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(12) Patent Application Publication (10) Pub. No.: US 2012/0114719 A1 Morariu (43) Pub US 2012O114719A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2012/0114719 A1 Morariu (43) Pub. Date: May 10, 2012 (54) TOPICAL MACQUIBERRY FORMULATION Publication Classification (51) Int. Cl. (75) Inventor: Marius Morariu, Brooklyn, NY 46R 8/97 (2006.01) (US) A61O 1/10 (2006.01) A61O 19/08 (2006.01) (73) Assignee: TRACE MARTYN 14 2.99 3. INTERNATIONAL, LLC, New (2006.01) York, NY (US A6IR 8/14 (2006.01) ork, NY (US) A61O 1/02 (2006.01) B82Y 99/00 (2011.01) (21) Appl. No.: 13/226,834 (52) U.S. Cl. ........... 424/401; 424/777; 424/63; 426/590; 44/275; 426/541; 977/798; 977/926 (22) Filed: Sep. 7, 2011 (57) ABSTRACT O O The present invention provides a topical formulation and Related U.S. Application Data method ofuse where the formulation comprises macquiberry (63) Continuation of application No. 11/525.288, filed on or a macquiberry extract containing anthocyanins having a Sep. 21, 2006, now abandoned very high oxygen radical absorbance capacity (ORAC). The • 1- us s formulation provides the macqui berry in a stabilized form which includes a glucuronide or glycuronide, a photostabi (60) Provisional application No. 60/719,530, filed on Sep. lizing agent, encapsulation, or light- and/or air-blocking 21, 2005. packaging. US 2012/01 14719 A1 May 10, 2012 TOPICAL MACQUIBERRY FORMULATION equivalents (TE)/g. In most fruits, ORAC values ranged from 7.8 to 33.7 umoleTE/g of fresh berries and the ORAC values of the leaves range from 69.7 to 182.2 umoleTE/g (Wang SY. 0001. This application claims priority pursuant to 35 U.S. Lin HS.J.Agric Food Chem. 2000 February; 48(2): 140-6.). C. S 119 from Provisional Patent Application Ser. No. 60/719, Comparatively, a fruit with an ORAC value of 8 umol TE/g of 530 filed Sep. 21, 2005, the entire disclosure of which is fresh berries will have an ORAC value of about 35umol TE/g hereby incorporated by reference. of driedberries and an ORAC of 34umol TE/g of freshberries corresponds with an ORAC of 162 ummol TE/g dried matter. FIELD OF THE INVENTION Black raspberries have a very high ORAC of 77 umole TE/g 0002 The present invention relates to the topical applica while boysenberries have an ORAC of 48 umole TE/g, and tion of compositions containing macqui berry or macqui red raspberries and blueberries have an ORAC of 24 and 23 berry extract in a topical formulation for the prevention and/ umole TE/g, respectively. (http://www.deckerfarm.com/anti or treatment of damage to skin, particularly skin damage oxidants.html). Acai is another fruit having a high ORAC resulting from chronoaging and photoaging. content (167 ORAC units/g according to Brunswick Labora tories). Other fruit having high ORAC values include pome BACKGROUND OF THE INVENTION granate (33.1 uplummole TE/g) and aronia berry (62 Lummole TE/g) as well as whole coffee fruit extract (6250 ORAC units 0003 Skin is subject to abuse by many extrinsic (environ per gram according to Brunswick Laboratories). The stage at mental) factors as well as intrinsic factors. A common extrin which the plant is harvested affects the ORAC value. Black sic factor is exposure to ultraviolet radiation. Whether extrin berries have their highest ORAC values during the green sic or intrinsic, the abuse results in skin aging. Skin aging stages, whereas red raspberries have their highest ORAC happens in two ways: (1) through the natural aging process values when ripe. The ORAC may be obtained by using the which dermatologists call chronological aging (also known method described by the U.S. Department of Agriculture's as chronoaging); and (2) through UV rays in Sunlight accel Agricultural Research Service (Prior and Cao,83(4) J. AOAC erating the aging process which dermatologists call photoag INT. 950-6 (2000)). Additionally, testing for ORAC, ing. Chronoaging results in thinning, loss of elasticity and H-ORAC, N-ORAC, S-ORAC, and ORAC-E (high through general degradation of skin. As the skin naturally ages, there put ORAC for oil-in-water emulsion) is available from Brun is a reduction in the cells and blood vessels that supply the swick Laboratories (www.brunswicklabs.com). skin. There is also a flattening of the dermal-epidermal junc 0007 Anthocyanins have been formulated intopical form. tion which results in weaker mechanical resistance. As a For example, U.S. Pat. Pub. 2004/0022818 provides a skin consequence, older persons are more Susceptive to blister care composition comprising fruit particles. Red and blue formation in cases of mechanical traumas or disease pro fruits, as well as other fruits which contain anthocyanins are cesses (Oikarinen et al., Photodermatal. Photoimmunol. Pho included in this composition. Similarly, U.S. Pub. 2003/ tomed., 7:3-4 (1990)). 0161897 and U.S. Pat. No. 6,361,786 provide a topical anti 0004. By contrast, photoaging, or premature aging, is a microbial factor having fruit juice (cranberry, Aronia berry, process in which the skin changes in appearance as a result of blackberry, grape or blueberry) and polyvinylprolidinone. A repeated exposure to Sunlight. Typically, photoaging occurs topical oil-in-water emulsion containing a surfactant/emulsi in areas of habitual exposure, Such as the scalp, face, ears, fier and a lipid, which may be an anthocyanin-containing neck, chest, forearms and hands. The changes associated with berry extract, is provided by WO 98/05294. U.S. Pat. No. photoaging include elastosis, atrophy, wrinkling, vascular 5,011.855 provides a cosmetic composition having a-lino changes (diffuse erythema, ecchymoses, and telangiectasias), lenic acid and an oil extracted from Ribes genus fruits. pigmentary changes (lentigines, freckles, and areas of hypo 0008. However, there are problems associated with these and hyper-pigmentation), and the development of seborrheic and other uses of antioxidants in a topical formulation. Par keratosis, actinic keratosis, comedones and cysts. ticularly, antioxidants are readily oxidized and lose their anti 0005 Antioxidants are useful agents treating the skin from oxidant capacity. Additionally, some of the oxidation prod damage caused by chronoaging and photoaging. The most ucts of antioxidants will have a deleterious effect; for useful antioxidants are those that provide the highest capacity example, vitamin C oxidizes to dehydroascorbate which is to absorb free radicals. The oxygen radical absorbance capac known to lead to the formation of advanced glycation end ity (ORAC) is a measurement of this (Dreher F, Maibach H. products (AGES) and therefore increase the signs of aging Curr Probl Dermatol. 2001:29:157-64.) Anthocyanins area skin. type of antioxidants that generally encompass a class of fla vonoid compounds that are naturally occurring, water 0009. Therefore, a topical formulation containing an anti soluble compounds, responsible for the red, purple, and blue oxidant with a much higher ORAC and consequently greater colors of many fruits, vegetables, cereal grains, and flowers. anti-oxidant power is needed in combination with a formula Most anthocyanins have a high ORAC rating compared to tion that protects the antioxidant from degradation and loss of other antioxidants and make them particularly useful for their the anti-oxidative power to be used in treating and protecting topical antioxidative properties. Additionally, anthocyanins the skin. are collagenase inhibitors, which helps in the prevention and reduction of wrinkles, increase in skin elasticity, etc., which SUMMARY OF THE INVENTION are caused by a reduction in skin collagen. 0006 For ripe berries, a rich source of anthocyanin anti 0010. It is an object of the present invention to provide a oxidants, there is generally a linear relationship between composition and method for treating and protecting the skin. ORAC values and anthocyanin content. High ORAC ratings 0011. In accordance therewith, a method and composition are generally defined as greater than 25 umole of Trolox is provided for treating skin, comprising a topical composi US 2012/01 14719 A1 May 10, 2012 tion containing macqui berry in a stabilized form and the administration of an effective amount of the topical compo TABLE 1-continued sition to the skin. 0012. In a preferred embodiment, the stabilized form of ORAC value macqui berry includes a macquiberry or macqui berry extract Fruit (Imole TEg) and a glucuronide or glycuronide, or a dermatologically aronia berry 62 acceptable salt thereof. boysenberry 48 pomegranate 33 0013. In another embodiment, the stabilized form of mac red raspbererry 24 quiberry includes a macqui berry or macqui berry extract or blueberry 23 a dermatologically acceptable salt thereof, which has been encapsulated or placed in light-blocking packaging. 0014. Additional agents such as NADH, an antioxidant, an 0020. The macqui berry is particularly advantageous AGE inhibitor, a collagen enhancing agent, a mitochondrial when used as a whole berry or partially purified extract. The resuscitant, a light reflecting agent or a Sunscreen, an anti berry or extract may be used as a liquid or juice, pulp, or in edemic agent, a glutathione or an inducer thereof, an anti solid, dried form. Other compounds within the macqui berry inflammatory agent, a phenylpropanoid glycoside, a depig are also advantageous for use in the topical formulation of the menting agent or agent addressing hyperpigmentation, a present invention Macnuiliberry contains a number of antho skin-protective lipid, hyaluronic acid, an alpha hydroxy acid, cyanins including: delfinidin-3-glucoarabinoside-5-gluco an agent useful for treating hormonal decline, an anti-acne side; delfinidin 3,5-diglucoside; cyanidine-3-glucoarabino agent, an agent altering lipolytic activity, an anti-cellulitic side-5-glucoside; cyanidine-3,5-diglucoside; delfinidin-3- agent, an agent altering anti-capillary-fragility, an anti glucoarabinoside; delfinidin-5-glucoarabinoside; delfinidin elastase agent. an anti-erythema agent; or an agent that raises 3-glucoside; cyaniding-3-glucoarabinoside; and cyaniding cyclic AMP may additionally be incorporated into the macqui 3-glucoside.
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