Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Liposomes
Patent
1988-06-20
1989-11-28
Page, Thurman K.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Liposomes
424941, 424449, A61K 3722
Patent
active
048836702
DESCRIPTION:
BRIEF SUMMARY
The present invention relates to cosmetic preparations containing soluble ubidecarenones prepared by dispersing in aqueous media mixtures having different ratios of ubidecarenones and acyl derivatives of 2-amino-ethansulphonic acid.
The ubidecarenones form an important class of liposoluble vitaminic principles, particularly 2,3-dimethoxy-5-methyl-6-decaprenyl-1,4-benzoquinone, known as ubidecarenone-10, localized at the mitochondrial level, plays a key-role in mammals in the electron-transfer system and more generally in the energy production.
Because of said important metabolic roles, the ubiquinone-10 is widely used in a large number of cardiac pathologies, protecting the myocardium from ischemic phenomena and preserving the functions thereof.
Moreover, because of the ability of ubidecarenone-10 of influencing both the tissutal respiration and the peroxidative phenomena of the cellular membranes, said vitamin is particularly interesting for the prevention of tissutal aging phenomena, particularly of the skin, which the recent biochemical knowledge ascribe, inter alia, to the action of free radicals, responsible of the structural alteration of the membrane lipids.
The development of biocompatible, hydrosoluble formulations is of particular interest for a better bioavailability of ubidecarenone-10 both in the pharmaceutical and cosmetic use.
The present invention concerns the development of a system able to carry in aqueous media the ubidecarenones, thanks to the interaction with amphipatic ions of general formula RNH--CH.sub.2 --CH.sub.2 --SO.sub.3, wherein R is an acyl radical having more than 5 carbon atoms, preferably a natural fatty acid of the normal, iso, anteiso series or cycloalkyl, saturated or unsaturated having from 8 to 26 carbon atoms. This class of amphipatic molecules is surprisingly able to carry the ubidecarenones in water, in the form of micellar and/or liposomial aggregates, even using an equimolar ratio of the two compounds.
A molar excess of the amphipatic solubilizing species is preferably used, from 2 to 4 times higher than the vitamin, said conditions granting a better and faster solubilization.
The preparation of hydrosoluble ubidecarenones may be carried out in different ways, for instance by sonicating an aqueous solution of the amphipatic species, to which the ubidecarenone is added or preferably by dispersing in water, under vigorous stirring, a mixture of ubidecarenone and N-acyl-2-amino-ethanesulphonate, prepared by evaporation of a solution of the two compounds in an organic solvent, in which both are soluble.
The micellar and/or liposomial systems so prepared are stable over long periods of time, even at extremely low or high environmental temperatures, that may be moreover lyophilized, yielding generally materials of waxy consistency, easily soluble in water by simple stirring.
The advantages attained by the invention in the cosmetic use are:
(a) the possibility of using hydrating, non-oily preparations, also in combination with other active principles;
(b) a good absorption of the active principle by the derma, because of its micellar and/or liposomial organization;
(c) a good tolerability even in prolonged treatments;
(d) the possibility of sterilizing by filtration the preparation thanks to its reduced size and to the stability of the micellar and/or liposomial aggregates;
(e) the possibility of modulating the characteristics of the preparation by changing the acyl residues of the solubilizing agent.
The invention provides therefore cosmetic compositions containing as the active principle compounds of ubidecarenone and N-acyl-2-amino-ethanesulphonates optionally in admixture with conventional cosmetic excipients.
The compositions of ubidecarenone and N-acyl-2-aminoethansulphonates find specific use in the cosmetic field in the prevention of tissutal aging phenomena. Said action exerted by ubidecarenone is to be ascribed to a specific protective mechanism from the peroxidative phenomena on the double bonds of the membrane unsaturated fatty acids and to the specific role
REFERENCES:
patent: 4325942 (1982-04-01), Taki et al.
patent: 4617187 (1986-10-01), Okuyama et al.
patent: 4636381 (1987-01-01), Takeda et al.
patent: 4695465 (1987-09-01), Kigasawa et al.
patent: 4767624 (1988-08-01), Okuyama et al.
De Rosa Mario
Zappia Vincenzo
Arval S.p.A.
Page Thurman K.
Prater P. L.
Schneider Walter H.
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