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1. WO2020117163 - LIPOSOMES ET ÉTHOSOMES CHARGÉS AVEC DE L'ACIDE ROSMARINIQUE APPROPRIÉS POUR UNE UTILISATION DANS LES COSMÉTIQUES

Note: Texte fondé sur des processus automatiques de reconnaissance optique de caractères. Seule la version PDF a une valeur juridique

[ EN ]

LIPOSOMES AND ETHOSOMES CHARGED WITH ROSMARINIC ACID SUITABLE FOR

USE IN COSMETICS

TECHNICAL FIELD

The present invention relates to liposomes or ethosomes charged with rosmarinic acid and the usage of said liposomes or ethosomes, charged with rosmarinic acid, in prevention of aging of skin or in treatment of skin aging or in elimination of the symptoms due to aging of skin.

PRIOR ART

Human skin shows selective permeability for the penetration of pluralities of drugs. The uppermost layer of the skin, namely stratum corneum layer on the epidermis, functions as an important barrier for the penetration. While lipophilic drugs can penetrate through the skin, the penetration of hydrophilic drugs is very difficult. For increasing penetration through the skin, penetration enhancers are used and methods like phonophoresis, electroporation, iontophoresis, injection without needle and micro-needles are utilized.

Moreover, liposomes and ethosomes which can carry various drug molecules having hydrophilic, lipophilic and amphiphilic structure are drug carrier systems used in enhancing penetration.

Antioxidants are chemical structures which preserve their currencies in cosmetic care products and which become a greater focus of interest evey passing day. When scientific publications are examined, in skin care products, there are studies about pluralities of antioxidants which can be used for retarding occurrence of aging indications or for mitigating the occurring indications.

However, although each antioxidant substance has the chance to reach the consumer inside a cosmetic product after a suitable formulation has been developed, a formulation is needed which will chemically preserve the efficiency of a substance, mixture or herbal extract which shows antioxidant characteristic in the in vitro conditions. An important step to be realized is that the formulation and the effectiveness of the active substance in the formulation shall be preserved and the formulation shall be maintained stable during the shelf lifetime.

When the cosmetic compositions existing in the known state of the art are taken into consideration, it is observed that new formulations are needed which will provide penetration of antioxidant agents to the lower layers of the skin without deteriorating the effectiveness of said antioxidant agents.

As a result, because of all of the abovementioned problems, an improvement is required in the related technical field.

BRIEF DESCRIPTION OF THE INVENTION

The present invention relates to liposomes and/or ethosomes charged with rosmarinic acid, for eliminating the above mentioned disadvantages and for bringing new advantages to the related technical field.

An object of the present invention is to provide penetration of liposome and/or ethosome structures, charged with rosmarinic acid and which do not have toxic effects of the known antioxidants, to skin in an effective manner.

In order to realize the abovementioned objects and the objects which are to be deducted from the detailed description below, the present invention relates to liposomes and/or ethosomes, wherein said liposomes and/or ethosomes are charged with rosmarinic acid.

DETAILED DESCRIPTION OF THE INVENTION

As a result of the studies made in the direction of the above mentioned objects, the invention owners have detected an increase in the penetration of rosmarinic acid through the skin in the study of penetration of liposome and ethosome formulations, comprising rosmarinic acid, through mouse skin. Particularly by means of ethosome formulation, a statistically more meaningful effect has been detected. Besides, thanks to rosmarinic acid penetrated to the skin, the inhibition of the enzymes which lead to skin aging also becomes possible. Thanks to these, the present invention surpasses the known state of the art and shows superior technical effect.

Rosmarinic acid is a compound having a wide usage area as antioxidant by means of its free radical effect in cosmetic field, and in the studies made, it has shown more antioxidant activity when compared with high antioxidant effective compounds like vitamin E and like trolox which is the analog of vitamin E. Rosmarinic acid is a natural antioxidant and it is a compound which is more preferred to be used since it does not lead to toxicity which may be formed by synthetic antioxidants like buthyl hydroxy toluene (BHT), buthyl hydroxy anisol (BHA) and propyl gallate. It is an antioxidant which is effective in preventing formation of lipid peroxides which are formed by physical and chemical external factors and which occur as a result of being subjected to UV rays.

A preferred application of the present invention relates to ethosomes charged with rosmarinic acid.

A preferred application of the present invention relates to liposomes charged with rosmarinic acid.

In another application of the present invention, ethosomes and/or liposomes are made of lecithin. In a preferred application of the present invention, the ethosomes are prepared with soybean phosphaditile choline and the liposomes are prepared with dipalmitoil phosphotidil choline.

In a preferred application of the present invention, ethosomes or liposomes are obtained from phospholipids, for instance, from phosphaditile choline, phosphaditile cerine, dipalmitoil phosphaditile choline, soybean phosphaditile choline, phosphaditic acid in an independent manner from each other. In other words, the subject matter liposomes and ethosomes can be obtained from phospholipids which are different from each other.

Another application of the present invention relates to pharmaceutical compositions comprising liposomes or ethosomes charged with rosmarinic acid.

In a preferred application of the present invention, the pharmaceutical compositions, comprising liposomes or ethosomes charged with rosmarinic acid, may comprise at least one auxiliary substance in addition to said liposomes or ethosomes.

Said auxiliary substance can be selected from a group selected from solvents, dispersers, emulsifying agents, surfactants, binders, lubricants, suspending agents, buffering couples, diluents, gelling agents.

Another application of the present invention is to use for a method to be used in the treatment of skin aging for the liposomes or ethosomes charged with rosmarinic acid and /or in the elimination of symptoms led by skin aging.

Another application of the present invention is to use liposomes or ethosomes charged with rosmarinic acid for the treatment of skin aging and/or for the elimination of the symptoms led by skin aging.

Another application of the present invention is to use liposomes or ethosomes charged with rosmarinic acid or the pharmaceutical composition comprising these in preparation of a drug to be used in treatment of skin aging and/or in elimination of the symptoms led by skin aging.

Within the scope of this specification, it is aimed that the“comprising” statement mentions the“covering” statement.

In technically suitable locations, the applications of the invention can be joined.

The applications are described so as to comprise specific characteristics/elements here.

The specification moreover essentially covers the other applications comprising said characteristics/elements or formed by said characteristics/elements.

Similar technical references like patents and applications have been included to this document by means of reference.

Here, specifically and apparently described applications can form the basis of a disclaimer in a stand-alone manner or together with one or more other applications.

Now, the present invention will be described with reference to the examples given below which are only for examplary purposes and which shall not be interpreted in a manner delimiting the scope of the present invention in any manner.

EXAMPLES:

Example 1 : Penetration of ethosomes and liposomes charoed with rosmarinic acid throuoh mouse abdominal skin

It is known that our effective substance, which is rosmarinic acid, is a strong antioxidant. The inhibitor effect of the Rosmarinic acid amounts, obtained from studies of penetration through mouse abdominal skin by utilizing this characteristic, on the collagenase and elastase enzymes, induced in the presence of free radicals, has been measured by means of kits.

When the results are examined, ethosomes charged with rosmarinic acid have shown inhibition of 72.89±0.99% and 80.1 ±0.813% on collagenase and elastase enzymes. Statistically, a meaningful difference has been obtained between ethosome and liposome formulations. In both enzyme kit measurements, it has been observed that ethosomes are more effective formulations when compared with liposomes. It is considered that the reason of this is that the amount of rosmarinic acid, penetrating through skin, is greater in the case of ethosomes. Another reason is that in the structure of ethosomes, there is ethanol which increases fluidity of the lipids, existing in the skin, and which increases penetration.

Since the ethosomes, comprising lower doses of rosmarinic acid when compared with the solution form, show antioxidant effect at a difference which is not meaningful, this shows the success of the ethosome formulation. Besides, when the effects of the examples on the malondialdehite (MDA) are compared in their own, ethosomes show statistically meaningful difference with respect to the lower dose of rosmarinic acid solution, and the liposomes have been found to be with the same meaning as the solution. When compared with the control group, ethosomes have inhibited MDA formation and DNA damage in a meaningful degree. Moreover, by means of the sweeper effect of the free radicals, ethosomes have shown effect with the same meaning as the antioxidant BHT. The usage thereof as alternative to toxicity, which will be formed by synthetic antioxidant, is possible.