Blockade of Melanin Synthesis, Activation and Distribution Pathway by a Nonprescription Natural Regimen Is Equally Effective to a Multiple Prescription-Based Therapeutic Regimen

December 2013 | Volume 12 | Issue 12 | Original Article | 1449 | Copyright © December 2013

Carl Thornfeldt MD,a,b Ronald L. Rizer PhD,c Nathan S. Trookman MDd

aCT Derm PC, Fruitland, ID
bEpisciences, Inc., Boise, ID
cThomas J. Stephens & Associates, Colorado Springs, CO
dColorado Springs Dermatology, Canon City, CO

Abstract
BACKGROUND: Disorders characterized by cutaneous hyperpigmentation (HP) are among the most common complaints in dermatologists' offices. These patients are also some of the most difficult to treat since current therapeutic regimens have high irritation rates and mediocre efficacy. Moreover, current regimens have the potential to induce post-inflammatory HP (PIH), a secondary disease that is more difficult to treat.
OBJECTIVE: To measure the effectiveness of a novel blend of primarily natural ingredients that inhibits all but one of the steps in melanin synthesis, activation and distribution. Three common types of HP were treated and compared with one of the most commonly prescribed available regimens. This comprises two prescription products and two nonprescription products containing known depigmenting lightening ingredients.
MATERIALS and METHODS: The initial trial consisted of 56 females of 3 different races were treated in a 3-armed parallel, investigatorblinded prospective controlled clinical trial of 18 weeks duration. The treatment phase was 12 weeks long, followed by a 6 week, nontreatment regression phase. This trial was conducted in the winter at over 6,000 feet above sea level. The natural ingredient (NI) blend consists of two cosmeceutical products together containing 22 ingredients. A second 1-year open trial of 31 panelists of 3 races was instituted to document continual improvement using both NI products without irritation and sensitization.
RESULTS: The novel herbal blend regimens had comparable efficacy in treating HP and preventing rebound of mottled HP, dyschromia and melasma as the commercial regimen containing two prescription products. The 12-month open study demonstrated continued visible improvement of the HP with NI regimens without irritation and sensitization.
CONCLUSION: The novel primarily natural ingredient product regimens are equally effective in treating three types of cutaneous HP as is a regimen containing prescription hydroquinone 4%, tretinoin 0.05% and two nonprescription leave on products.

J Drugs Dermatol. 2013;12(12):1449-1454.

INTRODUCTION

Cutaneous HP can produce profound psychosocial impacts depending upon one’s race and personality. It is the second most common complaint in dermatologist’s offices by African American patients, while 11th in frequency for Caucasians.1-3 The current prescription depigmenting agents hydroquinone (HQ), retinoic acid or tretinoin (TR) and corticosteroids (CS) are combined in one product which is considered to be one of the gold standards for treatment of HP yet the FDA states that its efficacy is 51%.4 HQ available as a 4% prescription but compounded extemporaneously up to 10% has been considered the mainstay for HP therapy. Its mechanism of action is inhibiting tyrosinase, the rate limiting enzyme in melanin synthesis, melanocyte cytotoxicity and modulating melanosome degradation. A regimen consisting of 4% HQ gel, ascorbic acid, magnesium ascorbyl phosphate and glycolic acid reduced melasma by 63% and 70% at the two study sites in 8 weeks with 33 panelists.5 A 10-week open clinical trial conducted at sites who sell this product combined the gold standard regimen control in this study with a destructive facial rejuvenation procedure reduced HP by 83%.6 TR at 0.01% to 0.1% is somewhat effective alone primarily by increasing the desquamation rate of keratinocytes containing excessive melanosomes coupled with antioxidant effect. This molecule and nonprescription retinol are known to increase penetration of HQ. Third generation prescription retinoids such as tazarotene and adapalene have similar functionality and efficacy as TR in treating HP. The CS range in potency from low potency hydrocortisone, midpotency fluocinolone, triamcinolone and dexamethasone, to ultra-potent clobetasol. They block activation of melanin synthesis but induce cutaneous atrophy.