Topical composition and its applicator, designed to relieve chalazione

Abstract

The invention relates to a topical composition comprising: - castor oil; - coconut oil, advantageously refined coconut oil, jojoba oil or avocado oil; - petroleum jelly; and its administration via a roll-on applicator for the treatment of chalazion in particular.

Description

Title of the invention: TOPICAL COMPOSITION AND ITS APPLICATOR, INTENDED TO RELIEVE CHALAZION technical field

[0001] The present invention relates to the field of dermatological care in connection with eye health, more particularly to the treatment of swellings present on the eyelid. More specifically, the invention relates to a topical composition for the treatment of chalazion. Prior state of the art

[0002] Several conditions, such as chalazion, stye, or blepharitis, are characterized by the appearance of a localized swelling on the eyelid. This swelling results in several unpleasant symptoms, such as swelling, a bump, redness, tingling, a burning sensation on the eyelid, or even watery eyes, or the formation of dandruff on the eyelashes.

[0003] The origin of eyelid swelling is variable and allows the pathology to be classified according to its origin: Blepharitis is a skin inflammation of the eyelid, caused by an infection or allergy, which results in swelling. A stye is an infection, usually bacterial, of the Meibomian gland located in the thickness of the eyelid, which is responsible for the swelling. A chalazion is caused by a non-infectious blockage of the Meibomian glands, which is responsible for the inflammatory swelling.

[0004] Thus, the cause of the chalazion is not of infectious origin, unlike blepharitis and stye.

[0005] In practice, Meibomian glands (tarsal glands) are sebaceous glands located in the epidermis of the eyelids. More precisely, they are situated in the eyelid cartilage, numbering 30 to 40 per eyelid, oriented perpendicularly to the free margin protected by the eyelashes. They secrete an oily substance, similar to sebum, which generally mixes with tears to lubricate the surface of the eye.

[0006] In cases where they do not function properly, particularly in the case of a chalazion, an excessive accumulation of secretions from the Meibomian glands causes them to become engorged, especially at their drainage opening located on the free edge of the eyelid. This engorgement results in an enlargement of the gland, in the form of an inflammatory cyst or granuloma. The chalazion can be internal or external. An external chalazion causes a thickening of the eyelid, visible on the eyelid. The eyelid may be red and swollen. An internal chalazion causes tearing and slight swelling under the eyelid.

[0007] Common, benign and without seriousness, the chalazion, which has no infectious cause, can resolve itself in several weeks.

[0008] However, depending on its size and location, a chalazion can become bothersome, painful, or even indent the cornea and / or cause blurred vision. If it persists, the chalazion must be surgically removed by making an incision in the gland through the conjunctiva under local anesthesia.

[0009] Before surgery and as soon as a chalazion appears, warm, moist compresses can be applied daily (2 to 3 times a day) to help the chalazion dissolve. Applying an antibiotic and / or cortisone ointment to the chalazion is also known.

[0010] However, these treatments have limited effectiveness: while they may temporarily alleviate symptoms, it is not uncommon for the chalazion to return.

[0011] In addition, the method of application is often complicated and restrictive for the patient.

[0012] Thus, applying a hot compress several times a day can be inconvenient: it requires a source of hot water and is time-consuming (5 to 10 minutes of application).

[0013] Applying antibiotic and / or cortisone ointment directly to the eyelid with a finger can be painful in the area of ​​the chalazion and may lead to infectious complications due to contamination if the hands have not been properly disinfected. Furthermore, manual application of an ointment does not allow for precise control of the dose applied or the targeted area, potentially resulting in unwanted penetration of the ointment into the eye.

[0014] Thus, there is an obvious need to develop new solutions for treating chalazion, which do not present the aforementioned disadvantages. Detailed description of the invention

[0015] The invention relates to a topical composition comprising judiciously chosen ingredients to be combined with a massage gesture, advantageously using a "roll-on" type application device.

[0016] As demonstrated in this application, this constitutes a particularly suitable solution for the management of chalazion, resulting in a reduction of irritation, redness and swelling of the eyelid and therefore improved comfort for the patient.

[0017] Definitions

[0018] The definitions below give the meaning generally used in the context of the invention and should be taken into account unless another definition is explicitly indicated.

[0019] The terms "about", "approximately", "in the order of" or "approximately" used in this document to denote a measurable value such as a quantity, a duration and others, shall be understood as encompassing variations of ± 20% or ± 10%, preferably ± 5%, more preferably ± 1%, and even more advantageously ±0.1% with respect to the specified value.

[0020] Ranges: Throughout this disclosure, various aspects of the invention may be presented in the form of a range of values ​​(range format). It should be understood that the description of values ​​in range form is done only for convenience and brevity and should not be interpreted as a limitation of the scope of the invention. Accordingly, the description of a range should be considered as having specifically disclosed all possible subranges as well as the individual numerical values ​​within that range. For example, the description of a range such as "from 1 to 6" should be considered as having specifically disclosed subranges such as 1 to 3, 1 to 4, 1 to 5, 2 to 4, 2 to 6, 3 to 6, etc. as well as individual numbers within that range, for example 1, 2, 2.7, 3, 4, 5, 5.3 and 6. This applies regardless of the extent of the range.

[0021] The term “abnormal,” when used in the context of organisms, tissues, cells, or components thereof, refers to organisms, tissues, cells, or components thereof that differ in at least one observable or detectable characteristic (e.g., age, treatment, time of day, etc.) from organisms, tissues, cells, or components thereof that exhibit the respective “normal” (expected) characteristic. Characteristics that are normal or expected for one type of cell or tissue may be abnormal for another type of cell or tissue.

[0022] The terms "patient," "subject," "individual," and others are used interchangeably in this document and refer to any animal or cell thereof, in vitro or in situ, that may be subjected to the methods described herein. In some non-limiting embodiments, the patient, subject, or individual is an animal, preferably a mammal, more advantageously a human.

[0023] For the purposes of the invention, a "disease" or "pathology" is a state of health in an animal in which its homeostasis is negatively affected and which, if left untreated, continues to deteriorate. Conversely, for the purposes of the invention, a "disorder" or "dysfunction" is a state of health in which the animal is able to maintain its homeostasis but in which the animal's health is less favorable than it would be in the absence of the disorder. In the absence of treatment, a The disorder does not necessarily lead to a deterioration in the animal's health over time.

[0024] A disease or disorder is "mitigated" ("reduced") or "improved" if the severity of a symptom of the disease or disorder, the frequency with which that symptom is experienced by the individual, or both, are reduced. This also includes the cessation of disease progression, that is, the stopping of the progression of the disease or disorder. A disease or disorder is "cured" ("restored") if the severity of a symptom of the disease or disorder, the frequency with which such a symptom is experienced by the individual, or both, are eliminated.

[0025] In the context of the invention, a “therapeutic” treatment is a treatment administered to a subject who presents the symptoms (signs) of a disease, with the aim of reducing or eliminating those symptoms. For the purposes of this invention, “treatment of a disease or disorder” means reducing the frequency or severity of at least one sign or symptom of a disease or disorder experienced by the subject. A treatment is said to be prophylactic when it is administered to prevent the development, spread, or worsening of a disease, particularly if the subject does not yet present the symptoms of the disease and / or if the disease has not been diagnosed.

[0026] As used herein, “treating a disease or disorder” means reducing the frequency or severity of at least one sign or symptom of a disease or disorder experienced by a subject. Disease and disorder are used interchangeably in the context of the treatment according to the invention.

[0027] For the purposes of the invention, an "effective amount" or "effective quantity" of a compound is the amount of compound that is sufficient to provide a beneficial effect to the subject to whom the compound is administered. The expression "therapeutically effective amount" refers to an amount that is sufficient or effective in preventing or treating (in other words, delaying or preventing the development, preventing the progression, inhibiting, reducing, diminishing, or reversing) a disease or disorder, including the relief of the symptoms of that disease or disorder.

[0028] In the following description, percentages (%) correspond to mass percentages (also called mass percentages), unless otherwise specified. Thus, the percentage of an ingredient corresponds to the mass of said ingredient relative to the total mass of the composition.

[0029] Thus, according to a first aspect, the present invention relates to a topical composition based on: - castor oil; - coconut, jojoba or avocado oil, advantageously coconut oil; and - petroleum jelly.

[0030] One of the ingredients of a composition according to the invention is castor oil.

[0031] Castor oil is a non-food vegetable oil, improperly called "Castor oil." It is obtained from the seeds of the castor bean plant (Ricinus communis) and is a colorless or light yellow viscous liquid. Its triglycerides are composed of approximately 90% C18 fatty acids, including ricinoleic acid (or (R)-(+)-12-hydroxy-9Z-octadecenoic acid), a hydroxylated omega-9 fatty acid that forms ricinolein, the major triglyceride of this oil. Its use in cosmetics is largely dedicated to the care of hair, eyelashes, and eyebrows.

[0032] According to a particular embodiment, castor oil represents from 40 to 60%, advantageously from 45 to 55%, even more advantageously 50% by weight of the composition.

[0033] A second ingredient of a composition according to the invention is a vegetable oil such as coconut oil, advantageously refined coconut oil.

[0034] Coconut oil is available in two main forms, depending on its production method: - Virgin coconut oil is obtained by cold pressing the fresh albumen of the coconut. Refined coconut oil, also known as copra oil, is obtained by hot-pressing the dried endosperm, then refining and deodorizing it. Very rich in saturated fatty acids, refined copra oil is used for its emollient properties.

[0035] It is used in cosmetics, in particular to nourish the skin and hair.

[0036] As is known, coconut oil is generally in solid form at a temperature below 25°C. For the preparation of the composition according to the invention, or even its use, it may be useful to heat this ingredient, or even the composition or its application device as described below, above this temperature.

[0037] Alternatively, jojoba oil or avocado oil may be used.

[0038] According to a particular embodiment, such an oil represents from 20 to 40%, advantageously from 25 to 35%, even more advantageously 30% by weight of the composition.

[0039] Vaseline constitutes the third ingredient of a composition according to the invention.

[0040] Vaseline (or petroleum jelly) is a petroleum distillate. It is formed Primarily composed of alkanes, with the general formula (CnH2n+2), and fluid at room temperature, petroleum jelly is an ointment used as an adjunct treatment for skin irritations, burns, and dryness. Its most well-known use is as a lip balm. It is also an ingredient in most cosmetic lotions, used as an excipient.

[0041] According to a particular embodiment, Vaseline represents from 5 to 20%, advantageously from 10 to 15%, even more advantageously 12% by weight of the composition.

[0042] According to one embodiment, the composition according to the invention comprises: - castor oil, which represents 40 to 60%, advantageously 45 to 55%, even more advantageously 50% by weight of the composition; and / or - coconut oil, advantageously refined coconut oil, representing 20 to 40%, advantageously 25 to 35%, even more advantageously 30% by weight of the composition; and / or - Vaseline, which represents 5 to 20%, advantageously 10 to 15%, even more advantageously 12% by weight of the composition.

[0043] Within the framework of the present invention, it has been shown that the combination of these 3 ingredients, none of which is considered a therapeutic active ingredient, had a beneficial effect in the management of chalazion.

[0044] In the context of the invention, a therapeutic active (or active substance or active principle or active ingredient) is defined as a compound or substance possessing a recognized pharmacological activity of its own in relation to a given pathology, which is generally associated with the status of a drug and obtaining marketing authorization.

[0045] Thus and according to a first embodiment, the composition according to the invention does not contain any therapeutic agent, in particular for ophthalmological or dermatological purposes.

[0046] Alternatively, the composition according to the invention may contain a therapeutic agent for the treatment of the same pathology as those covered by this application or of a different pathology, advantageously ophthalmological or dermatological. It should be noted that, alternatively, such a therapeutic agent may be administered separately and therefore not be contained in the composition according to the invention. Such administration may be carried out simultaneously or at different times.

[0047] Thus, and in relation to the chalazion, a corticosteroid (e.g., dexamethasone or hydrocortisone) and / or an antibiotic (e.g., azithromycin, neomycin, norfloxacin, oxytetracycline, ofloxacin, or rifamycin) may also be administered, or even added to a composition according to the invention. For the treatment of a stye, a suitable antibiotic will advantageously be used.

[0048] According to a particular embodiment, the composition according to the invention does not contain selenium disulfide (SeS2), glycerol monolaurate, caffeine and / or silk fibroin.

[0049] Furthermore, and as is known to those skilled in the art, the composition of the invention may include, in addition to the three aforementioned ingredients, a pharmaceutically acceptable carrier. In a particular embodiment, the term "pharmaceutically acceptable" means approved by a federal or state government regulatory agency or listed in the United States or European Pharmacopoeia or in another generally recognized pharmacopoeia for use in animals and humans. The term "carrier" means a diluent, adjuvant, excipient, or vehicle with which the aforementioned products are administered.

[0050] Thus, for a suitable formulation, the composition according to the invention may contain a thickening agent (or viscosity-enhancing agent) such as glyceryl behenate (CAS number 77538-19-3). For example, this could be the product Compritol® marketed by Gattefossé. In the context of the invention, a thickening agent is intended to increase the viscosity of a composition.

[0051] As is known to those skilled in the art, the amount of thickening agent is adjusted according to the desired viscosity of the composition, as indicated below. In a particular embodiment and in relation to glyceryl behenate, it advantageously represents 0.5 to 10%, advantageously 3 to 7%, and even more advantageously 5% by weight of the composition.

[0052] Furthermore, for a suitable formulation, the composition according to the invention may contain an emulsifying agent such as glyceryl or glyceryl monostearate (CAS No. 85251-77-0 (or 31566-31-1)) corresponding to the glycerol ester of stearic acid. For example, this could be the product Géléol® marketed by Gattefossé. In the context of the invention, the purpose of an emulsifying agent is to stabilize the composition.

[0053] As is known to those skilled in the art, the quantity of emulsifying agent is adjusted according to the desired consistency of the composition according to the invention. In a particular embodiment and in relation to glycerol monostearate, it advantageously represents 0.5 to 10%, advantageously 1 to 5%, and even more advantageously 3% by weight of the composition.

[0054] According to a preferred embodiment, a composition according to the invention does not contain preservatives, in particular those commonly used in connection with cream and ointment type products to be applied to the skin.

[0055] In a preferred embodiment, the composition according to the invention is formulated in accordance with routine procedures for a composition suitable for topical administration in humans. The area targeted by the administration is The skin, and more specifically the eyelids, are advantageously affected. The mucous membranes, conjunctiva, and / or cornea are not targeted.

[0056] According to a preferred embodiment, the composition according to the invention is in the form of a gel, an emulsion, an oil, a balm, a cream or an ointment, of homogeneous consistency and suitable for spreading in a wide range of temperatures (typically from 4°C to 40°C), while avoiding its runoff in particular in the eyes and without leaving a greasy film on the targeted area.

[0057] Advantageously, such a composition does not contain an aqueous phase or a reduced amount of aqueous phase to maintain microbiological stability without the addition of a preservative.

[0058] Even more advantageously, this composition is compatible with administration using a "roll-on" type applicator device.

[0059] Thus and according to another aspect, the present invention relates to a device, advantageously a storage and distribution device, even more advantageously a ball applicator, comprising a composition such as described above.

[0060] As is known in this technical field, a "roll-on" is a container, such as a tube or bottle, whose dispensing orifice is advantageously a rotating ball that releases its contents upon contact with the surface to be treated. This release can be aided by pressure applied to the container. Such a device allows for the storage and controlled local application of a composition (deposition of a specific quantity of the composition, uncontaminated by contact with fingers, onto a targeted area). Furthermore, it can be equipped with a cap or lid to protect the composition from air, water, and potential external contamination (pollutants, dust, etc.).

[0061] According to a particular embodiment, the container, transparent or opaque, is made of plastic, for example polyethylene (PE), advantageously high-density polyethylene (HDPE) such as the Polyfoil® device marketed by Neopac. COEX tubes can also be used: these are co-extruded polyethylene (PE) tubes lined with a barrier layer of ethylene vinyl alcohol (EVOH). It is advantageously flexible, i.e., it has the capacity to be deformed under the action of manually applied pressure. The ball, for example with a diameter of 10 mm, can be made of ceramic, plastic, or metal. Advantageously, a metal ball, for example stainless steel, provides a more effective massaging effect. The cap is advantageously made of plastic that can be covered with a metallic layer, for example polypropylene (PP), with an advantageously rigid structure.

[0062] The use of a rollerball applicator device, in addition to the advantages mentioned above, allows for the application of physical pressure and / or massage to the application area. This therefore contributes, through mechanical action, to the decongestion and relief of blockages in the Meibomian glands.

[0063] The composition according to the invention has a texture suitable for topical application around the eye, advantageously using such a device.

[0064] As is known in this technical field, the composition according to the invention can be sterilized before and / or after its packaging in the application device, advantageously the rollerball applicator. The sterilization techniques that can be implemented are well known to those skilled in the art. By way of example, a composition according to the invention can be filtered before its packaging.

[0065] The present invention also relates to compositions and devices as defined above for the prevention, including the prevention of recurrence, management and / or treatment of certain pathologies, in particular eyelid swelling.

[0066] Pathologies related to, associated with, resulting from or caused by a dysfunction of the Meibomian glands are particularly targeted within the framework of the present invention.

[0067] Examples include: chalazion, dry eye syndrome, blepharitis, and styes. Advantageously, pathologies related to occlusion (or occlusive dysfunction) of the Meibomian glands are targeted, even more advantageously non-infectious pathologies such as chalazion.

[0068] Indeed, a beneficial effect is reported, even in the absence of therapeutic active ingredient, linked to the formula of the composition according to the invention and to its method of administration.

[0069] Thus, and in other respects, the present invention also relates to: - a composition such as described above for the management of eyelid swelling, advantageously of pathologies related to a dysfunction of the Meibomian glands, even more advantageously of chalazion; - the use of a rollerball applicator comprising a composition such as described above for the management of eyelid swelling, advantageously of pathologies related to a dysfunction of the Meibomian glands, even more advantageously of chalazion; - a method for managing eyelid swelling, advantageously related to a pathology linked to Meibomian gland dysfunction, and even more advantageously to chalazion, by topical application, advantageously on the eyelid, of a composition such as described above, advantageously using a rollerball applicator.

[0070] The amount of the composition of the invention, in particular the three ingredients as described above, that is effective in the intended treatment can be determined by standard clinical techniques. Furthermore, in vivo and / or in vitro tests, such as those described in the examples below, may optionally be used to help predict optimal dosage ranges. The precise dose to be used may also depend on the severity of the disease and should be decided according to the practitioner's judgment and the individual patient's condition.

[0071] According to a preferred embodiment, the composition according to the invention is administered daily, with a minimum of twice a day, advantageously in the morning and evening, and up to 6 times a day. It should be noted that, in addition to the administration sequences of the composition, the rollerball applicator can be used alone, without releasing the composition, for the beneficial physical effect of massage, in particular the decongestion of the Meibomian glands.

[0072] Advantageously, treatment is initiated as soon as the condition appears (swelling, redness, irritation, etc., on the upper or lower eyelid), and even more advantageously after diagnosis by a physician or ophthalmologist. Treatment may last several days, weeks, or even months, advantageously until the symptoms have completely disappeared. Treatment can also be taken preventively, particularly to prevent recurrence.

[0073] Before applying the composition according to the invention, the area to be treated, advantageously the eyelid, may be: - cleaned using any suitable product such as soapy water or a disinfectant; - heated, for example by the application of hot water, particularly in the form of compresses.

[0074] Before application, the composition according to the invention, advantageously the administration device containing it, are brought to a temperature above 25°C, for example by rubbing between the hands.

[0075] As illustrated in the examples, the application of the composition according to the invention is advantageously done by massage using the roller applicator, namely back-and-forth, circular and / or longitudinal movements on and / or along the eyelid to be treated.

[0076] The disclosures of each patent, patent application, and publication cited in this application are incorporated by reference in their entirety. Without further description, it is deemed that a person skilled in the art may, by using the description and the following illustrative examples, produce and use the compounds of the present invention and implement the claimed methods. Examples of completed projects

[0077] The invention and its advantages will become clearer from the following embodiments. These, however, are not intended to be limiting.

[0078] The invention is further illustrated with the aid of a composition based on castor oil, coconut oil and petroleum jelly packaged in a metal ball applicator and in connection with the treatment of chalazion. 1 / Composition

[0079] A composition according to the invention may have the following formula:

[0080] [Tables 1] Ingredients Quantity (% by mass) Castor oil (natural non-hydrogenated castor oil) 50 Coconut oil (naturally refined coconut oil) Vaseline 12 Glyceryl behenate / Comprîtes® (Gatteîbssé) 5 Glyceryl monostearate / GeleoF (Gatteîbssé) 3

[0081] Table 1: Composition according to the invention 2 / Characterization of the composition

[0082] Viscosity:

[0083] The composition in Table 1 above has a viscosity value of 3800 mPa.s, suitable for application using a ball applicator. 3 / Use of the composition

[0084] 3-1 Application device:

[0085] After filtration, the composition of Table 1 is packaged in a ball applicator, namely a Polyfoil® tube (e.g., 10 mL capacity) fitted with a 10 mm diameter stainless steel ball. A removable polypropylene (PP) cap is placed on the ball to allow closure of the applicator.

[0086] 3-2 Application Protocol: Dosage

[0087] The composition of Table 1 is applied using the ball applicator described in point 3-1 as soon as the first signs of chalazion appear.

[0088] It is applied to the chalazion and eyelids at least twice a day, in the morning and evening, and up to 6 times a day.

[0089] If the chalazion does not disappear after 15 days of application, an ophthalmologist should be consulted, who may prescribe further treatment. Recommendations for use

[0090] For maximum effectiveness, it is recommended to warm the eyelids, for example with compresses, 5 to 10 minutes before application.

[0091] Hands should be washed before use.

[0092] If the user is wearing lenses or glasses, they should be removed.

[0093] It is advisable to warm the applicator between your hands before use if the outside temperature is below 20°C.

[0094] No instrument should be used to open the tube.

[0095] The cap should be removed.

[0096] The applicator ball is placed on the chalazion and on the eyelid skin to be treated.

[0097] Gently squeeze the tube and begin a longitudinal massage along the eyelid for 1 minute, then possibly continue with a rotational massage centered on the swelling.

[0098] Replace the cap on the tube.

Claims

Demands

1. Topical composition comprising: - castor oil, representing 40 to 60% by weight of the composition; - coconut oil, advantageously refined coconut oil, jojoba oil or avocado oil, representing 20 to 40% by weight of the composition; and - petrolatum, representing 5 to 20% by weight of the composition.

2. Composition according to claim 1, characterized in that: - castor oil represents 45 to 55%, advantageously 50% by weight of the composition; and / or - coconut oil, advantageously refined coconut oil, represents 25 to 35%, advantageously 30% by weight of the composition; and / or - petrolatum represents 10 to 15%, advantageously 12% by weight of the composition.

3. Composition according to any one of claims 1 to 2, characterized in that it is preservative-free.

4. Composition according to any one of claims 1 to 3, characterized in that it is in the form of a composition intended for topical application, advantageously a gel, an emulsion, an oil, a cream, a balm or an ointment.

5. Composition according to any one of claims 1 to 4 for use in the treatment of eyelid swelling.

6. Composition according to any one of claims 1 to 4 for use in the treatment of obstructive dysfunction of the Meibomian glands.

7. Composition for its use according to claim 6, characterized in that it is used in the treatment of chalazion.

8. Ball applicator comprising a composition according to any one of claims 1 to 4.