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CN113509399A - Chitosamine HCl liposome microcapsule, preparation method thereof and application thereof in removing melanin - Google Patents

Chitosamine HCl liposome microcapsule, preparation method thereof and application thereof in removing melanin Download PDF

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Publication number
CN113509399A
CN113509399A CN202110688558.3A CN202110688558A CN113509399A CN 113509399 A CN113509399 A CN 113509399A CN 202110688558 A CN202110688558 A CN 202110688558A CN 113509399 A CN113509399 A CN 113509399A
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CN
China
Prior art keywords
chitosamine
hcl
phase
liposome
stirring
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Pending
Application number
CN202110688558.3A
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Chinese (zh)
Inventor
林彤
周丹丹
姚尧
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Guangzhou Hengning Biotechnology Co ltd
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Guangzhou Hengning Biotechnology Co ltd
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Priority to CN202110688558.3A priority Critical patent/CN113509399A/en
Publication of CN113509399A publication Critical patent/CN113509399A/en
Pending legal-status Critical Current

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/60Sugars; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/02Cosmetics or similar toiletry preparations characterised by special physical form
    • A61K8/11Encapsulated compositions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/02Cosmetics or similar toiletry preparations characterised by special physical form
    • A61K8/14Liposomes; Vesicles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/55Phosphorus compounds
    • A61K8/553Phospholipids, e.g. lecithin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/63Steroids; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/67Vitamins
    • A61K8/678Tocopherol, i.e. vitamin E
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • A61Q19/02Preparations for care of the skin for chemically bleaching or whitening the skin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/40Chemical, physico-chemical or functional or structural properties of particular ingredients
    • A61K2800/56Compounds, absorbed onto or entrapped into a solid carrier, e.g. encapsulated perfumes, inclusion compounds, sustained release forms

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Birds (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Dermatology (AREA)
  • Medicinal Preparation (AREA)
  • Cosmetics (AREA)

Abstract

The invention discloses a chitosamine HCl liposome microcapsule, a preparation method thereof and application thereof in melanin removal. Chitosamine HCl liposome microcapsule, taking chitosamine HCl as effective component, encapsulating the chitosamine HCl in liposome to form suspension; according to weight percentage, the chitosamine HCl is 0.01-0.20%, the liposome is 0.05-1%, and the rest is aqueous solution. The liposome is prepared by dissolving soybean lecithin, cholesterol and vitamin E in anhydrous alcohol. The chitosamine HCl liposome microcapsule prepared by the invention has small nanocrystallized molecular weight, strong permeability and easy absorption; in addition, the skin-care product can decompose melanocytes when being coated on skin, thereby playing a role in removing melanin, and can be applied to cosmetics and medicines.

Description

Chitosamine HCl liposome microcapsule, preparation method thereof and application thereof in removing melanin
Technical Field
The invention relates to the technical field of cosmetics, in particular to a chitosamine HCl liposome microcapsule, a preparation method thereof and application thereof in melanin removal.
Background
Chitosamine HCl, english name (INCI): gluconamine HCL, alternative name of ingredients: glucosamine HCL. The existing chitosamine HCl mainly has the effects of resisting static electricity and serving as a hair conditioner in cosmetics and skin care products, has a risk coefficient of 1, is relatively safe, can be safely used, generally has no influence on pregnant women, and has no acne-causing property.
The liposome is a hydrophilic vesicle generally composed of phospholipid bilayers, and has the characteristics of improving the stability of encapsulated drugs, promoting the transdermal absorption of the drugs, prolonging the action time of the drugs, having a targeting effect on local disease parts, reducing the toxic and side effects of the drugs and the like. Thus, liposomes have been widely used as drug carriers in pharmaceutical formulations and cosmetic formulations.
However, due to the structural particularity of chitosamine HCl, liposome preparation is difficult, and the prior art does not describe the chitosamine HCl liposome.
Disclosure of Invention
The invention aims to overcome the defects of the prior art and provides a chitosamine HCl liposome microcapsule, a preparation method thereof and application thereof in melanin removal
In order to achieve the purpose, the invention adopts the following technical scheme:
a chitosamine HCl liposome microcapsule takes chitosamine HCl as an effective component, and the chitosamine HCl is wrapped in liposome to form a suspension; according to weight percentage, the chitosamine HCl is 0.01-0.20%, the liposome is 0.05-1%, and the rest is aqueous solution.
Preferably, in the above chitosamine HCl liposome microcapsule, the liposome is prepared by dissolving soybean lecithin, cholesterol and vitamin E in anhydrous alcohol.
The preparation method of the chitosamine HCl liposome microcapsule comprises the following steps:
(1) dissolving soybean lecithin, cholesterol and vitamin E in anhydrous alcohol, stirring to dissolve completely to obtain liposome as phase I; chitosamine HCl as phase II; dissolving disodium hydrogen phosphate, sodium dihydrogen phosphate, disodium EDTA and HL-10 in sterilized water to obtain phase III;
(2) putting the II-phase chitosamine HCl into a high-pressure micro-jet homogenizer and sterilized water for nanocrystallization;
(3) placing phase I in a round bottle, starting the device at 38-40 deg.C, stirring at 50r/min, and vacuum-0.1 mpa; stirring and evaporating the alcohol until no bubbles emerge from the bottle;
(4) putting part of phase III in a beaker, stirring and dissolving uniformly, adding phase I and phase II, and shaking until phase I and phase II are completely dissolved;
(5) pouring the uniformly mixed liquid obtained in the step (4) into a beaker for homogenizing;
(6) pouring the mixed liquid obtained in the step (5) into a round bottle, starting the device at the temperature of 38-40 ℃, stirring at the temperature of 50r/min, and vacuumizing to 0.1mpa until no bubbles exist in the liquid;
(7) pouring the mixed liquid obtained in the step (6) into a beaker, adding all the residual phase III liquid, magnetically stirring and homogenizing;
(8) pouring the mixed liquid obtained in the step (7) into a high-pressure micro-jet homogenizer again, opening the equipment until no bubbles exist in the liquid, and performing nanocrystallization treatment to obtain the chitosamine HCl liposome microcapsule
Compared with the prior art, the invention has the following beneficial effects: the chitosamine HCl liposome microcapsule prepared by the invention has small nanocrystallized molecular weight, strong permeability and easy absorption; in addition, the skin-care product can be coated on skin to decompose melanocytes, thereby playing a role in removing melanin and whitening skin, and can be applied to cosmetics and medicines.
Drawings
FIG. 1 is an original drawing of skin melanin;
FIG. 2 is an exploded view of melanocytes after 2 days of liposome-encapsulated chitosamine HCl exposure;
FIG. 3 is an exploded view of melanocytes after encapsulation of chitosamine HCl with liposomes for 5 d;
FIG. 4 is an exploded view of melanocytes after 7 days of action of liposome-encapsulated chitosamine HCl.
Detailed Description
Example 1: preparation of chitosamine HCl liposome microcapsules:
(1) dissolving soybean lecithin, cholesterol and vitamin E in anhydrous alcohol, stirring to dissolve completely to obtain liposome as phase I; taking 3g of chitosamine HCl as phase II; dissolving disodium hydrogen phosphate, sodium dihydrogen phosphate, disodium EDTA and HL-10 in sterilized water to obtain phase III;
the formula of the phase I is as follows:
soybean lecithin 15g
Cholesterol 2.85g
200ml of absolute alcohol
Vitamin E1.3 g.
The formula of phase III is:
disodium hydrogen phosphate 14.1g
Sodium dihydrogen phosphate 6.65g
EDTA disodium 2g
Sterilized Water 2000g
HL-10 16g。
(2) Putting the II-phase chitosamine HCl into a high-pressure micro-jet homogenizer and sterilized water for nanocrystallization;
(3) placing phase I in a round bottle, starting the device at 38 deg.C, stirring at 50r/min, and vacuum-0.1 mpa; stirring and evaporating the alcohol until no bubbles emerge from the bottle;
(4) putting part of phase III in a beaker, stirring and dissolving uniformly, adding phase I and phase II, and shaking until phase I and phase II are completely dissolved;
(5) pouring the uniformly mixed liquid obtained in the step (4) into a beaker for homogenizing;
(6) pouring the mixed liquid obtained in the step (5) into a round bottle, starting the equipment, stirring at the temperature of 38 ℃, and carrying out vacuum-0.1 mpa until no bubbles exist in the liquid;
(7) pouring the mixed liquid obtained in the step (6) into a beaker, adding all the residual phase III liquid, magnetically stirring and homogenizing;
(8) and (4) pouring the mixed liquid obtained in the step (7) into a high-pressure micro-jet homogenizer again, starting the equipment until no bubbles exist in the liquid, and carrying out nanocrystallization treatment to obtain the chitosamine HCl liposome microcapsule.
Example 2: preparation of chitosamine HCl liposome microcapsules:
(1) dissolving soybean lecithin, cholesterol and vitamin E in anhydrous alcohol, stirring to dissolve completely to obtain liposome as phase I; taking 3g of chitosamine HCl as phase II; dissolving disodium hydrogen phosphate, sodium dihydrogen phosphate, disodium EDTA and HL-10 in sterilized water to obtain phase III;
the formula of the phase I is as follows:
soybean lecithin 17g
Cholesterol 2.95g
200ml of absolute alcohol
Vitamin E2 g.
The formula of phase III is:
disodium hydrogen phosphate 14.8g
7.65g of sodium dihydrogen phosphate
EDTA disodium 3g
Sterilized Water 2000g
HL-10 14g。
(2) Putting the II-phase chitosamine HCl into a high-pressure micro-jet homogenizer and sterilized water for nanocrystallization;
(3) placing phase I in a round bottle, starting the device at 40 deg.C, stirring at 50r/min, and vacuum-0.1 mpa; stirring and evaporating the alcohol until no bubbles emerge from the bottle;
(4) putting part of phase III in a beaker, stirring and dissolving uniformly, adding phase I and phase II, and shaking until phase I and phase II are completely dissolved;
(5) pouring the uniformly mixed liquid obtained in the step (4) into a beaker for homogenizing;
(6) pouring the mixed liquid obtained in the step (5) into a round bottle, starting the equipment, stirring at 40 ℃, and carrying out vacuum-0.1 mpa until no bubbles exist in the liquid;
(7) pouring the mixed liquid obtained in the step (6) into a beaker, adding all the residual phase III liquid, magnetically stirring and homogenizing;
(8) and (4) pouring the mixed liquid obtained in the step (7) into a high-pressure micro-jet homogenizer again, starting the equipment until no bubbles exist in the liquid, and carrying out nanocrystallization treatment to obtain the chitosamine HCl liposome microcapsule.
Example 3 efficacy test
The chitosamine HCl liposome microcapsule obtained in example 1 is applied to cosmetics and is coated on the surface of the skin, and figure 1 is a skin melanin artwork without the coated chitosamine HCl liposome microcapsule; as can be seen from FIGS. 2-4, the skin melanocytes coated with chitosamine HCl liposome microcapsules have a significant decomposition effect on the melanocytes with the lapse of time.

Claims (4)

1. The chitosamine HCl liposome microcapsule is characterized in that the chitosamine HCl is taken as an active ingredient and is wrapped in liposome to form a suspension; according to weight percentage, the chitosamine HCl is 0.01-0.20%, the liposome is 0.05-1%, and the rest is aqueous solution.
2. The chitosamine HCl liposome microcapsule of claim 1, wherein said liposomes are made from soy lecithin, cholesterol and vitamin E dissolved in anhydrous alcohol.
3. The process for the preparation of chitosamine HCl liposome microcapsule according to claim 1, characterized by comprising the steps of:
(1) dissolving soybean lecithin, cholesterol and vitamin E in anhydrous alcohol, stirring to dissolve completely to obtain liposome as phase I; chitosamine HCl as phase II; dissolving disodium hydrogen phosphate, sodium dihydrogen phosphate, disodium EDTA and HL-10 in sterilized water to obtain phase III;
(2) putting the II-phase chitosamine HCl into a high-pressure micro-jet homogenizer and sterilized water for nanocrystallization;
(3) placing phase I in a round bottle, starting the device at 38-40 deg.C, stirring at 50r/min, and vacuum-0.1 mpa; stirring and evaporating the alcohol until no bubbles emerge from the bottle;
(4) putting part of phase III in a beaker, stirring and dissolving uniformly, adding phase I and phase II, and shaking until phase I and phase II are completely dissolved;
(5) pouring the uniformly mixed liquid obtained in the step (4) into a beaker for homogenizing;
(6) pouring the mixed liquid obtained in the step (5) into a round bottle, starting the device at the temperature of 38-40 ℃, stirring at the temperature of 50r/min, and vacuumizing to 0.1mpa until no bubbles exist in the liquid;
(7) pouring the mixed liquid obtained in the step (6) into a beaker, adding all the residual phase III liquid, magnetically stirring and homogenizing;
(8) and (4) pouring the mixed liquid obtained in the step (7) into a high-pressure micro-jet homogenizer again, starting the equipment until no bubbles exist in the liquid, and carrying out nanocrystallization treatment to obtain the chitosamine HCl liposome microcapsule.
4. The use of chitosamine HCl liposome microcapsules of claim 1 for the preparation of melanin-removing cosmetics.
CN202110688558.3A 2021-06-22 2021-06-22 Chitosamine HCl liposome microcapsule, preparation method thereof and application thereof in removing melanin Pending CN113509399A (en)

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CN202110688558.3A CN113509399A (en) 2021-06-22 2021-06-22 Chitosamine HCl liposome microcapsule, preparation method thereof and application thereof in removing melanin

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Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20060018851A1 (en) * 2004-06-28 2006-01-26 Procyte Corporation Methods and compositions for preventing and treating hyperpigmentation of skin
CN1901920A (en) * 2003-11-21 2007-01-24 雀巢技术公司 Food composition comprising glucosamine
CN105581978A (en) * 2014-10-20 2016-05-18 湖南师范大学 Glucosamine derivative cation liposome nanoparticle preparation method
CN110652658A (en) * 2018-06-28 2020-01-07 强生消费者公司 Compositions and methods for treating skin disorders using light and glucosamine hydrochloride
CN112754949A (en) * 2021-01-26 2021-05-07 烟台仙瑟商贸有限公司 Sustained-release skin-brightening essence composition and preparation method thereof

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1901920A (en) * 2003-11-21 2007-01-24 雀巢技术公司 Food composition comprising glucosamine
US20060018851A1 (en) * 2004-06-28 2006-01-26 Procyte Corporation Methods and compositions for preventing and treating hyperpigmentation of skin
CN105581978A (en) * 2014-10-20 2016-05-18 湖南师范大学 Glucosamine derivative cation liposome nanoparticle preparation method
CN110652658A (en) * 2018-06-28 2020-01-07 强生消费者公司 Compositions and methods for treating skin disorders using light and glucosamine hydrochloride
CN112754949A (en) * 2021-01-26 2021-05-07 烟台仙瑟商贸有限公司 Sustained-release skin-brightening essence composition and preparation method thereof

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
裘炳毅、高志红: "《现代化妆品科学与技术 中》", 31 March 2016, 中国轻工业出版社 *

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