USOO9463153B2 (12) United States Patent (10) Patent No.: US 9,463,153 B2 Morariu (45) Date of Patent: Oct. 11, 2016 (54) TOPICAL MACQUI BERRY FORMULATION A61K 8/44 (2013.01); A61K 8/46 (2013.01); A61K 8/4913 (2013.01); A61K 8/602 (71) Applicant: Tracie Martyn INTERNATIONAL, (2013.01); A61K 36/185 (2013.01); A61O I/00 LLC, Brooklyn, NY (US) (2013.01); A61O 19/00 (2013.01); A61O 19/08 (2013.01); A61 K 2800/26 (2013.01); (72) Inventor: Marius Morariu, Brooklyn, NY (US) A61 K 2800/52 (2013.01); A6 IK 2800/522 (2013.01) (73) Assignee: tadt,Marge International LLC, (58) Field of Classification Search (*) Notice: Subject to any disclaimer, the term of this See application file for complete search history. patent is extended or adjusted under 35 U.S.C. 154(b) by 0 days. (56) References Cited (21) Appl. No.: 14/480,182 U.S. PATENT DOCUMENTS (22) Filed: Sep. 8, 2014 2002/0187114 A1*ck 12/2002 Mankovitz. ............. A61ks: 2005/00 13880 A1* 1/2005 Magnuson et al. ........... 424,732 (65) Prior Publication Data US 2014/0377338A1 Dec. 25, 2014 OTHER PUBLICATIONS Related U.S. Application Data Miranda-Rottmann et al. Juice and phenolic fractions of the berry Aristotelia chilensis inhibit LDL oxidation in vitro and protect (63) Continuation of application No. 13/226,834, filed on human endothelial cells against oxidative stress. Journal of agricul Sep. 7, 2011, now Pat. No. 8,828,458, which is a tural and food chemistry, 50 (26): 7542-7, 2002.* continuation of application No. 1 1/525,288, filed on Sep. 21, 2006, now abandoned. * cited by examiner (60) Provisional application No. 60/719,530, filed on Sep. 21, 2005. Primary Examiner — Qiuwen Mi (74) Attorney, Agent, or Firm — Bryan D. Zerhusen; (51) Int. Cl. Locke Lord LLP A6 IK 36/00 (2006.01) A 6LX 8/97 (2006.01) (57) ABSTRACT A6 IK 8/44 (2006.01) A6 IK 8/46 (2006.01) The present invention provides a topical formulation and A6 IK 8/49 (2006.01) method of use where the formulation comprises macqui A6 IK 8/60 (2006.01) berry or a macqui berry extract containing anthocyanins A6 IK 36/185 (2006.01) having a very high oxygen radical absorbance capacity A61O 19/08 (2006.01) (ORAC). The formulation provides the macqui berry in a A6 IK 8/14 (2006.01) stabilized form which includes a glucuronide or gly A61O I/00 (2006.01) curonide, a photostabilizing agent, encapsulation, or light A61O 19/00 (2006.01) and/or air-blocking packaging. (52) U.S. Cl. CPC. A61K 8/97 (2013.01); A61K 8/14 (2013.01); 3 Claims, No Drawings US 9,463,153 B2 1. 2 TOPICAL MACQUI BERRY FORMULATION the prevention and reduction of wrinkles, increase in skin elasticity, etc., which are caused by a reduction in skin CROSS-REFERENCE TO RELATED collagen. APPLICATIONS For ripe berries, a rich source of anthocyanin antioxidants, there is generally a linear relationship between ORAC values and anthocyanin content. High ORAC ratings are This application is a Continuation application of U.S. generally defined as greater than 25umole of Trolox equiva patent application Ser. No. 13/226,834, filed Oct. 7, 2011, lents (TE)/g. In most fruits, ORAC values ranged from 7.8 now Issued Patent No. 8,828,458, issue date: Sep. 9, 2014: to 33.7 umole TE/g of fresh berries and the ORAC values of which is a Continuation application of U.S. patent applica the leaves range from 69.7 to 182.2 mole TE/g (Wang SY. tion Ser. No. 11/525,288, filed Sep. 21, 2006, abandoned; 10 Lin H S., J Agric Food Chem. 2000 February; 48(2):140-6). which claims priority to Provisional Patent Application No. Comparatively, a fruit with an ORAC value of 8 umol TE/g 60/719.530, filed Sep. 21, 2005, the entire contents of the of fresh berries will have an ORAC value of about 35umol aforementioned applications are hereby incorporated herein TE/g of driedberries and an ORAC of 34 umol TE/g of fresh by reference. berries corresponds with an ORAC of 162 umol TE/g dried 15 matter. Black raspberries have a very high ORAC of 77 FIELD OF THE INVENTION umoleTE/g while boysenberries have an ORAC of 48 umole TE/g, and red raspberries and blueberries have an ORAC of The present invention relates to the topical application of 24 and 23 umole TE/g, respectively. (http://www.decker compositions containing macqui berry or macqui berry farm.com/antioxidants.html). Acai is another fruit having a extract in a topical formulation for the prevention and/or high ORAC content (167 ORAC units/g according to Bruns treatment of damage to skin, particularly skin damage result wick Laboratories). Other fruit having high ORAC values ing from chronoaging and photoaging. include pomegranate (33.1 ulumole TE/g) and aronia berry (62 Lumole TE/g) as well as whole coffee fruit extract (6250 BACKGROUND OF THE INVENTION ORAC units per gram according to Brunswick Laborato 25 ries). The stage at which the plant is harvested affects the ORAC value. Blackberries have their highest ORAC values Skin is Subject to abuse by many extrinsic (environmen during the green stages, whereas red raspberries have their tal) factors as well as intrinsic factors. A common extrinsic highest ORAC values when ripe. The ORAC may be factor is exposure to ultraviolet radiation. Whether extrinsic obtained by using the method described by the U.S. Depart or intrinsic, the abuse results in skin aging. Skin aging ment of Agriculture's Agricultural Research Service (Prior happens in two ways: (1) through the natural aging process 30 and Cao, 83(4) J. AOAC INT. 950-6 (2000)). Additionally, which dermatologists call chronological aging (also known testing for ORAC, H-ORAC, N-ORAC, S-ORAC, and as chronoaging); and (2) through UV rays in sunlight ORAC-E (high throughput ORAC for oil-in-water emul accelerating the aging process which dermatologists call sion) is available from Brunswick Laboratories (www photoaging. Chronoaging results in thinning, loss of elas .brunswicklabs.com). ticity and general degradation of skin. As the skin naturally 35 Anthocyanins have been formulated in topical form. For ages, there is a reduction in the cells and blood vessels that example, U.S. Pat. Pub. 2004/0022818 provides a skin care Supply the skin. There is also a flattening of the dermal composition comprising fruit particles. Red and blue fruits, epidermal junction which results in weaker mechanical as well as other fruits which contain anthocyanins are resistance. As a consequence, older persons are more Sus included in this composition. Similarly, U.S. Pub. 2003/ ceptive to blister formation in cases of mechanical traumas 40 0161897 and U.S. Pat. No. 6,361,786 provide a topical or disease processes (Oikarinen et al., Photodermatal. Pho antimicrobial factor having fruit juice (cranberry, Aronia toimmunol. Photomed., 7:3-4 (1990)). berry, blackberry, grape or blueberry) and polyvinylprolidi By contrast, photoaging, or premature aging, is a process none. A topical oil-in-water emulsion containing a surfac in which the skin changes in appearance as a result of tant/emulsifier and a lipid, which may be an anthocyanin repeated exposure to Sunlight. Typically, photoaging occurs 45 containing berry extract, is provided by WO98/05294. U.S. in areas of habitual exposure, Such as the scalp, face, ears, Pat. No. 5,011,855 provides a cosmetic composition having neck, chest, forearms and hands. The changes associated a-linolenic acid and an oil extracted from Ribes genus fruits. with photoaging include elastosis, atrophy, wrinkling, vas However, there are problems associated with these and cular changes (diffuse erythema, ecchymoses, and telangi other uses of antioxidants in a topical formulation. Particu ectasias), pigmentary changes (lentigines, freckles, and 50 larly, antioxidants are readily oxidized and lose their anti areas of hypo- and hyper-pigmentation), and the develop oxidant capacity. Additionally, some of the oxidation prod ment of seborrheic keratosis, actinic keratosis, comedones ucts of antioxidants will have a deleterious effect; for and cysts. example, vitamin C oxidizes to dehydroascorbate which is Antioxidants are useful agents treating the skin from known to lead to the formation of advanced glycation damage caused by chronoaging and photoaging. The most 55 endproducts (AGEs) and therefore increase the signs of useful antioxidants are those that provide the highest capac aging skin. ity to absorb free radicals. The oxygen radical absorbance Therefore, a topical formulation containing an antioxidant capacity (ORAC) is a measurement of this (Dreher F. with a much higher ORAC and consequently greater anti Maibach H. Curr Probl Dermatol. 2001:29:157-64.) Antho oxidant power is needed in combination with a formulation cyanins are a type of antioxidants that generally encompass 60 that protects the antioxidant from degradation and loss of the a class of flavonoid compounds that are naturally occurring, anti-oxidative power to be used in treating and protecting the water-soluble compounds, responsible for the red, purple, skin. and blue colors of many fruits, vegetables, cereal grains, and flowers. Most anthocyanins have a high ORAC rating com SUMMARY OF THE INVENTION pared to other antioxidants and make them particularly 65 useful for their topical antioxidative properties. Addition It is an object of the present invention to provide a ally, anthocyanins are collagenase inhibitors, which helps in composition and method for treating and protecting the skin. US 9,463,153 B2 3 In accordance therewith, a method and composition is TABLE 1-continued provided for treating skin, comprising a topical composition containing macqui berry in a stabilized form and the admin ORAC value istration of an effective amount of the topical composition to Fruit (Imole TEg) the skin.