Hydrated lipidic lamellar phases or liposomes based on ecdystero

Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Liposomes

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Details

424401, 424417, 4284022, 514181, 514182, 514844, A61K 9127

Patent

active

051982250

DESCRIPTION:

BRIEF SUMMARY
The present invention relates essentially to compositions based on hydrated lipidic lamellar phases or liposomes containing an ecdysteroid, preferably ecdysterone, or one of its derivatives; and cosmetic, pharmaceutical, in particular dermatological, phytosanitary compositions or compositions for sericulture incorporating it.
The ecdysteroids are a group of 2,3,14-trihydroxy-.DELTA.-7-6-ketosteroids. Mention may be made of .alpha.-ecdysone or (2.beta.,3.beta.,14.alpha.-22/R/, 25-pentahydroxy-7-cholesten-6-one); 2-deoxyecdysone or (3.beta.,14.beta.,22/R/, 25-tetrahydroxy-5.beta.-7-cholesten-6-one), ecdysterone or .beta.-ecdysone or 2.beta.,3.beta.,14,20.beta.,22,25-hexahydroxy-7-cholesten-6-one; .beta.-ecdysone-22-acetate or 20-hydroxyecdysone-22-acetate or 7-cholesten-2.beta.,3.beta.,14,20,22/R/,25-hexol-6-one-22-acetate; 5-hydroxyecdysterone or 5.beta.,7-cholesten-2.beta.,3.beta., 5,14,20,22/R/25-heptahydroxy-6-one; .beta.-2-deoxyecdysone or 3.beta.,14,20,22/R/25-pentahydroxy-5.beta.,7-cholesten-6-one. The ecdysteroids, and in particular ecdysterone (in some cases called .beta.-ecdysone or even crustecdysone) are well known in the literature and cited in the Merck Index, 10th edition, 1983, page 505, No. 3 470.
It is known that the ecdysteroids, and in particular ecdysterone, play an important role both in insects in the animal kingdom and in the plant kingdom. In insects, these hormones play a key role in growth and reproduction. Ecdysterone is implicated in particular in the various metamorphoses up to the formation of the adult insect (see CNRS publication: Biologie 1990, "Enjeux et Problematiques" by A. Berkaloff et al.).
In plants, the activity of these substances has not been completely elucidated. They seem to act on flowering (CIENCIA e Cultura (1980), volume 32, No. 10, pages 1384-1390).
Furthermore, the use of hydrated lipidic lamellar phases or liposomes in cosmetic or pharmaceutical, in particular dermatological compositions, in which various active ingredients are incorporated, is already known (FR-A-2 540 381).
It has now been discovered, in a quite surprising and unexpected manner, that the incorporation of an ecdysteroid, preferably ecdysterone, or a derivative of the said ecdysteroid, or a plant or animal extract containing the said ecdysteroid or ecdysteroid derivative, at least in part in hydrated lipidic lamellar phase or in liposomes, causes an exacerbated activity of this substance or this extract. This relates in addition, and also in a completely unexpected manner, to all known activities of the ecdysteroid previously mentioned or an extract containing the latter. An even more radical improvement of activity was observed with respect to the activity of regeneration of the cutaneous structure and of anti-aging activity.
Consequently, a synergistic effect is obtained by the incorporation of an ecdysteroid, preferably ecdysterone or an ecdysteroid derivative or a plant or animal extract containing the said ecdysteroid at least in part in hydrated lipidic lamellar phases or in liposomes.
Thus, the aim of the present invention is to resolve the novel technical problem consisting in the provision of a new formulation of ecdysteroid(s), preferably ecdysterone or a derivative of the said ecdysteroid, or a plant or animal extract containing the said ecdysteroid, making it possible to potentiate its efficacy so as to allow its use in cosmetic, pharmaceutical, in particular dermatological, compositions as well as in compositions for sericulture and phytosanitary compositions.
The present invention solves this novel technical problem satisfactorily for the first time.
Thus, in accordance with a first feature, the present invention provides a composition based on hydrated lipidic lamellar phases or liposomes, characterized in that the said hydrated lipidic lamellar phases or the said liposomes contain at least in part at least one ecdysteroid or an ecdysteroid derivative, or a plant or animal extract containing the said ecdysteroid or a derivative of the said ecdysteroid.
According to a particu

REFERENCES:
patent: 4427649 (1984-01-01), Dingle et al.
patent: 4485054 (1984-11-01), Mezei et al.
patent: 4508703 (1985-04-01), Rodztaiak
patent: 4891219 (1990-01-01), Karr, Jr. et al.

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