CN108830037A - The analysis of the hyaluronic acid transdermal absorption factor of different dosage forms and compare - Google Patents
The analysis of the hyaluronic acid transdermal absorption factor of different dosage forms and compare Download PDFInfo
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- CN108830037A CN108830037A CN201810666812.8A CN201810666812A CN108830037A CN 108830037 A CN108830037 A CN 108830037A CN 201810666812 A CN201810666812 A CN 201810666812A CN 108830037 A CN108830037 A CN 108830037A
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- hyaluronic acid
- permeation rate
- skin permeation
- liposome
- azone
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Abstract
Hyaluronic acid (HA) is widely used in the multiple fields such as ophthalmology, surgery, shaping and beauty, organizational project and regenerative medicine.HA molecular weight is larger, cannot penetrate the cuticula of skin surface, so the skin permeation rate of research HA dosage form is an important job.The present invention is analyzed and has been compared to HA skin permeation rate, and different dosage forms HA skin permeation rate can provide experimental method and reference for the selection of relevant industries raw material.The present invention relates to the researchs of the transdermal test in vitro rate of different dosage forms HA：Uncrosslinked HA is 20%；Non- homogeneous HA 10%；Six HA 10% of homogeneous；Partial size 50nmHA liposome 15%；Partial size 82nmHA liposome 5%.Penetration promoter screening and condition optimizing are as the result is shown：HA+9% azone skin permeation rate is higher.Skin permeation rate：Uncrosslinked HA 0.22%, liposome HA 2.64%；Uncrosslinked HA+9% azone 0.35%, liposome HA+9% azone 1.26%.
Description
Technical field
The present invention relates to the Transdermal Absorption situation analysis of different dosage forms hyaluronic acid and compare.
Background technique
Hyaluronic acid (hyaluronic acid, HA) is a kind of linear natural macromolecular polysaccharide, is the master of extracellular matrix
Component part is wanted, is widely present in the tissue such as skin, the vitreous humor of eyeball and synovium of joint liquid.HA is good natural guarantor
The wet factor has the characteristics that good biocompatibility, nonantigenic, viscoplasticity and degradation are non-toxic, therefore is widely used in eye
The multiple fields such as section, surgery, treatment joint, shaping and beauty, wound repair, organizational project.
In practical applications, since HA relative molecular mass is larger, the cuticula of skin surface cannot be penetrated.Liposome is
By drug encapsulation in the miniature vesicular body formed in lipoids bilayer, there is non-immunogenicity, nontoxic, easy realization to target
The features such as property.Using liposome as the drug of carrier or other functional components easily enter cuticula, are formed in epidermis and intradermal
Drug-reservoir, the sustainable performance effect of drug have become the research hotspot of dermatosis treating medicine treatment and cosmetics.Liposome pair
Skin has excellent moisture-keeping function, and the liposome for especially having wrapped up moisturizing materials such as HA etc. is more excellent moisture retention substance.
The principle of the present invention：Relationship between the HA of different dosage forms and skin absorption is different, leads to the journey being absorbed by the skin
Spend different, the present invention analyzes and compares to the transdermal situation of different dosage forms HA.Wherein, the lipoid and cutin of liposome
The lipid interaction of layer, increases the mobility of skin lipid, keeps cuticula wet, and aquation is reinforced, and makes between horn cell
Structure change, to promote the transmission of drug.
Application of the invention：The analysis result of the HA Transdermal absorption of different dosage forms can be drug, cosmetics, biomaterial etc.
The selection of industry raw material provides laboratory reference.
Summary of the invention
1. different dosage forms HA percutaneous penetration：Skin defeathering after rat was put to death in 6-8 weeks, removes skin, removes fat deposit,
Physiological saline rinsing, sets in 4 DEG C of physiological saline and saves, and blots skin surface physiological saline with filter paper when use.It will be processed
Rat skin is clipped between supply chamber (R1) and miniature reception cell (R2), and keratoderma is towards supply chamber.
2. it is separately added into the HA of the various dosage forms of 2mL in supply chamber, 35 DEG C of water bath with thermostatic control.Detection receives in cell thoroughly after 4h
The HA concentration crossed, and calculate skin permeation rate.
3. calculation method 1 (volume calculating)：Skin permeation rate (%)=R1 (total volume-residual volume)/R1 (total volume) ×
100；
Calculation method 2 (concentration calculation)：Skin permeation rate (%)=(the rear HA concentration × volume of transmission)/(the preceding HA concentration of transmission ×
Volume) × 100.
Specific embodiment
1. the preparation of different dosage forms HA and the foundation of standard curve
1.1 uncrosslinked HA solution：Cosmetics-stage hyaluronic acid is weighed, appropriate distilled water is added, 10mg/mL is configured to and does not hand over
Join HA solution.
The HA solution of 1.2 non-homogeneous：The hyaluronic acid of crosslinking is taken to be configured to 10mg/mL solution.
The HA solution of 1.3 homogeneous six times：Take HA solution high pressure homogenizer homogeneous six times repeatedly of the non-homogeneous of 10mg/mL.
1.4 liposome HA solution：Following reagent is weighed in beaker：4.0g phosphatide, 0.8g Tween 80,0.8g cholesterol,
20g ethyl alcohol, stirs evenly.Take HA solution in a round bottom flask, water-bath is preheated to 50 DEG C, by 5 milliliters of syringes of phospholipid solution
(No. 7 syringe needles) at the uniform velocity injects in HA solution, stirring, until eliminate ethyl alcohol in solution, uses high pressure homogenizer homogeneous rouge repeatedly
Plastid suspension, and detect liposomal particle size.
The HA solution of 1.5 different dosage forms establishes standard curve respectively.
2. building the receiving chamber of miniature Transdermal absorption instrument diffusion cell
3. different dosage forms HA percutaneous penetration
Skin defeathering after rat was put to death in 6-8 weeks, removes skin, removes fat deposit, and 4 DEG C of physiology salts are set in physiological saline rinsing
It is saved in water, blots skin surface physiological saline with filter paper when use.By processed rat skin be clipped in supply chamber (R1) and
It receives between cell (R2), keratoderma is towards supply chamber.
It is separately added into the HA of 2mL different dosage forms in supply chamber, 35 DEG C of water bath with thermostatic control.
After 4h, the HA concentration (be collected in and receive in cell) of transmission is detected, and calculates transmitance.
Calculation method 1 (volume calculating)：Skin permeation rate (%)=R1 (total volume-residual volume)/R1 (total volume) × 100；
Calculation method 2 (concentration calculation)：Skin permeation rate (%)=(the rear HA concentration × volume of transmission)/(the preceding HA concentration of transmission ×
Volume) × 100.
1. percutaneous penetration of table (screening of HA dosage form)
The HA liposome transdermal effect that uncrosslinked HA and partial size are 50.7nm is preferable, considers to reinforce transdermal effect using penetration promoter
Fruit.
2. percutaneous penetration of table (penetration promoter screening)
It is better than 50% and 2% that 10% ethyl alcohol helps effects, but ethyl alcohol helps the effect unobvious in general, examines
Consider other penetration promoters.
The skin permeation rate of concentration calculation more quantifies, and the transdermal effect ratio of HA+ penetration promoter (9% azone) is passed through without penetration promoter and skin
Azone is handled good, and the skin permeation rate of liposome is much higher than uncrosslinked HA, and the mouse skin of experiment does not need pretreatment and (uses in advance
Penetration promoter impregnates).
The comparison of the uncrosslinked HA of table 3. and liposome HA D (i50=50.7) transdermal test in vitro result
Liposome HA skin permeation rate is much higher than uncrosslinked HA skin permeation rate, and uncrosslinked HA skin permeation rate is 0.224 ± 0.019%
(mean ± STD), liposome HA skin permeation rate are 2.64 ± 0.721% (mean ± STD)；The case where containing 9% azone (penetration promoter)
Under, uncrosslinked HA skin permeation rate is 0.353 ± 0.027% (mean ± STD), and liposome HA skin permeation rate is 1.258 ± 0.077%
(mean±STD)。
Claims (7)
1. relating to the Transdermal Absorption situation of different dosage forms hyaluronic acid.
2. percutaneous penetration (screening of several hyaluronic acid dosage form) is the result shows that transdermal absorption factor is：Uncrosslinked hyaluronic acid
(20%)；Non- homogeneous clear matter is sour (10%)；Six hyaluronic acids (10%) of homogeneous；Partial size is the hyaluronic acid lipid of 50.7nm
Body (15%)；Partial size is the hyaluronic acid liposome (5%) of 82.4nm.
3. percutaneous penetration (penetration promoter screening) is as the result is shown：9% azone is obvious as penetration promoter effect；10% ethyl alcohol helps
Effects are better than 50% and 2%, but ethyl alcohol helps the effect less than 9% azone in general.
4. the analysis of transdermal condition optimizing the result shows that：Hyaluronic acid+penetration promoter (9% azone) skin permeation rate than other conditions (such as
Penetration promoter is not added, 2%, 10%, 50% ethyl alcohol makees penetration promoter) it is good；The mouse skin of experiment does not need pretreatment (in advance with helping
Saturating agent is impregnated).
5. calculation method 1 (volume calculating)：Skin permeation rate (%)=supply chamber (total volume-residual volume)/supply chamber (total volume)
×100。
6. calculation method 2 (concentration calculation)：Skin permeation rate (%)=(penetrating rear hyaluronic acid concentration × volume)/(through preceding transparent
Matter acid concentration × volume) × 100.
7. the skin permeation rate of liposome hyaluronic acid is approximately higher than 10 times of uncrosslinked hyaluronic acid：Uncrosslinked hyaluronic acid skin permeation rate is
0.224 ± 0.019% (mean ± STD), liposome hyaluronic acid skin permeation rate are 2.64 ± 0.721% (mean ± STD)；Contain
In the case where 9% azone (penetration promoter), uncrosslinked hyaluronic acid skin permeation rate is 0.353 ± 0.027% (mean ± STD), lipid
Body hyaluronic acid skin permeation rate is 1.258 ± 0.077% (mean ± STD).
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Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101296691A (en) * | 2005-08-05 | 2008-10-29 | 努沃研究公司 | Transdermal drug delivery formulation |
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2018
- 2018-06-26 CN CN201810666812.8A patent/CN108830037A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101296691A (en) * | 2005-08-05 | 2008-10-29 | 努沃研究公司 | Transdermal drug delivery formulation |
Non-Patent Citations (1)
| Title |
|---|
| 高峰等: "《药剂学实验》", 31 March 2015, 华东理工大学出版社 * |
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