KR101831352B1 - Photosensitizer of indocyanine green-containing composition and compositions comprising the same - Google Patents

Abstract

The present invention relates to a method of inhibiting secretion of sebum by intense pulse light (IPL) or laser irradiation comprising at least one polyhydric alcohol selected from the group consisting of propylene glycol and ethoxydiglycol, To provide a photosensitizer of the green-containing composition. The present invention also provides a pharmaceutical composition for inhibiting sebum secretion or treating acne, which contains indocyanine green as an active ingredient, and a cosmetic composition for suppressing sebum secretion or improving acne, comprising the above photosensitizing agent.

Description

INDUSTRIAL APPLICABILITY A photosensitizer of indocyanine green-containing composition and a composition comprising the same,

The present invention relates to a photosensitizer of an indocyanine green-containing composition for inhibiting sebum secretion by intense pulse light (IPL) or laser irradiation or for treating acne. The present invention also relates to a pharmaceutical composition for inhibiting sebum secretion or treating acne and a cosmetic composition for suppressing sebum secretion or improving acne, which contains indocyanine green as an active ingredient and contains the above photosensitizing agent.

Acne is an inflammatory disease that occurs in the skin and hair follicles. It is caused by sebaceous gland enlargement and activation through environmental factors and hormones, excessive sebum production, abnormal keratinization process, and keratosis or hyperkeratosis of keratinocyte It acts as a primary cause. That is, if sebum is not secreted naturally and stays in the hair follicle together with keratin and cell debris, a characteristic lesion of acne will develop.

Indocyanine green is a chromophore selectively distributed only in the sebaceous glands. When IPL or laser of a specific wavelength (750 ~ 850 nm) is irradiated, energy is selectively converted into heat energy at the chromophore absorption site, Decreases sebum secretion by destroying developed sebaceous glands. Accordingly, methods of suppressing sebum secretion or treating acne by IPL or laser irradiation including a chromophore such as indocyanine green are known in various documents (International Patent Publication No. WO 2003/017824, U.S. Patent Application Publication No. 2006/0128771 ). Such a therapeutic method has the advantage of reducing sebum secretion itself and at the same time reducing undesirable damage (blisters, burns) of surrounding tissues, and thus can be usefully applied to suppress sebaceous glands and to treat (or alleviate) acne.

The present inventors have conducted various studies to develop indocyanine green-containing compositions for inhibiting sebum secretion or treating acne by more advanced IPL or laser irradiation. Surprisingly, the present inventors have found that when formulating a specific polyhydric alcohol or a mixture thereof with indocyanine green, the photosensitivity of indocyanine green is significantly increased, thereby inhibiting sebum secretion by IPL and laser irradiation or treating acne Activity can be effectively promoted.

Accordingly, it is an object of the present invention to provide a use of the specific polyhydric alcohol or a mixture thereof as a photosensitizing agent in an indocyanine green-containing composition for inhibiting sebum secretion by IPL or laser irradiation or for treating acne.

It is another object of the present invention to provide a pharmaceutical composition for suppressing sebum secretion or treating acne and a cosmetic composition for suppressing sebum secretion or improving acne, which comprises the specific polyhydric alcohol or a mixture thereof as a photosensitizing agent.

According to one aspect of the present invention there is provided an indocyanine green-containing composition for the prevention of sebum secretion by IPL or laser irradiation or for the treatment of acne, comprising polyhydric alcohol selected from the group consisting of propylene glycol and ethoxydiglycol A photosensitizer of the composition is provided.

According to another aspect of the present invention, there is provided a composition comprising: indocyanine green as an active ingredient; And a photosensitizer selected from the group consisting of propylene glycol and ethoxydiglycol. The pharmaceutical composition for inhibiting sebum secretion or treating acne by IPL or laser irradiation is provided.

According to still another aspect of the present invention, there is provided a composition comprising: indocyanine green as an active ingredient; And a photosensitizer selected from the group consisting of propylene glycol and ethoxydiglycol. The cosmetic composition for suppressing sebum secretion or improving acne by IPL or laser irradiation is provided.

According to the present invention, when a specific polyhydric alcohol or a mixture thereof, that is, propylene glycol and / or ethoxydiglycol, is formulated together with indocyanine green, the photosensitivity of indocyanine green after application of the skin is It has been found that by significantly increasing the IPL and laser irradiation wavelength of 750 to 850 nm, sebum secretion inhibition or acne treatment activity can be effectively promoted. Accordingly, the pharmaceutical composition and the cosmetic composition according to the present invention can be effectively used for inhibiting sebum secretion by IPL and laser irradiation or for treating (and alleviating) acne.

Figure 1 shows the absorbance measurement results of an indocyanine green 0.1% solution containing an alcohol or a polyhydric alcohol.
2 shows the results of absorbance measurements of a 0.1% solution of indocyanine green containing propylene glycol and ethoxydiglycol by concentration ((5% by weight to 50% by weight), respectively).
Figure 3 shows the absorbance measurements of a 0.1% solution of indocyanine green containing 20% by weight of propylene glycol, 10% by weight of ethoxydiglycol, and mixtures thereof.
4 is a graph showing the results of an emulsion composition containing 20% by weight of propylene glycol, 10% by weight of ethoxydiglycol and 0.1% by weight of indocyanine green, and also containing various emulsifiers by concentration (0.1% by weight to 3% This is the result of the absorbance measurement of the solution.
Figure 5 shows clinical trial results of 0.1% Indocyanine Green. FIG. 5A shows the result of a clinical trial using only 0.1% indocyanine green, and FIG. 5B shows the results of clinical tests using 20% by weight of propylene glycol, 10% by weight of ethoxydiglycol, 1% by weight of polysorbate 80, And 0.1% by weight of cyanine green.

The present invention relates to a method for inhibiting sebum secretion by IPL or laser irradiation comprising a polyhydric alcohol selected from the group consisting of propylene glycol and ethoxydiglycol, or a photosensitizing agent for an indocyanine green-containing composition for the treatment of acne to provide.

Propylene glycol and / or ethoxydiglycol can increase the photosensitivity of the indocyanine green-containing composition, thereby inhibiting sebum secretion or treating acne by IPL and laser irradiation at a wavelength of 750-850 nm Can be effectively promoted.

The photosensitizer according to the present invention may preferably be a mixture of propylene glycol and ethoxydiglycol. The weight ratio of propylene glycol to ethoxydiglycol is preferably 1.5 to 2.5: 1, more preferably 2: 1.

The present invention also provides a pharmaceutical composition for inhibiting sebum secretion or treating acne comprising the above photosensitizing agent and a cosmetic composition for suppressing sebum secretion or improving acne. Specifically, the present invention relates to a composition comprising indocyanine green as an active ingredient; And a photosensitizer selected from the group consisting of propylene glycol and ethoxydiglycol. The present invention also provides a pharmaceutical composition for inhibiting sebum secretion or treating acne by IPL or laser irradiation, ; And a photosensitizer selected from the group consisting of propylene glycol and ethoxydiglycol. The present invention provides a cosmetic composition for suppressing sebum secretion or improving acne by IPL or laser irradiation.

In the pharmaceutical composition or cosmetic composition according to the present invention, the photosensitizing agent may preferably be a mixture of propylene glycol and ethoxydiglycol. The weight ratio of propylene glycol to ethoxydiglycol is preferably 1.5 to 2.5: 1, more preferably 2: 1.

The pharmaceutical composition or cosmetic composition according to the present invention can further enhance the skin permeability of indocyanine green by containing an emulsifier. Such emulsifiers include emulsifiers commonly used in the art. Preferably, the pharmaceutical composition or cosmetic composition according to the present invention comprises polyoxyethylene (20) sorbitan monolaurate, polysorbate 20, polyoxyethylene (20) sorbitan monolaurate, Polyoxyethylene (20) sorbitan monopalmitate, Polysorbate 40, polyoxyethylene (20) sorbitan monostearate, Polysorbate 60), polyoxyethylene (20) sorbitan monopalmitate, , Polyoxyethylene (20) sorbitan monooleate, and polysorbate 80). And an emulsifier selected from the group consisting of polyethylene glycol hydrogenated castor oil (e.g., PEG-40 hydrogenated castor oil, PEG-60 hydrogenated castor oil, etc.). Among them, a composition containing polyoxyethylene (20) sorbitan monooleate can be preferably used as an emulsifier since the highest photosensitivity can be obtained.

The pharmaceutical composition of the present invention may comprise a delivery vehicle, such as a delivery vehicle, a delivery vehicle, an emulsion, and the like, and may contain a pharmaceutically acceptable carrier, Can be formulated into parenteral formulations. The pharmaceutically acceptable carrier may include an aqueous diluent such as purified water, sterilized water, phosphate buffered saline, or a solvent. In the pharmaceutical composition of the present invention, the dose of indocyanine green may be sufficient for suppressing sebum secretion or treatment of acne by IPL or laser irradiation. However, the amount of indocyanine green administered may be sufficient for the patient's condition, sebaceous secretion and / Type, and period of time. For example, the indocyanine green may be applied at a concentration of 0.05 to 3% by weight, preferably at a concentration of about 0.1% by weight, once IPL or laser irradiation.

As described above, the cosmetic composition according to the present invention includes indocyanine green, a photosensitizing agent, and optionally an emulsifier, and can be manufactured into various forms according to a method commonly used in the field of cosmetic compositions. For example, the cosmetic composition of the present invention may be in the form of a conventional cosmetic composition such as a solution, a suspension, an emulsion, and a cream. The cosmetic composition may be prepared by a conventional method together with a carrier or additives commonly used in cosmetics . The concentration of the indocyanine green in the cosmetic composition of the present invention may be 0.05 to 3% by weight, preferably about 0.1%. Of course, the concentration may vary depending on the desired sebum secretion inhibition or the degree of acne relieving activity and the like.

The pharmaceutical composition or cosmetic composition according to the present invention may contain 0.05 to 3% by weight of indocyanine green, 25 to 35% by weight of a photosensitizer, and 0.1 to 3% by weight of an emulsifier in water (for example, purified water). In one embodiment, the present invention provides a composition comprising: 0.1% by weight of indocyanine green; 20% by weight of propylene glycol; 10% by weight ethoxydiglycol; 1% by weight of polyoxyethylene (20) sorbitan monooleate; And 68.9% by weight of water, for inhibiting sebum secretion by IPL or laser irradiation or for treating acne. In another embodiment, the present invention provides a composition comprising: 0.1% by weight of indocyanine green; 20% by weight of propylene glycol; 10% by weight ethoxydiglycol; 1% by weight of polyoxyethylene (20) sorbitan monooleate; And 68.9% by weight of water, wherein the cosmetic composition for suppressing sebum secretion or improving acne by IPL or laser irradiation is provided.

Hereinafter, the present invention will be described in more detail with reference to examples. However, these examples are for illustrating the present invention, and the scope of the present invention is not limited to these examples.

Example 1. Evaluation of optical sensitivity to IPL or laser irradiation

The photosensitivity for IPL or laser irradiation was evaluated by measuring the absorbance at 810 nm using a UV-NIR spectrometer [UV-1800 (Ishima, Korea)].

0.1% by weight indocyanine green; Absorbance was measured at 810 nm on a diluent containing 10% by weight of each of ethanol, propylene glycol, glycerin, ethoxydiglycol, dipropylene glycol, butylene glycol, or polyethylene glycol-400 . A dilution of purified water containing 0.1% by weight of Indocyanine Green as a control was also measured. As a result, propylene glycol and ethoxydiglycol showed the highest absorbance values (see FIG. 1). The absorbance of propylene glycol and ethoxydiglycol was measured by the same method with different concentrations (5 wt.% To 50 wt.%). As a result, the absorbance of propylene glycol and ethoxydiglycol was found to be 20 wt% (20% by weight), propylene glycol (20% by weight), ethoxydiglycol (10% by weight) and mixtures thereof (propylene glycol 20% by weight, ethoxydiglycol Containing 10 wt% of lycoricol) was measured. As a result, a solution containing two substances together showed a higher absorbance than a solution containing a single substance (See FIG. 3).

 Based on the above results, it was confirmed that an aqueous solution containing 20% by weight of propylene glycol, 10% by weight of ethoxydiglycol, and 0.1% by weight of indocyanine green was added to the aqueous solution containing polysorbate 20, polysorbate 80, Absorbance was measured in the same manner by adding Bait 60, a Pigi-60 hydrogenated castor oil, or a Pigi-40 hydrogenated castor oil by concentration (0.1 wt% to 3 wt%). As a result, an aqueous solution containing 1 wt% of polysorbate 80 showed the highest absorbance value (see Fig. 4).

Thus, from the above results, it can be seen that the composition of 0.1 wt% indocyanine green, 20 wt% propylene glycol, 10 wt% ethoxydiglycol, 1 wt% polysorbate 80 and 68.9 wt% Or light sensitivity to laser irradiation.

Example 2. Clinical evaluation

Group A (0.1% by weight indocyanine green, 99.9% by weight purified water), group B (20% by weight propylene glycol, ethoxydiglycerol, 10% by weight of Cole, 1% by weight of polysorbate 80, 0.1% by weight of indocyanine green, and 68.9% by weight of purified water). Exclusion criteria were pregnancy or lactation, simple squamous cell carcinoma, and infected skin lesions. During the treatment period, the use of topical or oral medication for the treatment of acne was prohibited. Before treatment, the face was wiped off with alcohol after cleansing, and then two types of 0.1% indocyanine green solution of each group were massaged for 30 minutes on each face. Long wavelength pulse laser diode (MeDioStar miXT, Asclepion, Germany) was used to irradiate the entire surface of the 810 nm wavelength. The same procedure was repeated four times at intervals of two weeks. Results Measurements were taken with a digital camera under the same conditions (same light, room, camera). The sebum was measured after 8 weeks using a sebum analyzer (Sebumeter SM 815, Epigem, Korea). Results Data were assessed using the Kruskal-Wallis test and p values less than 0.05 were defined as statistically significant.

The clinical evaluation result is shown in Fig. As can be seen from FIG. 5, when the solution containing 99.9% by weight of purified water and 0.1% by weight of indocyanine green was applied, the sebum secretion amount was reduced by an average of 12%, but the solution containing the photosensitizing agent according to the present invention The amount of sebum secretion decreased by 34%. In addition, visual acne improvement was also higher.

Claims (14)

Indocyanine green as an active ingredient; A photosensitizer selected from the group consisting of propylene glycol and ethoxydiglycol; And a polyoxyethylene (20) sorbitan monooleate as an emulsifier. The pharmaceutical composition for inhibiting sebum secretion or treating acne by intense pulse light or laser irradiation. The pharmaceutical composition according to claim 1, wherein the photosensitizer is a mixture of propylene glycol and ethoxydiglycol. The pharmaceutical composition according to claim 2, wherein the weight ratio of propylene glycol to ethoxydiglycol is 1.5 to 2.5: 1. 4. The pharmaceutical composition according to claim 3, wherein the weight ratio of propylene glycol to ethoxydiglycol is 2: 1. delete delete The pharmaceutical composition according to claim 1, which comprises 0.05 to 3% by weight of indocyanine green, 25 to 35% by weight of a photosensitizing agent, and 0.1 to 3% by weight of an emulsifier in water. Indocyanine green as an active ingredient; A photosensitizer selected from the group consisting of propylene glycol and ethoxydiglycol; And a polyoxyethylene (20) sorbitan monooleate as an emulsifier. The composition of the present invention is a cosmetic composition for suppressing sebum secretion or improving acne by intense pulse light or laser irradiation. The cosmetic composition according to claim 8, wherein the photosensitizer is a mixture of propylene glycol and ethoxydiglycol. The cosmetic composition according to claim 9, wherein the weight ratio of propylene glycol to ethoxydiglycol is 1.5 to 2.5: 1. 11. The cosmetic composition according to claim 10, wherein the weight ratio of propylene glycol to ethoxydiglycol is 2: 1. delete delete The cosmetic composition according to claim 8, which comprises 0.05 to 3% by weight of indocyanine green, 25 to 35% by weight of a photosensitizer, and 0.1 to 3% by weight of an emulsifier in water.

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