[go: up one dir, main page]

WO2021234536A1 - Gel de contour des yeux et son procédé de préparation - Google Patents

Gel de contour des yeux et son procédé de préparation Download PDF

Info

Publication number
WO2021234536A1
WO2021234536A1 PCT/IB2021/054209 IB2021054209W WO2021234536A1 WO 2021234536 A1 WO2021234536 A1 WO 2021234536A1 IB 2021054209 W IB2021054209 W IB 2021054209W WO 2021234536 A1 WO2021234536 A1 WO 2021234536A1
Authority
WO
WIPO (PCT)
Prior art keywords
vitamin
liposomes
gel
lipophilic
tpgs
Prior art date
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.)
Ceased
Application number
PCT/IB2021/054209
Other languages
English (en)
Inventor
Alessandro Zanini
Marco VELLANTE
Eugenio Sodo
Giovanni Cavallo
Fulvio FOSCHINI
Roberto GIUVA
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Offhealth SpA
Original Assignee
Offhealth SpA
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Offhealth SpA filed Critical Offhealth SpA
Priority to EP21732115.7A priority Critical patent/EP4110265A1/fr
Publication of WO2021234536A1 publication Critical patent/WO2021234536A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • 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
    • A61K8/03—Liquid compositions with two or more distinct layers
    • 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
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/34—Alcohols
    • 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
    • A61K8/67—Vitamins
    • 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
    • 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
    • A61K8/678—Tocopherol, i.e. vitamin E
    • 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
    • A61K8/92—Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof
    • A61K8/922—Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof of vegetable origin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q1/00—Make-up preparations; Body powders; Preparations for removing make-up
    • A61Q1/14—Preparations for removing make-up
    • 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
    • A61Q19/005—Preparations for sensitive skin

Definitions

  • the present invention relates to an eye contour gel, with a soothing and cleansing action of the eyelid waterline and the periocular area, indicated for the treatment of blepharitis or similar diseases, which gel will be defined hereinafter as lipophilic because it consists of liposomes which carry lipophilic substances.
  • said gel comprises a lipophilic composition consisting of:
  • Liposomes obtained by extrusion at a pressure between 800 and 1000 atm so as to have a particle size less than one micron, and consisting of non-hydrogenated phospholipids which carry Vitamin A Palmitate, Bisabolol, Tea Tree oil and Vitamin E TPGS, Xanthan gum as a viscosifying, gelling and structuring agent with good wetting ability, and
  • Ferulic acid also intercalated in the liposome phospholipids, which is stable and protects Vitamin A Palmitate from degradation, a molecule which has been taken as a stability index of the entire formulation containing other lipophilic ingredients, which would be unstable even if inside liposomes.
  • the liposomes consisting of a double layer of phospholipids and known for the soothing and emollient properties thereof, have the ability to act as carriers and make the carried substances more bioavailable, synergistically acting with Vitamin A, ferulic acid and Vitamin E TPGS in protecting the eyelid surface from the degenerative action of free radicals and UV rays.
  • the aforementioned formulation combines two important factors for the well-being of the eye: the moisturizing capacity of Xanthan Gum and the ability to supply a lipid component, by virtue of well-defined liposomes, to the surface surrounding the eyes by the liposomes.
  • a first aspect of the invention is that the experimentation carried out has shown that by controlling the following parameters:
  • the product obtained has an excellent stability which was found in all types of packaging, in particular in multi dose packages with commercial-type curved-tip dispenser.
  • a preferred composition of the obtained formulation is the following:
  • Formula 5 Liposomal solution with Xanthan Gum and Ferulic acid 0.040% by weight. which is a formulation of a structured gel containing vitamin E TPGS with the fundamental addition of ferulic acid which, also inserted in the liposomes at 0.04% by weight, solves the instability problem of Vitamin A
  • Another aspect of the invention relates to a formulation adapted to resolve the problem of the dispersibility (solubilization) of the lipophilic components in an aqueous phase by means of a mixture of non-hydrogenated phospholipids and active ingredients and at least three successive high-pressure extrusions between 800 and 1000 atm, to maintain the particle size of the liposomes at a value less than one micron or to reach a size less than 200 nm with four successive extrusions, as demonstrated experimentally.
  • Another aspect of the invention relates to a formulation like the previous one in which the addition of a specific amount of xanthan gum allows the (original) liposomal solution to assume a texture/body/volume thereof, thus becoming a product to spread on skin with the light action of the fingertips.
  • Another aspect of the invention relates to the method of preparing a liposomal solution for a structured gel which, in order to give the liposomal structure a greater ability to coordinate water molecules, includes the formation of liposomes characterized by having PEG chains outside the structure thereof consisting of the hydrophilic tail of Vitamin E TPGS while the lipophilic head thereof, Vitamin E, is inserted into the phospholipid (lipophilic) double of the liposomes.
  • Vitamin E TPGS in the liposome preparation step, thus the Vitamin E is inserted into the phospholipid multilayer, while the hydrophilic part thereof, PEG, remains outside the liposomes.
  • This allows the liposomal structure to increase the ability to coordinate water, since the liposomes with PEG chains outside the structure thereof act as "traps” (WHC, Water Holding Capacity) or as "binders” (WBC, Water Binding Capacity).
  • the liposomes according to the invention can be considered “pegylated” liposomes, even if the true pegylated liposomes are those consisting of phospholipids to which PEG chains have been added by means of a synthesis reaction.
  • Another aspect of the invention relates to an industrial preparation method of a lipophilic gel which comprises the solubilization step in solvent (ethanol) of the various ingredients Bisabolol, Tea Tree Oil, Vitamin A Palmitate, Vitamin E TPGS and Ferulic Acid and a subsequent vacuum drying which ensures a particular stability of the Vitamin A Palmitate.
  • Another aspect of the invention relates to a simplified and faster process than the previous one, which by eliminating the steps of solubilization in ethanol and the subsequent drying, reduces production times and costs while still providing a liposome gel, referred to below as FAST, the stability of which is only slightly lower than that obtained with the process described above.
  • a further aspect of the invention concerns the evaluation of the impact which the primary packaging can have on the product stability.
  • Anterior blepharitis is inflammation which affects the outer edge of the eyelids, where the eyelashes are attached; it is very often due to the presence of staphylococcal bacteria normally present on the skin which, for unknown reasons, cause this inflammatory reaction to the eyelids in some conditions.
  • Bisabolol is an oil which has soothing properties, with the effect of reducing skin redness by reducing inflammation, and Vitamin A Palmitate (oil) has a restorative effect and is a strong antioxidant.
  • Vitamin A palmitate is kept in tightly closed containers, away from light and at a temperature below 15°C.
  • the product could also solidify for prolonged storage periods. If the product solidifies, before use, it must be heated in a water bath to 45-50°C (maximum for 4 hours), stirring occasionally. It is apparent that the use thereof in a gel to be used on the face is impractical.
  • Xanthan gum is a polymer of natural origin which, by virtue of the particular chemical structure thereof, has been shown to have strong abilities to reduce oxidative stress levels on the ocular surface.
  • Xanthan gum is particularly suitable for the removal of desquamation residues of the eyelid surface in the event of inflammatory phenomena such as anterior blepharitis and blepharoconjunctivitis.
  • xanthan gum has a low cost which allows the use thereof even at high concentrations greater than 0.5%, a detail which is not negligible at the industrial production level due to the impact of the high costs thereof.
  • ferulic acid it has been described for use in cosmetic compositions as a skin lightener, sunscreen, skin anti-wrinkle agent, but the incorporation thereof into the aqueous phase of cosmetic compositions is problematic, while it is not easily incorporated into the oily phase of an emulsion or anhydrous compositions, given the limited solubility thereof in cosmetically acceptable solvents other than water, so much so that the instability problem thereof has been addressed.
  • a cosmetic composition in aqueous phase where the ferulic acid is stable is described in the published application WO 01/07004 A1.
  • Vitamin A Palmitate in the presence of Vitamin E TPGS is completely new and not deducible from the reference technical literature, intercalating it in the liposomes and making it carried thereby, as described in the present invention.
  • the claimed product is a hydrogel containing only liposomes, which are the unique and specific carrier for the active components: Tea Tree oil, Bisabolol, Vitamin A Palmitate and Vitamin E TPGS, and where the ferulic acid is deeply inserted (intercalated) in the phospholipid structure of the liposomes, even if it is not an oil, during an innovative preparation process which forms a peculiar feature of the invention, to carry out an overt protective action, synergistically with the liposomal structure, against Vitamin A Palmitate, which would be unstable even if inside the liposomes.
  • liposomes which are the unique and specific carrier for the active components: Tea Tree oil, Bisabolol, Vitamin A Palmitate and Vitamin E TPGS, and where the ferulic acid is deeply inserted (intercalated) in the phospholipid structure of the liposomes, even if it is not an oil, during an innovative preparation process which forms a peculiar feature of the invention, to carry out an overt protective action, synergistically with the
  • fig. 1 is a photo showing the very fluid, poorly structured and non-mucus adhesive texture of a typical liposomal solution of stable liposomes, without any precipitate
  • fig. 2 is a second photo instead showing the product obtained by adding xanthan gum to the liposomal solution in fig. 1 as a viscosifying and structuring agent
  • fig. 3 is a diagram of a liposome with Vitamin E TPGS, where the outer structure of the PEG coordinates many water molecules
  • fig. 4 shows the graph of the stability over time of Vitamin A Palmitate for a gel containing Xanthan Gum and Vitamin E TPGS at 25°C and 40°C for 6 months
  • FIG. 5 shows the graph of the stability over time of Vitamin A Palmitate for a gel containing Vitamin E TPGS in association with Ferulic Acid at 0.03%, at 25°C and at 40°C for 6 months
  • fig. 6 shows the graph of the stability over time of Vitamin A Palmitate for a gel containing Vitamin E TPGS in association with Ferulic Acid at 0.04%, contained in a multi-dose dispenser, respectively at 25°C and 40°C
  • fig. 7 shows the graph of the stability over time of Vitamin A Palmitate for a gel containing Vitamin E TPGS in association with Ferulic Acid at 0.04%, contained in a bottle with a nanoemulsion dispenser at 25°C and 40°C;
  • fig. 8 shows the graph of the stability over time of Vitamin A Palmitate for a gel containing Vitamin E TPGS in association with Ferulic Acid at 0.04%, contained in a single-dose dispenser bottle, at 25°C and 40°C;
  • fig. 9 shows the graph of the stability over time of the ferulic acid of the product stored in a primary multi dose container
  • fig. 10 shows the graph of the stability over time of the ferulic acid of the product stored in a primary multi dose container with a curved-tip dispenser
  • fig. 11 shows the graph of the stability over time of the ferulic acid of the product stored in a primary single dose container
  • Vitamin E TPGS fig. 12 shows the graph of the stability over time of the Vitamin E TPGS of the product stored in a primary multi-dose container
  • fig. 13 shows the graph of the stability over time of the Vitamin E TPGS of the product stored in a primary multi-dose container with a curved-tip dispenser
  • fig. 14 shows the graph of the stability over time of the Vitamin E TPGS of the product stored in a primary single-dose container
  • NIG fig. 15 shows the graph of the stability over time of the NIG of the product stored in a primary multi-dose container
  • fig. 16 shows the graph of the stability over time of the NIG of the product stored in a primary multi-dose container with a curved-tip dispenser
  • fig. 17 shows the graph of the stability over time of the NIG of the product stored in a primary single-dose container.
  • fig. 18 shows the graph of the stability over time of Vitamin A Palmitate for the FAST gel
  • fig. 19 shows the graph of the stability over time of Ferulic Acid for the FAST gel
  • fig. 20 shows the graph of the stability over time of Vitamin E TPGS for the FAST gel
  • fig. 21 shows the graph of the stability over time of the NIG for the Fast gel.
  • Fig. 22 shows the graph of the pH stability over time.
  • fig. 23 shows the graph correlating the liposome particle size to the pressure exerted during the extrusion step: the average size is equal to 82. 7 nm after a cycle of 4 extrusions.
  • the first task of the present invention was to overcome the problems which make the simultaneous presence of Vitamin A Palmitate, Bisabolol, and Tea tree oil difficult in a composition in the form of a gel which can be delicately distributed on the eyelids and the eyelid waterline.
  • FORMULA 1 proved effective from the point of view of the liposomal carrying of the components indicated above, but insufficient in relation to the practical use thereof as a gel, as the simple liposomal formulation for the concentration and features of non-hydrogenated phospholipids and the size of the liposomes less than 1 micron) does not have a visible and tangible texture (body- volume) and does not have the mucus adhesiveness which is expected from a gel to be applied on the eyelids or in the periocular area through a light action of the fingers.
  • the stability data of the vitamin A palmitate indicated a decrease in titer after only two months of 15% and 28%, at 25° and 40°C, respectively, as reported in the following TABLE A.
  • Vitamin E TPGS was then added, in the initial liposome preparation step, to the base formula viscosified and structured with Xanthan gum, so that the lipophilic part, Vitamin E (recognized as an antioxidant), was inserted in the phospholipid multilayer, while the hydrophilic part, the PEG, remained outside the liposomes, giving the whole liposomal structure: a greater antioxidant capacity inside the phospholipid multilayer due to the presence of vitamin E inserted therein, and a greater ability to coordinate the water molecules outside the lipid layer due to the presence of the hydrophilic PEG chains.
  • Ferulic Acid is a well-known antioxidant which can synergistically act with liposomes, containing Vitamin A Palmitate, Bisabolol and Tea Tree Oil, in protecting the eyelid surface from the action of free radicals and of UV rays.
  • a first composition of the formulation with Vitamin E is a well-known antioxidant which can synergistically act with liposomes, containing Vitamin A Palmitate, Bisabolol and Tea Tree Oil, in protecting the eyelid surface from the action of free radicals and of UV rays.
  • the product has improved the stability thereof.
  • this formulation was divided into different types of primary, multi-dose, multi-dose with curved dispenser, single-dose containers.
  • the first evaluation was carried out on a multi-dose package. The data are shown in fig. 6 and in the following table D.
  • Liposomal solution Vitamin A Palmitate, Vitamin E TPGS, Xanthan Gum, Ferulic Acid 0.040% w/w
  • Tables E and F show the stability results at 25°C and 40°C, respectively, for the multi-dose with curved dispenser and single-dose containers (primary packaging), as shown in the graphs in fig. 7 and 8.
  • the summary table G below highlights such a conclusion.
  • the single-dose package provides the product, again with reference to the Vitamin A Palmitate titer, greater stability: at 25°C a decrease of 7.93% in the initial titer after 6 months at 25°C and at 40°C a decrease of 14.73%.
  • the procedure for preparing such a liposomal solution includes:
  • the graph shown in fig 23 correlates the particle size of the liposomes to the pressure exerted during extrusion. Experimentally, after 4 successive extrusions, an average size of 82 .7 nm can be reached.
  • the liposomes as such before being viscous with the addition of Xanthan gum, have a size less than one micron. And it is this peculiarity which gives greater stability to the preparation, together with a better dispersibility of the active ingredients, which is very important and necessary for the low concentration thereof (Tea Tree Oil, Bisabolol, Vitamin A Palmitate, as the ferulic acid has not yet been added.
  • the solution obtained has the features of a translucent yellowish liposomal solution, without any precipitate, typical of stable liposomes.
  • the liposomal formulation does not have a visible texture (body) and is particularly fluid: as seen in fig. 1, it is not structured, it is not mucus adhesive: once placed on the skin, it does not give the impression of a cream or gel to be spread with a slight movement of the fingers.
  • the FORMULA 1 shown in Table I was improved by adding a viscosifying and mucus adhesive polysaccharide, such as Xanthan Gum, which at a certain concentration forms a compact gel.
  • a viscosifying and mucus adhesive polysaccharide such as Xanthan Gum
  • Xanthan Gum a viscosifying and mucus adhesive polysaccharide
  • This polysaccharide has the ability to coordinate many water molecules, giving the final product a remarkable moisturizing and emollient capacity, which is particularly important for a product with cosmetic purposes such as that on which our interest is focused.
  • the product is not stable.
  • the product is not satisfactory due to the poor chemical stability thereof, expressed as a decrease in the Vitamin A palmitate titer.
  • THIRD STEP A stabilization activity of Vitamin A Palmitate intercalated in the liposomes viscosified with Xanthan Gum was undertaken and FORMULA 3 reported below was reached, which comprises Vitamin E TPGS at 0.045%. FORMULA 3
  • Fig. 4 and Table B show the stability results at 25°C and at 40°C, from which it can be deduced that the product is not stable.
  • a stabilization activity of the formulation in the entirety thereof was carried out, and in particular of the Vitamin A Palmitate, intercalated in the liposomes viscosified with Xanthan Gum and the following formulation was reached, comprising the addition of Ferulic acid at 0.030% w/w.
  • the procedure for preparing such a liposomal solution includes the following steps:
  • the product composed of liposomes with Vitamin A Palmitate, Bisabolol, Tea Tree Oil, Vitamin E TPGS and Ferulic Acid, and gelled with Xanthan Gum, is identified in:
  • the product was divided into different primary containers: Multi-dose bottle, with curved-tip dispenser, and single-dose.
  • Table H and the graph in fig. 9 show the stability over time of the ferulic acid of the product stored in a primary multi-dose container.
  • Table I and the graph in fig. 10 show the stability over time of the ferulic acid of the product stored in a primary multi-dose container with curved-tip dispenser.
  • Table J and the graph in fig. 11 show the trend of the stability over time of the ferulic acid of the product stored in a primary single-dose container.
  • Table K groups the stability of ferulic acid in the different containers: the conclusion is that ferulic acid has excellent stability in all types of packaging.
  • TABLE L and the graph in fig. 12 show the stability over time of the Vitamin E TPGS of the product when it is stored in a primary multi-dose container.
  • Table M and the graph in fig. 13 show the stability over time of Vitamin E TPGS of the product stored in a primary multi-dose container with a curved-tip dispenser.
  • Vitamin E TPGS has excellent stability in all types of packaging.
  • Table P and the graph in fig. 15 show the stability over time of the NIG of the product stored in a primary multi-dose container. TABLE P
  • Table Q and the graph in fig. 16 show the stability over time of the NIG of the product stored in a primary multi-dose container with curved-tip dispenser. TABLE Q
  • NAG Sodium Hydroxymethylglycinate
  • TABLE T collects the pH trend in the three primary packages: multi-dose bottle, with curved-tip dispenser and single-dose strip.
  • the three pH trends do not show variations greater than 0.15 pH units.
  • Vitamin E TPGS stability

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Birds (AREA)
  • Epidemiology (AREA)
  • Chemical & Material Sciences (AREA)
  • Dermatology (AREA)
  • Biophysics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Emergency Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Dispersion Chemistry (AREA)
  • Cosmetics (AREA)

Abstract

La présente invention concerne une composition lipophile pour un gel de contour des yeux, avec une action apaisante et nettoyante sur la ligne des paupières et la zone périoculaire indiquée pour le traitement de la blépharite ou de maladies similaires, comprenant : des liposomes ayant une taille de particule inférieure à un micron, voire inférieure à 200 nm, constitués de phospholipides non hydrogénés qui portent du palmitate de vitamine A, du bisabolol, de l'huile de théier et de la vitamine E TPGS, de la gomme xanthane en tant qu'agent viscosant, gélifiant et structurant présentant une bonne capacité de mouillage, et de l'acide férulique qui, spécifiquement intercalé dans les liposomes, protège le palmitate de vitamine A contre une dégradation. En ajoutant de la vitamine E TPGS dans l'étape de préparation de liposomes, la vitamine E est insérée dans la multicouche de phospholipides, tandis que sa partie hydrophile, PEG, reste à l'extérieur des liposomes. Cela permet à la structure liposomale d'augmenter la capacité de coordonner l'eau, puisque les liposomes avec des chaînes PEG à l'extérieur de la structure de ceux-ci agissent comme « pièges » (capacité de rétention d'eau, WHC) ou comme « liants » (capacité de liaison à l'eau, WBC).
PCT/IB2021/054209 2020-05-18 2021-05-17 Gel de contour des yeux et son procédé de préparation Ceased WO2021234536A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
EP21732115.7A EP4110265A1 (fr) 2020-05-18 2021-05-17 Gel de contour des yeux et son procédé de préparation

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IT102020000011365 2020-05-18
IT202000011365 2020-05-18

Publications (1)

Publication Number Publication Date
WO2021234536A1 true WO2021234536A1 (fr) 2021-11-25

Family

ID=72178913

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IB2021/054209 Ceased WO2021234536A1 (fr) 2020-05-18 2021-05-17 Gel de contour des yeux et son procédé de préparation

Country Status (2)

Country Link
EP (1) EP4110265A1 (fr)
WO (1) WO2021234536A1 (fr)

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998011877A1 (fr) * 1996-09-18 1998-03-26 Dragoco, Inc. Composition de poudre seche contenant un principe actif encapsule dans des liposomes
US5853755A (en) * 1993-07-28 1998-12-29 Pharmaderm Laboratories Ltd. Biphasic multilamellar lipid vesicles
US20050214357A1 (en) * 2003-12-31 2005-09-29 Industrial Technology Research Institute Liposome and preparation method of the same
WO2008047394A1 (fr) * 2006-10-16 2008-04-24 Opocrin S.P.A. Compositions pour l'hygiène des paupières et l'hygiène périoculaire à tolérabilité oculaire et cutanée améliorée

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5853755A (en) * 1993-07-28 1998-12-29 Pharmaderm Laboratories Ltd. Biphasic multilamellar lipid vesicles
WO1998011877A1 (fr) * 1996-09-18 1998-03-26 Dragoco, Inc. Composition de poudre seche contenant un principe actif encapsule dans des liposomes
US20050214357A1 (en) * 2003-12-31 2005-09-29 Industrial Technology Research Institute Liposome and preparation method of the same
WO2008047394A1 (fr) * 2006-10-16 2008-04-24 Opocrin S.P.A. Compositions pour l'hygiène des paupières et l'hygiène périoculaire à tolérabilité oculaire et cutanée améliorée

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
DATABASE GNPD [online] MINTEL; 24 September 2010 (2010-09-24), ANONYMOUS: "Lifting Cream Cleanser", XP055771243, Database accession no. 1402029 *
DATABASE MEDLINE [online] US NATIONAL LIBRARY OF MEDICINE (NLM), BETHESDA, MD, US; January 2018 (2018-01-01), MAHER THURAYA NOAMAN: "The use of tea tree oil in treating blepharitis and meibomian gland dysfunction.", XP002801962, Database accession no. NLM29563688 *
OMAN JOURNAL OF OPHTHALMOLOGY, vol. 11, no. 1, January 2018 (2018-01-01), pages 11 - 15, ISSN: 0974-620X *

Also Published As

Publication number Publication date
EP4110265A1 (fr) 2023-01-04

Similar Documents

Publication Publication Date Title
Grampurohit et al. Microemulsions for topical use–a review
CN1130195C (zh) 基于乙氧化脂肪醚或乙氧化脂肪酯的毫微乳及其用途
DE69900065T2 (de) Nanoemulsion aus Blockcopolymeren von Ethylenoxid und Propylenoxid und deren Verwendungen in Kosmetika, Dermatologie, Pharmazeutika und/oder Ophthalmologie
CN1119984C (zh) 基于脱水山梨糖醇脂肪酸酯的毫微乳液及其应用
JP4203394B2 (ja) 高濃度のトリテルペノイドを含有する微小化リポソーム及びその製造方法
US6468551B1 (en) Cosmetic or dermatological preparations based on emulsifiers which are free from ethylene oxide and propylene oxide, for the preparation of microemulsion gels
CA2611144C (fr) Compositions comprenant un lipide et un copolymere de styrene et d'acide maleique
CH649915A5 (fr) Composition cosmetique a base d'une dispersion aqueuse de spherules lipidiques.
WO2008120249A1 (fr) Produits pharmaceutiques à base de lipides polaires et non polaires pour utilisation ophtalmique
HUE030841T2 (en) Preparations containing quaternary ammonium compounds
CN101686911B (zh) 囊泡组合物及皮肤外用剂
WO2018020903A1 (fr) Agent externe pour la peau
EP2162116B2 (fr) Vehicule sous forme d'une emulsion huile-dans-eau notamment destine a une utilisation optalmique ou dermocosmetique
KR20100118107A (ko) 벨벳 효과를 가진 피부 사용을 위한 글리코겐을 포함하는 화장품 조성물
JP2006213696A (ja) 皮膚外用剤
CN110897919B (zh) 一种抗氧化乳化组合物及其应用与含该组合物的护唇膏
WO2021234536A1 (fr) Gel de contour des yeux et son procédé de préparation
EP3888634B1 (fr) Formulation ophtalmique et son utilisation
WO2022181744A1 (fr) Composition de liposomes
CN101897949B (zh) 低刺激性透明乳化液剂型以供眼睛或眼睛周围有关组织表面免疫调节及消炎的眼用药物组合物
KR102802924B1 (ko) 식물 유래 단백질 기반 화장료용 나노 입자 조성물
KR102892685B1 (ko) ab:MAX 기술을 사용하여 안정성이 개선된 리포좀 및 그 제조방법
JP7735140B2 (ja) 乳化組成物
KR20240130643A (ko) 안정성이 개선된 탈모 치료 또는 예방용 나노 리포좀 조성물
JP2025127792A (ja) 水中油型乳化化粧料

Legal Events

Date Code Title Description
121 Ep: the epo has been informed by wipo that ep was designated in this application

Ref document number: 21732115

Country of ref document: EP

Kind code of ref document: A1

ENP Entry into the national phase

Ref document number: 2021732115

Country of ref document: EP

Effective date: 20220927

NENP Non-entry into the national phase

Ref country code: DE