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
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
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.
Cutaneous HP can produce profound psychosocial impacts
depending upon oneâ€™s race and personality. It
is the second most common complaint in dermatologistâ€™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.