Treatment of Facial Photodamage Using a Novel Retinol Formulation

May 2013 | Volume 12 | Issue 5 | Original Article | 533 | Copyright © May 2013

Michael H. Gold MD,a,b Leon H. Kircik MD,c-e Vivian W. Bucay MD,f,g
Monika G. Kiripolsky MD,h,i and Julie A. Biron BSca

aTennessee Clinical Research Center, Nashville, TN
bDepartment of Medicine, Division of Dermatology, Vanderbilt University School of Medicine, Nashville, TN
cMount Sinai Medical Center, New York, NY
dIndiana University School of Medicine, Indianapolis, IN
ePhysicians Skin Care, PLLC, Louisville, KY
fPrivate Practice, San Antonio, TX
gUniversity of Texas Health Science Center, San Antonio, TX
hPrivate Practice, San Diego, CA
iScripps Memorial Hospital, La Jolla, CA

BACKGROUND: Photoaged skin is characterized by a variety of clinical, histologic, and biochemical features.
OBJECTIVE: To determine the efficacy of a new topical formulation of 1% retinol and the effects of this same formulation using a 0.5% retinol concentration to minimize irritation.
METHODS: Patients at 2 sites (n=6, n=5) with photodamaged skin applied a novel suspension of retinol (1%) daily to their faces for 8 to 12 weeks. Clinicians graded improvement in ultraviolet-induced features at 4 to 6 weeks and at 8 to 12 weeks. Positive results of the observational pilot study warranted a follow-up study on the low concentration. At a third site, females (n=30) with facial photodamage applied the same formulation with or without retinol (0.5%) daily for 8 weeks. Twenty-two subjects applied the test product and 8 applied vehicle according to a randomized, double-blinded, institutional review board–approved protocol. Improvements in photodamage features were graded at 4 and 8 weeks.
RESULTS: In the observational pilot study, most participants showed improvement in overall photodamage, crow’s feet, elasticity,wrinkles, brightness, and hyperpigmentation at 60 to 80 days. Improvements at 60 to 80 days were greater than at 30 to 46 days. In the low-concentration study with 0.5% retinol, improvements were modest, most likely due to the lower retinol concentration. Burning, pruritus, dryness, and erythema were minimal with the 0.5% retinol concentration.
CONCLUSIONS: The topical formulation of 1% retinol improves photodamaged skin for at least 8 to 12 weeks. Although improvements with the 0.5% retinol were more modest, side effects such as burning, dryness, pruritus, and erythema during the 8-week study period were minimal. These encouraging results justify a longer-term study to determine whether topically applied 0.5% retinol can provide benefits comparable with those seen with topically applied 1% retinol.

J Drugs Dermatol. 2013;12(5):533-541.


Repeated exposure to solar ultraviolet (UV) radiation causes human skin to age prematurely (photoaging).1,2 Photoaged skin is characterized by a variety of clinical, histologic, and biochemical features. Wrinkles, uneven pigmentation (including lentigines and ephelides), laxity, and a rough appearance are common.3,4 Histologic changes include disorganized collagen fibrils in the dermis, reduced levels of types I and III collagen precursors and cross-links, increased ratios of type III to type I collagen, and increased levels of elastin.4,5
All-trans retinoic acid (RA), or tretinoin, is the primary topical pharmaceutical used to improve the appearance of photoaged skin.2 RA induces expression of procollagen genes, which in turn likely upregulate production of procollagens I and III, resulting in increased deposition of collagen fibrils.1 The beneficial effects of topical tretinoin on photodamaged skin have been described in detail by Kligman and colleagues.6 These authors also noted that skin irritation may occur during the first month of treatment, especially in young, fair-skinned patients.
Because of the skin irritation commonly associated with the use of topical RA, interest has emerged in another vitamin A derivative, retinol, reported to have similar benefits to RA but with less skin irritation.7 Two groups8,9 have reported that topical retinol is metabolized to RA in the skin. Kang and colleagues10 and Varani et al11 described epidermal thickening, reduced levels of matrix metalloproteinases, increased growth of fibroblasts, and increased collagen synthesis in human skin after retinol application.7