipid is 12%The activity of 3%
Medicine is 4-n-n-butyl resorcinol, and the interfacial agent of 10% is900K, the polyhydric alcohol of 2% is pentanediol,
The phospholipid of 0.5% is lecithin, and remaining is water, and above mark refers both to mass fraction.Obtain Q19, degree of crystallinity 9.7%.
Embodiment 8
According to the preparation method of embodiment 1, prepare the sample of other 12 kinds of drug-loading systems in table 3 respectively,
Measuring particle diameter, be shown in Table corresponding line column data in 4, phase boundary potential is shown in Table 5 corresponding line column data, degree of crystallinity and embedding degree
It is shown in Table 6 and table 7 corresponding line column data respectively.
Claims (10)
1. a nanoscale solid state lipid drug-loading system, by active medicine, liquid fatty substance, Solid lipid, polyhydric alcohol, phospholipid, boundary
Face activating agent and water composition, it is characterised in that according to mass fraction, described active medicine is 2%-5%, and described liquid fatty substance is
8%-14%, described Solid lipid is 6%-12%, and described polyhydric alcohol is 1%-3%, and described phospholipid is 0.5%-1%, described
Interfacial agent is 8%-14%, and remaining is water, and the particle diameter of described drug-loading system is 110nm-6040nm.
2. drug-loading system as claimed in claim 1, it is characterised in that described active medicine is 4-n-n-butyl resorcinol,
Mass fraction is 3%.
3. drug-loading system as claimed in claim 1, it is characterised in that described liquid fatty substance is selected from least one chemical combination following
Thing: Hawaii Oleum Glycines, Ribes nigrum L. oil, Miglyol 812N or blueweed oil.
4. drug-loading system as claimed in claim 1, it is characterised in that described Solid lipid is that palm wax, Apis cerana Fabricius, behenic acid are sweet
Grease or spermaceti.
5. drug-loading system as claimed in claim 1, it is characterised in that described polyhydric alcohol is pentanediol, and mass fraction is 2%.
6. drug-loading system as claimed in claim 1, it is characterised in that described phospholipid is lecithin, and mass fraction is 0.5%.
7. drug-loading system as claimed in claim 1, it is characterised in that described interfacial agent is selected from least one chemical combination following
Thing: decyl glucoside, PLURONICS F87, Tween-80 or glyceryl monostearate.
8. drug-loading system as claimed in claim 1, it is characterised in that the interface charge of described drug-loading system is | 25.1 | mV-|
70.9 | mV, degree of crystallinity is 0.7%-36.5%.
9. the preparation method of drug-loading system described in a claim 1, it is characterised in that be prepared from by following steps:
1) opening the cooling water of high pressure homogenizer, the heater opening high pressure homogenizer is heated to 80-90 DEG C;Start high pressure homogenize
Machine, in keeping circulation to make machine, line temperature maintains 80-90 DEG C;The amount all medicines of scale respectively, by liquid fatty substance, Solid lipid
And active medicine mixing heated at constant temperature is to 80-90 DEG C, obtains oil phase;
2) by water, interfacial agent, polyhydric alcohol and phospholipid mixing heated at constant temperature to 80-90 DEG C, aqueous phase is obtained;
3) by step 1) in oil phase add to step 2) in aqueous phase, constant temperature, in 80-90 DEG C, obtains mixed phase;
4) by step 3) in mixed phase put into high pressure homogenizer and carry out front emulsifying, rotating speed 7000-9000rpm, second time 80-200,
Form mixed phase emulsion, it is thus achieved that sample;
5) by step 4) the mixed phase samples of latex that completes of front emulsifying feeds in high pressure homogenizer, waits that air is got rid of completely;
6) after air is got rid of completely, start the program that homogenizes, obtain described drug-loading system.
10. the purposes that drug-loading system described in claim 1 is applied in the formula of cosmetics.
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Cited By (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN107595655A (en) * | 2017-10-10 | 2018-01-19 | 上海格兰化妆品有限公司 | A kind of salicylic drug-loading system and its preparation method and application |
CN111743799A (en) * | 2020-07-07 | 2020-10-09 | 台湾美联生物科技有限公司 | Nanoscale solid lipid carrier, preparation method thereof and cosmetic containing nanoscale solid lipid carrier |
CN112603869A (en) * | 2021-01-07 | 2021-04-06 | 广州玖睿生物科技有限公司 | Whitening spot-lightening cream and preparation method thereof |
CN115590818A (en) * | 2022-09-09 | 2023-01-13 | 江南大学(Cn) | Thermo-sensitive nano liposome capable of realizing step release of active substances and application thereof |
Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN103070390A (en) * | 2011-10-26 | 2013-05-01 | 丰益(上海)生物技术研发中心有限公司 | Nano-liposome carrier composition and preparation method thereof |
CN103860389A (en) * | 2012-12-17 | 2014-06-18 | 贝侬生化(苏州工业园区)有限公司 | Nanostructured lipid carrier loaded with phenylethyl resorcinol, preparation method thereof and cosmetic containing same |
CN104146883A (en) * | 2014-07-10 | 2014-11-19 | 上海应用技术学院 | Phenylethyl resorcinol-cladded nano-solid lipid carrier and preparation method thereof |
-
2016
- 2016-08-30 CN CN201610781607.7A patent/CN106236596A/en active Pending
Patent Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN103070390A (en) * | 2011-10-26 | 2013-05-01 | 丰益(上海)生物技术研发中心有限公司 | Nano-liposome carrier composition and preparation method thereof |
CN103860389A (en) * | 2012-12-17 | 2014-06-18 | 贝侬生化(苏州工业园区)有限公司 | Nanostructured lipid carrier loaded with phenylethyl resorcinol, preparation method thereof and cosmetic containing same |
CN104146883A (en) * | 2014-07-10 | 2014-11-19 | 上海应用技术学院 | Phenylethyl resorcinol-cladded nano-solid lipid carrier and preparation method thereof |
Non-Patent Citations (2)
Title |
---|
李智轩: "4-正丁基间苯二酚之包埋与分析技术开发", 《台湾博硕士论文》 * |
裘炳毅等: "《现代化妆品科学与技术 下》", 31 March 2016, 中国轻工业出版社 * |
Cited By (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN107595655A (en) * | 2017-10-10 | 2018-01-19 | 上海格兰化妆品有限公司 | A kind of salicylic drug-loading system and its preparation method and application |
CN111743799A (en) * | 2020-07-07 | 2020-10-09 | 台湾美联生物科技有限公司 | Nanoscale solid lipid carrier, preparation method thereof and cosmetic containing nanoscale solid lipid carrier |
CN112603869A (en) * | 2021-01-07 | 2021-04-06 | 广州玖睿生物科技有限公司 | Whitening spot-lightening cream and preparation method thereof |
CN115590818A (en) * | 2022-09-09 | 2023-01-13 | 江南大学(Cn) | Thermo-sensitive nano liposome capable of realizing step release of active substances and application thereof |
CN115590818B (en) * | 2022-09-09 | 2024-05-07 | 江南大学 | Thermosensitive nanoliposome capable of realizing stepped release of active substances and application thereof |
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