Cosmetiscope June 2020

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Summer 2020 • Vol. 26 • Issue 6

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Caffeine—A Widely Used Topical Ingredient in Personal Care Products with Numerous Claims for Activity in Skin …by Paul Thau

affeine is the most widely used drug in the world. Its use in skin care products has existed for a range of applications for many years; however, based upon emerging knowledge about the influence of caffeine on skin biochemistry, there has been renewed rationale and justification for the use of caffeine and its derivatives for these applications. Further, advanced delivery systems to enhance performance are now available. This review covers information from scientific literature and patent information related to caffeine’s chemistry, applications, and methods to enhance its topical delivery and efficacy.

Chemistry

Caffeine is synthesized in plants from the purine nucleotides, adenosine monophosphate, guanosine monophosphate, and inosinic acid. These in turn are transformed into xanthosine, and then theobromine, which is the next to last precursor of caffeine. Being readily available as a byproduct of the coffee decaffeination process, caffeine is generally not commercially produced by chemical synthesis. Pure anhydrous caffeine is a white colorless powder having a melting point of 237–238 °C. Caffeine is moderately soluble in water (2 g/100 mL) and very soluble in ethanol (15 g/100 mL). It is weakly basic (pKa = ~0.6) requiring strong acid to protonate it. However, it does not form stable salts of strong acids, since they are hydrolyzed readily in water. The solubility of caffeine in water increases in the presence of organic acids or their alkali salts (e.g., benzoates, citrates, or salicylates). Monographs for caffeine citrate and caffeine sodium benzoate are included in the U.S. Pharmacopeia.

 Figure 1. The molecular structure of caffeine. Pharmacological Activity of Caffeine

Caffeine is naturally produced by several plants and is found in coffee beans, guarana, cacao beans, and tea. In nature, caffeine acts as a natural pesticide. It paralyzes and kills insects that attempt to feed on the plants. Its pharmacological activities include cardiac and respiratory stimulation and promotion of kidney diuresis. The therapeutic dose of caffeine is about the same as the amount found in an average cup of coffee, between 100 and 200 milligrams. (continued on Page 4)

SKIN MICROBIOME: PERSPECTIVES ON AGING, COMPROMISED SKIN AND COSMETICS NYSCC Programs...see page 6 for more information.


2020 NYSCC EXECUTIVE BOARD & COMMITTEE Chair Giorgino Macalino gmacalin@estee.com

Chair-Elect Susanna Fernandes fernandes.susie@gmail.com Treasurer Stephen Carter treasurer@nyscc.org Treasurer-Elect Mohamed Abdulla treasurer-elect@nyscc.org Secretary Leor Fay Tal secretary@nyscc.org Advisor Sonia Dawson advisor@nyscc.org Program Maria Mo program@nyscc.org By-Laws Amy Marshall amy.marshall@altana.com

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Letter from the Chairman …Giorgino Macalino

elcome! If you are like me, you are grateful for the amenities afforded us in PHASE I of the COVID-19 pandemic with beaches, parks, and golf courses being accessible and allowing us some bit of social engagement and a glimpse of normalcy that we have sorely missed! I hope you and yours continue to be safe and healthy. Since I last communicated with you, we have wrapped our “pilot” At Home Live Webinar Series and are reviewing the analytics to determine how to move forward and ensure the same high-level content, engagement, and success. The good news is we’ve learned that these programs are part of essential business—attracting thousands of registrants and viewers over the course of five weeks! One initial take-away is that deep dives into specific topics are welcome, such as the Microbiome webinar program the week of June 15th. We plan to curate and present this content so it can fit into your lives in this ever-changing environment. These programs will be linked with the robust ingredients and product offerings that are part of NYSCC Suppliers’ Day through the Digital Pop-Up and Solutions Center, providing innovative exhibitors with a forum to showcase the latest and most-in-demand formulations and solutions. Never allowing things to stay status-quo, we continue to review and determine how the NYSCC’s “face to the world” (our website!) can be most valuable. With a full team of volunteers, we re-designed and launched what I believe is one of the Chapter’s most captivating websites with motion graphics, videos, photos, content, easy-to-find event info, and so much more. To add more depth to the website, we want to “look back” and showcase how the Chapter has grown and evolved over the years. Expanding on the foundation built with the 40th Anniversary Retrospective, I have asked all volunteers to contribute in creating a virtual showcase of our growth, our dedication, and most of all, our people (You!) who have contributed to make our Chapter the largest and most vibrant across the globe. If you have anything you would like to contribute, please reach out to Sophia Chen (historian@nyscc.org) with content and pictures that will demonstrate our contribution to the SCC’s mission across our region and around the world. We can’t wait to reveal this new website layer! As you know, this year we chose Revolutionary Disruptors as our theme, and we will continue to provide you with the technical education that will propel your professional development and allow you to disrupt the norm and realize success. Take a look at what’s on the calendar (https://nyscc.org/event-schedule/). • June 15-18: Skin Microbiome: Perspectives on Aging, Compromised Skin and Cosmetics, will showcase a Live Q&A Panel in conjunction with a library of content available over the course of the week. The contents highlight a holistic view of the skin microbiome and its impact on cutaneous structure in healthy, aged and compromised states. Join us for this complimentary event!

Communications Cathy Piterski cathy.piterski@givaudan.com Special Events Amy Marshall amy.marshall@altana.com Cosmetiscope Editor Roger Mcmullen roger_mcmullen@fdu.edu Cosmetiscope Advertising Bret Clark rbclark@ashland.com Social Media Estelle Gu socialmedia@nyscc.org

• August 12: Sun Care Symposium will be a full week following the same format as the Skin Microbiome event. A library of content will be made available for a defined period of time with a “live” wrap-up session finale including all presenters. We are optimistically looking forward to Suppliers’ Day (https://nyscc.org/suppliers-day/) on September 30th – October 1st at the Jacob K. Javits Convention Center to bring the industry together for learning, discovering, and discussing the latest innovations in the product development process. Stay tuned for exciting Suppliers’ Day updates in the coming months in the Cosmeticscope! In closing, I would like to sincerely thank Estelle Gu, Maria Mo, and the entire AHLS team for bringing these programs to life. The feedback we’ve received from other chapters and members around the world has been so positive. We know we are on to something and need to continue it! Stay tuned and visit www.nyscc.org often. We are continually adding opportunities for you to learn, network, and engage. Your success is our success. Let’s keep it going! 2

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Caffeine—A Widely Used Topical Ingredient in Personal Care Products

(continued from Page 1)

Pharmaceutical and Cosmetic Uses of Caffeine in Topical Skin Products

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From a recent review of cosmetic and OTC dermatologic products containing caffeine, it has been catalogued as having a diverse range of claimed activities. There are numerous studies that validate the benefits of ingested caffeine. However, studies are still required to determine the long-lasting benefits of caffeine when used topically as a part of an anti-aging regimen or inclusion in sunscreens and anticellulite products. New biochemical information related to the topical use of caffeine combined with results of in vitro, ex vivo, and in vivo studies have provided increased credibility for some classical and new applications for caffeine and its derivatives. Some of the claimed biological activities of this hydrophilic alkaloid consist of: • Caffeine is used as an active compound in anti-cellulite products because it prevents excessive accumulation of fat in cells. It is claimed to stimulate the degradation of fats during lipolysis through inhibition of the phosphodiesterase activity. • Caffeine has been documented to have potent antioxidant activity. • Caffeine helps protect cells against UV radiation and slows down the process of photoaging of the skin. • Caffeine in cosmetics has also been shown to increase the microcirculation of blood in the skin and also to stimulate the growth of hair through inhibition of 5-α-reductase activity.

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Caffeine is administered topically and transdermally for a variety of pharmaceutical and cosmetic preparations and it is also used as a model hydrophilic compound in dermal risk assessment studies. Caffeine has also been used as a model compound for the delivery of many hydrophilic compounds having similar properties. Table 1. Commercial cosmetic formulations that contain caffeine as an active. Product

Brand (Manufacturer)

Rosaliac UV Riche Anti-redness Moisturizer

La Roche-Posay (L’Oréal)

Eye Fuel (Visibly Combats Dark Circles & Tired, Puffy Eyes)

Kiehl’s Since 1851 (L’Oréal)

Photo Finish Hydrating Under Eye Primer

Smashbox (Estée Lauder Companies)

Wake Up Blush and Highlighter

Almay (Revlon)

Sebum Clearing Masque

Dermalogica (Unilever)

Ready Eyeshadow 4.0

bareMinerals (Shiseido)

Clearly Brighter Anti-Puff Eye Roller

Garnier SkinActive (L’Oréal)

Caffeinated Body Cream

Bath Buzz

Swiss Formula, Health Brilliance, Firm & Glow with Caffeine

St. Ives (Unilever)

Table 1 contains a list of selected skin care products currently on the market that contain caffeine as a principal active ingredient. In addition, U.S. Patents issued during the past 25 years provide many examples of methods to improve and enhance the activity of caffeine on skin: Two examples are shown below: U.S. Patent 5,523,090 AP. Znaiden et al. Assignee: Chesebrough-Ponds, Inc. June 4, 1996 Skin Treatment Composition Skin treatment compositions for improving skin strength and firmness and reducing signs of cellulite. The compositions contain a xanthine (e.g., caffeine or theophylline) and an inositol phosphoric acid, and/or alpha hydroxy acid. The ratio of the xanthine to the acid is in a specific range to maintain the xanthine in a solubilized state. A method of preventing or reducing the signs of cellulite by applying a mixture of an inositol phosphoric acid and an alpha hydroxy acid is also disclosed. 4

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U.S. Patent 2019 0,307,654 T. Florence et al. Assignee: Mary Kay Inc. October 10, 2019 Cosmetic Compositions and Uses Thereof Disclosed is a method for reducing the appearance of cellulite or improving the texture of skin in a target region of skin that has cellulite or rough skin texture, the method comprising topically applying a composition to the target region that includes an effective amount of a mixture of caffeine, escin, and an aqueous-alcoholic extract from Ascophyllum nodosum, wherein topical application of the composition reduces the appearance of cellulite or improves the texture of the skin.

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Summary

Caffeine has important biological activity, which can be harnessed in a variety of different cosmetic product forms. New findings concerning the biological properties of this alkaloid will make the range of caffeine’s applications in the field of cosmetology and dermatology even broader in the future. For this purpose, more research is necessary to determine the appropriate concentrations and delivery systems for caffeine penetration in the skin. It should be noted that there is limited scientific data from clinical trials and insubstantial information about the side effects of the cosmetic use of caffeine. More research is needed to confirm or modify claims for cosmetic applications of caffeine. It is my personal view that if caffeine did not have centuries of usage in beverages, the topical use of caffeine in skin care products would have required it to have been approved by an OTC Panel.

Bibliography

1. A. Herman and A.P. Herman, Caffeine’s mechanisms of action and its cosmetic use, Skin Pharmacol. Physiol., 26(1), 8-14 (2013). 2. L. Luo and M.E. Lane, Topical and transdermal delivery of caffeine, Int. J. Pharm., 490(1-2), 155-64 (2015). 3. S. Luebberding, Cellulite: an evidence-based review, Am. J. Clin. Dermatol., 16(4), 243-256 (2015).

About the Author

Paul Thau was employed at Cosmair/L’Oréal USA for over 22 years, during which time he served as Assistant Vice-President of Cosmetic R&D and then as Senior Research Fellow. His cosmetic industry experience spans more than fifty years and includes R&D positions at Revlon, Bristol-Myers, CIBA Pharmaceutical, and Warner-Lambert. Paul has served the Society of Cosmetic Chemists in many capacities including Chairman of the New York Chapter in 1971 and President of National in 1988. Later he was a member of the IFSCC Presidium and Scientific Committee. Paul is a Fellow of the SCC and holds fifteen U. S. patents. He was presented with the Society of Cosmetic Chemists Maison de Navarre Award in 2005. From 1999 until 2014, Paul ran a cosmetic consulting company, PaCar Tech, which specialized in the areas of innovative product development, new cosmetic raw materials, technology transfer, and technology acquisition. Paul may be reached by e-mail (Pathau21@gmail.com) or mobile telephone (908-451-9558).

31st IFSCC Congress Yokohama, Japan October 20-23, 2020

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Skin Microbiome: Perspectives on Aging, Compromised Skin, and Cosmetics June 15th – 22nd Digital Pop-Up and Solutions Center

For more information, visit the Events section of the NYSCC website (www.nyscc.org).

Event Chairs: Sarah de Szalay (Sarah.deSzalay@rb.com) and Aysel Calkap (aysel.calkap@dsm.com) Event Sponsors:

Schedule June 15-22 June 18

Library of content from the Skin Microbiome webinar available LIVE panel of speakers for question and answer period: The Influence of Cosmetic Ingredients on the Skin Microbiota – Patrick Gonry – Gobiotics-Ingredients Fresh Insights into the Skin Microbiome and Product Claim Essentials – Carl D’Ruiz – DSM Nutritional Products, LLC The Host-Microbiota Axis in Skin Ageing and Repair – Mat Hardman, Ph.D. – Hull York Medical School The Gut Microbiome and the Hair Follicle – Aleksander Richards – Nutrafol The Gut-Skin Connection and its Relation to Acne – Raja Sivamani, M.D. – University of California, Davis

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kin Microbiome: Perspectives on Aging, Compromised Skin and Cosmetics will showcase a library of content over the course of the week with a holistic view of the skin microbiome and its impact on cutaneous structure in healthy, aged, and compromised states. Join us for this complimentary event!

Speaker Abstracts and Biographies The Influence of Cosmetic Ingredients on the Skin Microbiota

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– Patrick Gonry – Gobiotics-Ingredients

n this session, I will provide a discovery presentation of the external influences on the skin microbiota. These consist of temperature, UV radiation, and use of cosmetic products. The surprising effect of cosmetic ingredients on the balance and diversity of the skin microbiota will be demonstrated by in vivo data. The following ingredients have been studied: water, alcohol, preservatives, surfactants, and emulsifiers. Based on these results, an attempt to define a balanced skin microbiota and healthy diversity will be proposed. Special attention will also be given to intimate and oral microbiota.

n Patrick Gonry

Patrick graduated as a chemical engineer at the University of Ghent, Belgium in 1991. Afterwards, he finished an intensive specialization in cosmetic manufacturing and obtained a degree in Dermato-Cosmetic Science at the University of Brussels. In 2001, he started the consultancy company S&C, supporting cosmetic producers and raw material suppliers in product development, global legislation, and toxicology. He trained many cosmetic chemists and technical sales representatives. Since 2002, his research and passion have been dedicated to the skin microbiota, which resulted in the launch of the first prebiotic ingredient dedicated to baby care and intimate hygiene. He is the driving force behind many skin microbiota cosmetics in Europe. Through his latest company Gobiotics-Ingredients, he offers the industry scientific solutions to support skin microbiota claims. Patrick is a determined scientist with concrete solutions and a heart for the invisible world on our skin.

Fresh Insights into the Skin Microbiome and Product Claim Essentials

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____________________________________________________________

– Carl D’Ruiz – DSM Nutritional Products, LLC

n Carl D’Ruiz

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Mr. D'Ruiz is an accomplished regulatory leader with more than 20 years of experience in providing scientific and regulatory strategic direction for the global development, marketing, and sustainability of consumer and professional product brands. He has held key R&D, regulatory, quality, clinical, and scientific affairs positions at Ciba, Dial, Henkel, Newell Rubbermaid, and currently is the Senior Manager of Regulatory and Governmental Affairs for Personal Care Products, NA at DSM Nutritional Products, LLC. He is regarded as a thought leader within the industry on the subject of topical OTC drugs, cosmetics, and personal care products, and specializes in public health, regulatory, and scientific issues associated with

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The Host-Microbiota Axis in Skin Ageing and Repair ____________________________________________________________

– Mat Hardman – Hull York Medical School

ur skin is “home” to a multitude of microorganisms, collectively termed the skin microbiota. While existing studies have meticulously explored the role of gut microbiota in health and disease, far less information is available on the significance of skin microbiota in physiology and pathology. Amidst the demographics of an ageing population, age is a well-known contributory factor to skin disease, poor acute healing, and a primary risk factor in the etiology of chronic wounds. Research in this area has historically focused on the contribution of structural and functional changes in the skin (host tissue) to pathology, while age-associated changes in the skin microbiota have been largely ignored. Research from our group and others has highlighted the extensive cross-talk between the skin microbiota and host skin cell, which ultimately directs skin physiology. In this talk I will provide an update on current understanding of the contribution of skin microorganisms to skin biology and pathology. I will focus on the effects of ageing and diabetes on skin function and dysfunction—including ineffective repair. I will argue that successful development of effective interventions in this area will require a detailed understanding of the host-microbiota axis, underpinned by emerging “omics” and powerful new sequencing technologies.

n Mat Hardman, Ph.D.

Professor Mat Hardman is Chair in Skin Biology and Wound Repair and Director of Research at the Hull York Medical School (UK). He has 25 years of experience in the field of skin biology with a specific focus on skin ageing and wound healing. Mat trained at the University of Manchester (UK) where he was one of only two researchers nationally to be awarded consecutive Junior and Senior AgeUK Fellowships in ageing research. He established his own research group in 2007 and was promoted to Reader in 2016. Mat is former Director of the Manchester EPSRC and MRC Centre for Doctoral Training in Regenerative Medicine and spent three years as Research Director in the School of Life Sciences. Current interests in the group include: exploring the complex interactions between the skin microbiota and host response, particularly in the context of ageing wound repair; characterizing the effects of ageing and menopause on skin structure and function; exploring the role of hair follicles and stem cells in skin biology and repair; and developing more predictive pre-clinical models for skin and wound research. ____________________________________________________________

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The Gut Microbiome and the Hair Follicle – Aleksander Richards – Nutrafol

he gut is the mirror of one’s overall health. There are many organ systems that the gut microbiota can influence and exert their effects on. From axis—such as the gut-liver, gut-skin, gut-hair, and gut-thyroid—the intestinal bacteria control our health destiny. The largest nerve in the body, the vagus nerve, has an activation point in the microbiome, which can subsequently send electrical signals that promote anti-inflammatory and cortisol reduction pathways. These pathways control the hair growth cycle as well. Furthermore, gut inflammation can increase the space between gap junctions, increase 8

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intestinal permeability, and decrease bacterial adhesion to the intestinal lining—all of which reduce nutrient absorption. Nutrients such as iodine, selenium, and the absorption of nutraceuticals are integral for maintaining a proper hair growth cycle. These actives and minerals subsequently influence the thyroid, liver, and adrenals in a manner that is integral to one’s hair growth. This is just one of the many pathways I will describe that show how crucial a healthy and varied microbiome is for one’s hair health and wellness.

n Aleksander Richards

Aleks Richards graduated from Fordham University in 2016 with a bachelor’s degree in Biology and Pre-Med. He is currently Senior R&D Manager at Nutrafol, a company specialized in treating hair loss and thinning using nutraceuticals. Aleks has been involved in the formulation of Nutrafol leading products. He currently leads the biology research team focusing on specific and novel pathways relating to hair loss. The microbiome has been a focus of his research and he contributed to the formulation of specific probiotics to target hair loss and thinning. _________________________________________________________

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The Gut-Skin Connection and its Relation to Acne – Raja Sivamani, M.D. – University of California, Davis

esearch into how gut health affects the skin, and the concept of the gut-skin axis, have contributed to the growth of the concepts “healthy from within” and “beauty from within.” This scientific knowledge is now being applied to acne, which traditionally relied largely on antibiotics and retinoids as treatment modalities. The discovery of the gut-skin axis has been a key factor pushing the science forward in this field as we learn how the gut microbiome and gut related signaling mediators may influence acne. Different factors involved in the gut-skin axis in relation to acne will be discussed including the role of nutrition, the role of shifts in the gut microbiome, and associated changes in gut derived signals that can reach the skin.

n Raja Sivamani, M.D.

Dr. Raja Sivamani is a board-certified dermatologist as well as an Ayurvedic Practitioner and hosts the wellness platform Jivome and has two clinics Pacific Skin Institute and Zen Dermatology. He is the Director of Clinical Research in the Department of Dermatology at the University of California, Davis and he is the CoDirector of the Microbiome Research Initiative at the California State University, Sacramento. He focuses on general and integrative dermatology including medical, surgical, and cosmetic services with training in bioengineering as well as Allopathic and Ayurvedic medicine. He merges modern research and science with a personalized approach to each patient. His training in Ayurvedic medicine lets him take a more humanistic approach to patient care, science, and research. Dr. Sivamani has over 110 peer-reviewed publications and a textbook on cosmeceuticals. He leads many clinical studies that focus on the impact of foods, nutrition, microbiome, and gut-skin axis on the skin as well as studies on standard Western medications and devices. Finally, he is a deep believer in integrative medical education and one of the primary editors for LearnSkin.com.

NYSCC Sponsorship Opportunities The NYSCC Sponsorship Committee is proud to invite interested parties to sponsor NYSCC educational events throughout the year. Sponsorship Committee: Yelena Zolotarsky (yelenazol@gmail.com) and Daphne Benderly (dbenderly@presperse.com) For more information, please visit: http://nyscc.org/sponsorship-opportunities/ S um m er 2 02 0

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Obituary

t is with deep regret we announce the passing of Gary Agism (72), on Friday, May 15th from complications related to COVID-19. Gary, a proud graduate of Grinell College, was a member of the SCC for more than 40 years, most recently with the Mid-Atlantic Chapter of the SCC. He was employed by Pfizer Consumer Healthcare since 1984 holding multiple patents and also served his country in the U.S. Navy from 1969-1973. Gary was a devoted mentor, educator, and friend to the society. He always had a smile and was often known for delivering the last presentation at the SCC National Meetings on Friday afternoons, drawing a full house, where he would not only present top-quality science, but would sing and recite the classics. A beloved and colorful fixture known not only for his industry knowledge, but also his colorful vests, Gary was a frequent speaker at chapter events for many years. He also served the SCC in various roles during his membership including Area Councilor, Mid-Atlantic Chapter Chair, Area Director, National Committee Member and/or Chair (Constitution and Bylaws, Nominations, COCA, COSA, CEP Advisory, Medal Award), and various national officer seats culminating in his role as SCC President in 2009.

2020 NYSCC Events Calendar

• For updated NYSCC information, visit us on the web at: www.nyscc.org • For National SCC information: www.scconline.org

June 15-18 Skin Microbiome: Perspectives on Aging, Compromised Skin and Cosmetics – Online Symposium (www.nyscc.org) August 12 Sun Care Symposium – Online Symposium (www.nyscc.org) September 23 Color Cosmetics – Color Trend Forecast – Lightbox, New York, NY September 30 NYSCC Suppliers’ Day – Jacob K. Javits Center, New York, NY – October 1 October 13 Effect Pigments Symposium – Nanina’s in the Park, Belleville, NJ November 18 Beyond Hair Care and Officer Installation – Brooklyn Botanical Garden, Brooklyn, NY

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Call for Papers

December 15 NYSCC Mentor Mentee Mixer – New York, NY

he Cosmetiscope editorial committee invites all interested parties to submit feature technical articles for publication in the NYSCC monthly newsletter. Authors of feature articles are eligible to win the prestigous NYSCC Literature Award ($1,000) for the best front-page article published during the calendar year. Authors also receive $200 reimbursement to attend a theatrical performance of their choice. Writing an article for your peers is a very rewarding experience, both personally and professionally, and will ensure your place in NYSCC history. You may choose whatever topic you feel would be interesting to fellow colleagues in our industry. We also welcome any other types of commentaries or articles that may be published in the Career Corner, Technical Tidbit section, or as a Letter to the Editor. Please send correspondence to: roger_mcmullen@fdu.edu. 10

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