DESCRIPTION

The present invention relates to a formulation for the topical administration and in particular to a topical formulation in the form of a cream for the treatment of psoriasis containing a mixture of herbal extracts.

Psoriasis is a chronic inflammatory skin disease which 1 -2% of the world population is suffering from. It is more common among Scandinavian populations and less frequent among American Indians and Afroamericans. Both sexes suffer from the disease in the same way. Even if psoriasis could affect any part of the body, it prefers knees, elbows, scalp, inter-gluteal furrow, palms, soles. Looking at the statistics, it is noted that its spread, even if worldwide, is so distributed:

Scandinavian countries 7-8%

Australia 5-6%

Germany 4%

USA 3.2%

Canada 2-3%

Europe 2-3%

UK 2%

China 0.37%

Kuwait 0.11 %

Triggering factors which have been indicated: injuries, infective agents, drugs (such as lithium salts and β-blockers), cold climate, psychogenic factors (such as stress and ansiety conditions), metabolic disorders (such as diabetes mellitus and hypokalemia), endocrine factors, etc.

Some familiarity has been found in about 30% of cases.

Psoriasis is not an infective disease, but it can cause anyway difficulties in relationships with other people and then influence an optimal quality of life in many people suffering from it.

There are known several topical as well as systemic treatments which are used to decrease the discomfort caused by the disease and/or to temporarily eliminate the symptoms, but there are no therapies for the time being. The treatments include the application on the skin of softening agents and hydrating agents able to maintain the skin hydrated and mitigate the symptoms as well as phototherapy as well as the pharmacological treatment with antihystaminics, steroids, antiseptics for topical use, immunomodulators for topical use, antidepressants, vitamin D analogs and acetylsalicylic acid.

The pharmacological treatments have also the drawback of possible side effects which occur also by topical application due to the systemic adsorption of the active ingredients which are applied to injured skin, sometimes on particularly large areas. There is still the need of a topical treatment able to mitigate and/or significantly decrease the symptoms of psoriasis for long periods without showing undesired side effects.

The present invention fulfils this need providing a topical formulation, in particular a cream, based on herbal extracts able to efficiently mitigate and eliminate for long periods the symptoms of psoriasis.

Object of the present invention is a topical formulation containing a phytotherapeutic combination of Tilia tomentosa, preferably as glycerine macerate, Cedrus libani, preferably as tincture, Viola tricolor, preferably as tincture, Ribes nigrum, preferably as glycerine macerate, Secale cereale, preferably as glycerine macerate, Lavanda officinalis essential oil, bergamot essential oil and cajeput essential oil.

The topical formulation object of the present invention is particularly efficient for the treatment of psoriasis.

Tilia tomentosa has the neurovegetative system as preferential organ, showed sedative, antispasmodic properties, which may be due partly to farnesol, a terpene with neurosedative properties. By acting on the serotonine level, which contributes to increase, it is able to improve the mood and to promote an anxiolytic and mildly antidepressant activity. Furthermore, it has also depurative properties, by decreasing cholesterol and uric acid. Detailed information about the properties of Tilia tomentosa have been published by EMA in 2012 (Final assessment report on Tilia tomentosa Moench, flos).

Cedrus libani has organotropism for the skin and shows to be particularly suitable in case of dermatosis characterized by dry skin and itch. It improves tissue vascularization and oxygenation. Furthermore, it experimentally reduces cholesterolemia.

Viola tricolor has proved emollient properties and since the middle age its efficient properties in the treatment of skin disorders were known. It contains violanthin, salycilic acid, carotenoids binding and removing free radicals, so playing an important role on the immune system. Detailed information about the properties of Viola tricolor are reported in the monograph published by EMA in 201 1 (Final community herbal monograph on Viola tricolor L). Traditionally used for the treatment of several skin disorders, also its use for psoriasis in the form of infusion of the whole herb to be applied externally has been recently disclosed (Amenta et al., Fitoterapia 2000, 71 : 13- 120).

Ribes nigrum has organotropism for the adrenal gland. It is defined as an adaptogen plant, has the capacity to increase the efficacy of other plants and to act specifically on physiologic processes with the result of increasing the physical resistance against environmental stress and the general efficiency in situations of exceptional load. In a broad sense, it increases the organism's resistance to stress. The use of bud derivative is indicated in clinic events wherein the stimulation of the adrenal gland is needed, such as in allergic and inflammatory events. Experimental studies showed a remarkable inhibiting activity of the inflammatory processes. Detailed information about the properties of Ribes nigrum are reported in the monograph published by EMA in 2010 (Final community herbal monography on Ribes nigrum L, folium). Secale cereale has organotropism for both liver and skin, has antibiotic and healing properties at the dermal and epidermal level. In naturopathic medicine it is used as oral drops for the treatment of psoriasis in combination with Cedrus libani and Ficus carica.

Lavandula has healing and antiseptic properties, controls the nervous system, anxiety, depression, rejuvenates and nurses all kinds of skin. Detailed information about the properties of lavender essential oil are reported on the monograph published by EMA in 2012 (Final community herbal monograph on Lavandula angustifolia Miller, aetheroleum).

Bergamot contains dextrorotatory limonene, which has properties aimed to limit cell proliferation, in addition to induce apoptosis in cancer cells, useful for anxiety and depression and excellent antiseptic, and it is an optimum product for herpes sores. Cajeput has remarkable anti-inflammatory and antibiotic activity.

All the herbal components of the phytotherapeutic combination contained in the formulation object of the present invention are essential to achieve the desired efficacy in the treatment of psoriasis.

In fact, even if some herbal components are already used for the treatment of psoriasis, their efficacy is remarkably lower compared to the results obtained with the formulation object of the present invention. The relative volume ratios of the herbal components also vary within defined ranges to obtain the optimal efficiency even if the most characterizing and innovative feature of the present formulation is the qualitative composition of the phytotherapeutic combination.

In a preferred embodiment of the topical formulation object of the present invention, the relative volume ratios of each component of the phytotherapeutic combination are the following:

Tilia tomentosa 15-20%

Cedrus libani 20-40%

Viola tricolor 15-20%

Ribes nigrum 15-20%

Secale cereale 4-6%

Lavanda officinalis essential oil 1-1.5%

Bergamot essential oil 1.2-2%

Cajeput essential oil 0.6-1 %

the total being 100%.

Still more preferably, the relative volume ratios of each component of the phytotherapeutic combination are the following:

Tilia tomentosa 18.3%

Cedrus libani 36.5%

Viola tricolor 18.3%

Ribes nigrum 18.3%

Secale cereale 5.0%

Lavanda officinalis essential oil 1.2%

Bergamot essential oil 1.6%

Cajeput essential oil 0.8%

The topical formulation object of the present invention is preferably a cream but can be also a lotion, an ointment or another form suitable for the topical application on injured and/or irritated skin.

The formulation can contain also other herbal components as well as softening agents and hydrating agents conventionally used in the preparation of topical formulations, particularly in the preparation of creams.

The preparation of the topical formulations object of the present invention is carried out according to conventional techniques, for example by incorporating the herbal active components into a neutral vegetal cream base.

The formulation is applied onto the area to be treated two or three times a day up to disappearance of the symptoms of psoriasis. After the disappearance of the symptoms it is preferred to continue the treatment once a day to prevent or delay the eventual reappearance of the symptoms. The duration of the treatment will mainly depend on the severity and extent of the disease and can generally vary from 3/4 weeks to 2/3 months.

The efficacy of the topical formulation object of the present invention has been assessed by administration to on patients suffering from psoriasis of different severity on different parts of the body.

Some cases are reported herein after.

In all cases, a cream formulation containing a phytotherapeutic combination of Tilia tomentosa glycerine macerate (18.3% v/v), Cedrus libani tincture (36.5% v/v), Viola tricolor tincture (18.3% v/v), Ribes nigrum glycerine macerate (18.3% v/v), Secale cereale glycerine macerate (5.0% v/v), Lavanda officinalis essential oil (1.2% v/v), bergamot essential oil (1.6% v/v) and cajeput essential oil (0.8% v/v) was used. Case 1

Man, 50 years old, with palmar psoriasis.

Use of the cream two/three times a day with reduction of the sores after about a week of treatment and disappearance after about twenty days.

Then, the cream was administered once a day without reappearance of the sores. Case 2

Woman, 92 years old, with vulgar psoriasis on the pre-sacral area.

Use of the cream twice a day with improvement and disappearance of the itch after ten days. The treatment was continued for two months with complete disappearance of the sores and normalization of the skin.

No reappearance of the sores after four years.

Case 3

Man, 65 years old, suffering from palmar psoriasis with fissures.

Use of the cream two/three times a day with healing of the fissures in 15/20 days and disappearance of the sores after a month and a half.

The use of the cream was continued only in case of reappearance of the fissures, noting that the plaques tended to reappear less frequently when the cream was used in a more constant and prolonged manner. Case 4

Man, 46 years old, suffering from palmar psoriasis with fissures.

Use of the cream two/three times a day with complete healing of the fissures after about 20 days. After suspension of the treatment the fissures tended to form again, but they did not form again by using the cream once a day.

The treatment was suspended for four months without relapses.

Case 5

Woman, 75 years old, with vulgar psoriasis on gluteus, pre-sacral area and abdomen.

Use of the cream on half body only with remission of itch and reduction of plaques after 20 days. After a month and a half the skin remained slightly irritated but smooth and without itching in the plaque area.

The other untreated half of the body was unchanged.

Case 6

Man, 70 years old, with a large psoriasis plaque on the pre-sacral area, with remarkable thickening of the skin and considerable white plaques.

Use of the cream discontinuously with disappearance of the plaques after about a month but tissue thickened and irritated.

Case 7

Man, 45 years old, with psoriasis plaques on both legs and elbows.

Use of the cream once a day with clear improvement of the treated area even if skin irritation remains.

Case 8 (comparative)

A patient with psoriasis plaques on gluteus was treated with a mixture of Cedrus libani, Viola tricolor and Ribes nigrum for 30 days without significant improvements. By using the cream object of the present invention a remarkable improvement of the treated area was obtained after only 20 days of treatment.