A process using radiofrequency and a cosmetic composition

A cosmetic process combining non-polymeric active ingredients with bipolar radiofrequency pulses addresses the limitations of existing radiofrequency technologies, enhancing ingredient penetration and efficacy while ensuring safety for skin care applications.

FR3149509A1Pending Publication Date: 2024-12-13LOREAL SA
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Patent Information

Application Number
FR2023005789
Authority / Receiving Office
FR · FR
Patent Type
Applications
Current Assignee / Owner
Filing Date
2023-06-08
Publication Date
2024-12-13

AI Technical Summary

Technical Problem

Existing radiofrequency technologies for skin care face challenges in effectively delivering active ingredients due to the risk of skin burning and limited penetration, necessitating a method that enhances the efficacy and safety of these devices.

Method used

A cosmetic process involving the application of a non-polymeric cosmetic active ingredient with a molecular weight between 100 Da to 700 Da, combined with bipolar radiofrequency pulses between 100 kHz and 100 MHz, to enhance the penetration and effectiveness of active ingredients.

Benefits of technology

Significantly improves the penetration and effectiveness of active ingredients into the skin, offering a safe and efficient method suitable for both professional and domestic use, with enhanced collagen remodeling and reduced risk of skin damage.

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Abstract

The invention relates to a non-therapeutic, cosmetic skin treatment method comprising: applying a cosmetic composition comprising a non-polymer cosmetic active ingredient with a molecular weight by weight ranging from 100 Da to 700 Da to a target area of ​​the skin; and exposing the target area of ​​the skin to a succession of pulses of an electric current, the pulses having a frequency between 100 kHz and 100 MHz, and the electric current being supplied by a bipolar radiofrequency cosmetic device having at least one electrode and at least one counter-electrode. Figure 1
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Description

Title of the invention: A method using radio frequency and a cosmetic composition

[0001] The present invention relates to a non-therapeutic cosmetic process for improving the appearance of the skin using radiofrequency-based technology and a cosmetic composition.

[0002] More generally, a cosmetic product is a product as defined in Regulation (EC) No 1223 / 2009 of the European Parliament and of the Council of 30 November 2009 on cosmetic products. Technological background

[0003] Non-ablative devices for home use are designed to deliver thermal energy to the skin for biological effects such as: stimulating natural collagen production, lifting and firming the skin to reduce wrinkles. To be compatible with home use, the thermal energy delivered to the skin must be limited within a certain range to ensure good tolerance and prevent burns.

[0004] Radio frequency (RF) is an electromagnetic wave and not a photonic emission process. It is an alternating electric current: the change in polarity + / - at the skin surface causes a molecular vibration which produces a quantity of heat depending on the intensity of the current and time according to Ohm's law: E = I x R x t.

[0005] Radio frequency current is a sinusoidal current. In the general definition, the frequency of the current is between 3 kHz and 300 GHz; in cosmetics, most of the instruments listed have a current frequency between 100 kHz and 10 MHz.

[0006] The complexity of radiofrequency techniques is linked to the different modes of energy delivery. Energy can be delivered externally, and depending on the emission mode, a distinction is made between monopolar radiofrequency and, much more widespread, bipolar radiofrequency. The current flows between two electrodes, causing tissue heating which is the basis of the effective thermal effect. The depth of the thermal effect is equal to half the distance between these electrodes. Thus, increasing the number of electrodes follows this logic to increase the surface area and depth of treatment, but the terms tripolar, quadripolar, or octapolar are essentially marketing ploys.

[0007] The energy delivery is limited, as is the pulse duration, to avoid potential thermal damage to the epidermis, which could lead to burns or even scarring. This explains the operating method of these so-called external bipolar techniques, which involve a repeated rotary movement on the skin surface. for a variable duration depending on the device. But most importantly, limiting the energy delivered only results in a modification of the extracellular environment, including collagen and elastin.

[0008] Consequently, monopolar and bipolar radiofrequencies are classified as subcutaneous (superficial) radiofrequencies, meaning they are suitable for external and superficial skin treatment. The effectiveness of these treatments is limited by the risk of skin burns above 42°C.

[0009] To overcome this risk of skin irritation, another method has been proposed: fractional radiofrequency, also delivered externally, with probes that increase the pulse duration and decrease the energy level by having a controlled coagulation effect on superficial and dermal tissues. The active electrode is divided into a multitude of microelectrodes in order to distribute the thermal energy more evenly than in the strictly bipolar case, which multiplies the heat density concentrated at a single point, as is felt in bipolar electrodes at the point of contact with the skin, into several small areas.

[0010] Finally, intratissue radiofrequency, or HiFR (High-intensity Focused Radiofrequency), has been developed more recently. There is no focusing in the "optical" sense of the term, but rather a local action deep within the tissue. The objective is to deliver all the energy deep into the tissues, for example, using microneedles. This can involve high-intensity, fractional, intratissue, multi-layer microneedle radiofrequency. This technique allows for the delivery of greater power since it bypasses the skin barrier thanks to the microneedles. The thermal effect at the needle tip can reach 65°C.

[0011] As a result, high-intensity radiofrequencies are referred to as subcutaneous or deep radiofrequencies. They can be used to firm tissues or improve the appearance of scars and stretch marks.

[0012] It is known to use radiofrequency technologies for skin care or rejuvenation applications as described in CN113317870, CN107998509, CN110141355, WO2021243403, WO2016162234, WO201687289, CN111616794.

[0013] Document WO201540049 discloses a non-invasive treatment device for heating an internal region of the skin using a radiofrequency electric current, an external skin surface region adjacent to the internal region being provided with a treatment substance selected to be transportable through the skin under the influence of an electric field and further selected to increase electrical transmission to the internal region, the device comprising:

[0014] - a first treatment electrode configured and arranged to allow the electric current to pass through an external surface of the skin and through the internal region;

[0015] - a radio frequency generator configured and arranged so that, during In use, the electric current generated by the radiofrequency generator is applied through a first treatment electrode to the external surface of the skin and through the internal region;

[0016] - a first field electrode configured and arranged to provide, in use, an electric field in the skin to transport the treatment substance to the internal region;

[0017] - an electric field generator configured and arranged such that, during In use, a direct current electric field generated by the electric field generator is applied through the first field electrode to the substance being treated, thereby transporting at least a portion of the substance being treated from the outer surface region to the inner region; and

[0018] - a control unit.

[0019] Document CN108452436 discloses a high-frequency radio frequency micro-vibration device. The high-frequency radio frequency micro-vibration device comprises a main control circuit board, a motor, an eccentric gear, and a stainless steel output head. A current flows through the stainless steel output head and reaches the face, then passes through the face, the front of the chest, the arms, the palm, and reaches the stainless steel buttons. It returns to the high-frequency radio frequency micro-vibration device to form a closed loop, promoting better absorption of cosmetics.

[0020] Document CN112007279 discloses a portable anti-wrinkle device with (a) a shell, which includes a retaining part and a head part; (b) at least one radio frequency contact disposed on the head; and (c) a capsule holder adapted to hold a capsule of cosmetic composition.

[0021] Document FR3014321 discloses a processing module for a product intended to be applied to the user's body, in particular a cosmetic and / or pharmaceutical product. This processing module is configured to activate the product, for example by radio frequency, and is arranged to be removably attached to a support defined by a receptacle containing the product. Such a processing module enables the product to be activated, particularly in situ, i.e., on the user's body, notably to optimize the effectiveness of the applied product and / or to improve its penetration into the user's body.

[0022] Document JP2011194175 discloses a cosmetic device comprising a Radio Frequency (RF) transmitter and a pair of RF electrodes. A control device delivers a control signal to the RF transmitter. The RF transmitter comprises, For example, an inverter converts direct current from a battery (not shown) into high-frequency current (alternating current). The RF transmitter delivers this converted high-frequency current to the RF electrode based on the control signal. When the RF electrodes are placed against the skin, the skin acts as an electrical resistance, connecting them. This electrically closes the circuit between the RF transmitter and the RF electrode, allowing the high-frequency current to flow. Because there is skin in the path of the circuit, particularly between the two RF electrodes, radiofrequency current can be delivered to the skin. The electrical energy is consumed as heat in the skin, which acts as an electrical resistance, warming the skin to promote the diffusion of cosmetic agents.

[0023] There remains a need to benefit from a process enabling the improvement of the efficiency of radiofrequency devices in cosmetics.

[0024] The objective is to bring multiple advantages to non-ablative RF and / or high-frequency microcurrent technology by improving the mode of action, in particular by selecting formulas with active ingredient coupling properties for which the RF signal will also act as a skin penetration booster.

[0025] Another objective of the invention is to determine types of active ingredients capable of adding to or even forming a synergy with the biological effects of collagen remodeling directly induced by the RF signal. Definition of the invention

[0026] The present invention addresses this need through a non-therapeutic, cosmetic skin treatment method, comprising:

[0027] The application, to a target area of ​​the skin, of a cosmetic composition comprising a non-polymer cosmetic active ingredient having a molecular weight by weight ranging from 100 Da to 700 Da,

[0028] Exposure of the target area of ​​the skin to a succession of pulses of an electric current, the pulses having a frequency between 100 kHz and 100 MHz and the electric current being supplied by a bipolar radiofrequency cosmetic device having at least one electrode and at least one counter-electrode.

[0029] The combined action of the pulse with a frequency between 100 kHz and 100 MHz and the cosmetic composition comprising the non-polymer cosmetic active ingredient has the effect of significantly promoting the penetration of such active ingredients in order to increase their effectiveness, in particular when the composition is applied concomitantly with the RF treatment, compared to a topical application of the same composition applied alone or compared to the RF treatment carried out alone, i.e. without the cosmetic composition.

[0030] This involves delivering thermal energy to the skin using a radio generator frequencies, especially in a range compatible with both professional and home use (e.g., a non-invasive application head, limited heating of the skin surface, with a sensor and an ON-OFF switch to ensure good tolerance / absence of side effects of the routine).

[0031] The process can be intended for domestic or professional use, for example in a beauty salon.

[0032] In particular, the time required to complete the steps is short. The process is therefore perfectly suited for everyday domestic use, for example during a lunch break.

[0033] The process can be repeated several times, preferably several times a month, the period between two applications preferably ranging from 1 to 15 days, more preferably from 1 to 7 days and even more preferably from 1 to 2 days.

[0034] Preferably, the target area has an equivalent diameter less than or equal to 1 cm.

[0035] Preferably, the target area has an equivalent diameter greater than 0.1 mm, or even greater than 0.5 mm, in particular greater than 1 mm.

[0036] Cosmetic composition

[0037] Step b) can be carried out after step a). Preferably, step b) and step a) are carried out concurrently.

[0038] Step a) of applying the cosmetic composition can be carried out only once on the same target area.

[0039] Alternatively, step a) of applying the cosmetic composition can be repeated several times on the same target area, for example between 2 and 200 times.

[0040] Step a) of application can be carried out between 1 and 5 times a day on the same target area.

[0041] The cosmetic composition can be applied at least once a day for at least 6 days, preferably at least twice a day for at least 7 days, in particular for at least 14 days, better for at least 21 days, even better for at least 28 days, better for at least 35, 42, 49 or 56 days.

[0042] The cosmetic composition includes at least one non-polymer cosmetic active having a molecular weight by weight ranging from 100 Da to 700 Da, in particular chosen from the list below.

[0043] Preferred active ingredients having a molecular weight by weight ranging from 100 Da to 700 Da

[0044] 2,4-diamino-6-piperidinopyrimidine-3-oxide or "Minoxidil" described in US-4,139,619 and US-4,596,812,

[0045] Aminexil or 2,4-diaminopyrimidine 3-oxide, described in WO 96 / 09048,

[0046] Xanthine derivatives such as diethylaminoethyl theophylline hydrochloride and caffeine.

[0047] In particular, the composition according to the invention comprises a content of active ingredient(s) presenting a molecular weight by weight ranging from 100 Da to 700 Da ranging from 0.01% to 10%, and preferably from 0.1% to 5% by weight, relative to the total weight of the composition.

[0048] Additional active ingredients and adjuvants

[0049] The cosmetic composition may include one or more additional active ingredients and / or one or more of the adjuvants commonly used in the cosmetic field.

[0050] The cosmetic composition further comprises a physiologically acceptable medium. Such a medium is considered physiologically acceptable when it does not generate tingling, pulling, or unacceptable discomfort for the user.

[0051] Pharmaceutical forms

[0052] A composition used according to the invention can be presented in all the galenic forms normally used in the cosmetic field.

[0053] More specifically, this composition is intended for topical application. Preferably, such a composition is not intended to be rinsed off after application.

[0054] A composition according to the invention is preferably intended to be applied to skin.

[0055] Preferably, the skin is the skin of the face and / or body, in particular of the face and / or hands, preferably of the face, and more particularly of the forehead and / or wings of the nose and / or chin, the corners of the lips and eyes.

[0056] A composition may alternatively take the form of a face and / or body care or makeup product, and be packaged for example as a cream in a jar or as a fluid in a tube or pump bottle or dropper bottle.

[0057] Radio frequency pulse

[0058] Step b) can be performed only once on the same target area.

[0059] Alternatively, step b) can be repeated several times on the same target area, particularly several times a month.

[0060] Step b) can be repeated to cover an entire area of ​​skin inhomogeneity.

[0061] Step b) of exposure can be carried out between 1 and 20 times over a period of two months.

[0062] The period between two repetitions of step b) can be between 1 and 15 days, in particular between 1 and 7 days, between 1 and 2 days or even every day.

[0063] Such durations allow a high level of treatment performance in a relatively short period compared with the prior art.

[0064] The process, in particular step b), can be carried out using a portable device in particular known under the reference RF Ultrasonic Device, model EH-XR10 ® marketed by Panasonic, the Newa ® marketed by EndyMed.

[0065] The pulses preferably have a constant duration. In one variant, the Pulses have a variable duration. Two consecutive pulses of ranks n and n+1 can therefore have different respective durations.

[0066] The energy emitted per pulse (for 5 kOhms) is preferably between 0.6 mJ and 70 mJ. The device can be configured to emit radio frequencies for a certain predefined operating time, then switch off automatically.

[0067] The total light power received by the area to be treated during a pulse is advantageously between 0.067 W and 0.67 W.

[0068] The distance between the device and the area to be treated can be between 0cm and 100 cm, preferably between 0 and 1 or 2 cm.

[0069] Together

[0070] The invention further relates, in addition to the above, to an assembly for carrying out the process described above comprising a cosmetic radiofrequency device generating electrical pulses of a frequency between 100kHz and 100 MHz and a cosmetic composition comprising a non-polymer cosmetic active having a molecular weight by weight ranging from 100 Da to 700 Da.

[0071] The assembly can be marketed in a single package, including an instruction guide enabling the user to implement the process according to the invention. Preferred modes of implementation

[0072] Preferably, the method according to the invention has one or more of the following characteristics, taken alone or in combination:

[0073] the electric current has a voltage amplitude ranging from 70 V to 200 V and an intensity ranging from 0.1 mA to 10 mA,

[0074] the pulses each having a duration (tpUke) between 0.2 ms and 1 s, with a rest interval (Toff) between them between 1 ms and 1000 ms,

[0075] the supplied current having a duty cycle (tpulse / (tpulse+Toff)) varying from 2% to 98%, where tpulse denotes the duration of a pulse and Toff the interval between two successive pulses,

[0076] The surface area of ​​the electrode(s) (2) in contact with the keratinous materials varies from 0.1 to 20 cm2,

[0077] the device is held in the hand,

[0078] it comprises a topical application of the composition to the target area before the application of the electric current and / or during said application,

[0079] It consists of manually moving the electrode(s) of the device over the target area while subjecting the latter to said electrical current pulses,

[0080] The exposure of the target area of ​​the skin is carried out for a duration between 2 minutes and 10 minutes,

[0081] The pulses have a pulse duration of Ton between 2 ms and 1000 ms,

[0082] The electric current density applied by the electrode ranges from 0.2 mA / cm2 to 50 mA / cm2,

[0083] the non-polymer active ingredient comprises a hydrophilic or lipophilic group,

[0084] the non-polymer active ingredient has a log P between -5 and 4,

[0085] the non-polymer active ingredient is chosen from compounds derived from pyrimidine or xanthine,

[0086] The non-polymer active ingredient is selected from 2,4-diamino-6-piperidinopyrimidine-3-oxide, 2,4-diaminopyrimidine 3-oxide, theophylline, caffeine or a mixture thereof.

[0087] The value of a logP represents the partition coefficient of a compound. It can be determined according to the method described in the article by Meylan and Howard, "Atom / Fragment contribution method for estimating octanol-water partition coefficient," J. Pharm. Sci., 84, 83-92 (1995). This value can also be calculated by commercially available software that determines the logP value from the structure of the molecule. For example, the Epiwin software from the United States Environmental Protection Agency can be cited. Description of the figures

[0088] [Fig.1]

[0089] [Fig. 1] is a schematic diagram of the method according to the invention implemented with the Newa ® device marketed by EndyMed,

[0090] [Fig.2]

[0091] [Fig.2] is a schematic diagram of the method according to the invention implemented with the RF Ultrasonic Device, model EH-XR10 ® marketed by Panasonic,

[0092] [Fig.3]

[0093] Fig. 3 describes the experimental protocol for preparing the samples.

[0094] [Fig.4],

[0095] [Fig.4] shows the cutaneous absorption of caffeine after one hour (in pg / cm2),

[0096] [Fig.5],

[0097] Figure 5 shows the cutaneous absorption of minoxidil after one hour (in pg / cm²). Example

[0098] The devices used in this example are the commercial Newa ® devices marketed by EndyMed and RF Ultrasonic Device, model EH-XR10 ® marketed by Panasonic.

[0099] The implemented composition is described in Table 1.

[0100] The composition in gel form is prepared from the weight proportions described below. Percentages are by weight relative to the total weight of the composition. The percentage of active ingredients (AI) is also specified where necessary.

[0101] The molecular weight in MW weight is expressed in Da. [Tables 1] Compounds Quantity (g) Properties CAFFEINE (1,3,7-TRIMETHYL XANTHINE) ANHYDROUS called "caffeine" 0.5 MW: 194 logP: -0.07 2,4-DIAMINO 6-PIPERIDINO PY-RIMIDINE N-OXIDE Called "minoxidil" 0.5 MW: 209 LogP: 0.87 ACRYLATES / C-10-C30 ALKYL ACRYLATE CROSSPOLYMER 3 — ETHYL ALCOHOL 96° UNDENATURED 40 — 2 METHYLPENTANE-2,4-DIOL 15 — DEIONIZED WATER q.s. 100 —

[0102] As shown in Figures 1 and 2, a sample of human skin 1 is fixed at its periphery to a Franz cell 2, so that an exposure surface 3 is exposed to radio frequencies. Specific operating conditions are assigned to each device. The RF application is performed remotely, and the sample is then placed on the Franz cell.

[0103] The following skin samples are prepared:

[0104] “Passive”: The sample is treated solely by composition.

[0105] “Stripped”: The sample is treated by stripping.

[0106] “Newa”: Skin treated with Newa® and the composition for 1 min. Then, the composition remains on the skin for Ih.

[0107] “Panasonic”: Skin co-treated with Panasonic (Radiofrequency + Ultrasound mode) and with the composition for 1 minute. Then, the composition remains on the skin for 1 hour.

[0108] The detailed protocol is shown in [Fig.3].

[0109] Fig. 4 shows the caffeine absorption profile in the stratum corneum (SC), epidermis, dermis, and the cumulative absorption in the stratum corneum, epidermis, and dermis.

[0110] Fig. 5 shows the absorption profile of minoxidil in the stratum comeum (SC), epidermis, dermis, and cumulative absorption in the stratum comeum, epidermis, and dermis.

[0111] To measure the absorption profiles of caffeine and minoxidil, the analytical device is used under the following operating conditions: An LC-MS / MS coupling is used to quantify caffeine and minoxidil in the skin compartments in order to establish the absorption profile. The analysis of the two molecules is performed using the same analytical method, the mobile phases of which are methanol and a mixture of water + 0.1 wt% formic acid. The stationary phase is a 50 mm long, 2.1 mm diameter C18 column with 2.7 µm particles. The ionization source used is positive ESI. To allow for optimal chromatographic results, the injection is performed in gradient.

[0112] Finally, we observe an increase of more than double: for minoxidil which hardly penetrates when applied topically, an increase of more than 20 times and for caffeine, an increase of more than 5 times.

Claims

Claims

1. A method of non-therapeutic, cosmetic treatment of the skin, comprising: a. Applying, to a target area of ​​the skin, a cosmetic composition comprising a non-polymeric cosmetic active agent having a molecular weight by weight ranging from 100 Da to 700 Da, b. Exposing the target area of ​​the skin to a succession of pulses of an electric current, the pulses having a frequency of between 100 kHz and 100 MHz and the electric current being supplied by a bipolar radiofrequency cosmetic device having at least one electrode and at least one counter-electrode.

2. The method of claim 1, wherein the electric current has a voltage amplitude ranging from 70 V to 200 V and an intensity ranging from 0.1 mA to 10 mA.

3. A method according to any preceding claim, the pulses each having a duration (tpUke) of between 0.2 ms and 1 s, with a rest interval (Toff) between them of between 1 ms and 1000

4. ms. Method according to any one of the preceding claims, the supplied current having a duty cycle (tpulse / (tpulse+Toff)) varying from 2% to 98%, where tpulse denotes the duration of a pulse and Toff the interval between two successive pulses.

5. Method according to any one of the preceding claims, the surface area of ​​the electrode(s) (2) in contact with the keratin materials varying from 0.1 to 20 cm2.

6. A method according to any preceding claim, the device being hand-held.

7. A method according to any preceding claim, comprising topical application of the composition to the target area prior to and / or during application of the electrical current.

8. A method according to any preceding claim, comprising manually moving the electrode(s) of the device on the target area while subjecting the latter to said electric current pulses.

9. A method according to any preceding claim, wherein the exposure of the target area of ​​the skin is carried out for a period of between 2 minutes and 10 minutes.

10. A method according to any preceding claim, the pulses having a pulse duration Ton comprised between 2 ms and 1000 ms.

11. A method according to any preceding claim, wherein the electric current density applied by the electrode ranges from 0.2 mA / cm2 to 50 mA / cm2.

12. Method according to any one of the preceding claims, the non-polymeric active agent comprising a hydrophilic or lipophilic group.

13. A method according to any one of the preceding claims, the non-polymeric active having a log P of -5 to 4.

14. Method according to any one of the preceding claims, the non-polymeric active agent being chosen from compounds derived from pyrimidine or xanthine.

15. A method according to any one of the preceding claims, the non-polymeric active agent being chosen from 2,4-diamino-6-piperidino pyrimidine-3-oxide, 2,4-diaminopyrimidine 3-oxide, theophylline, caffeine or a mixture thereof.

16. Assembly for carrying out the method according to any one of the preceding claims comprising a radiofrequency cosmetic device generating electrical pulses of a frequency between 100 kHz and 100 MHz and a cosmetic composition comprising a non-polymeric cosmetic active ingredient having a molecular weight by weight ranging from 100 Da to 700 Da.

Citation Information

Patent Citations

  • Radio frequency beauty treatment handle

    CN107998509A

  • High-frequency radio-frequency micro-vibration beauty instrument

    CN108452436A

  • New type skin beautifying instrument

    CN110141355A

  • Multifunctional skin beautifying instrument

    CN111616794A

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    CN112007279A