Polymeric Emulsion Technology Applied to Tretinoin

April 2019 | Volume 18 | Issue 4 | Supplement Individual Articles | 148 | Copyright © April 2019


Leon H. Kircik MD,a Zoe D. Draelos MD,b Diane S. Berson MDc

School of Medicine at Mount Sinai, New York, NY; Indiana School of Medicine, Indianapolis, IN; Physicians Skin Care, PLLC, Louisville, KY; DermResearch, PLLC, Louisville, KY; Skin Sciences, PLLC, Louisville, KY BDermatology Consulting Services, PLLC, High Point, NC cDepartment of Dermatology, Weill Medical College of Cornell University, New York-Presbyterian Hospital, New York, NY

to vehicle as early as week 8 and week 4, respectively. Mean percentage change (LS mean) from baseline to week 12 in inflammatory lesion counts was 52.1% versus 41.0% with vehicle (P less than .001, Figure 7), and in noninflammatory lesion counts 46.1% versus 29.9% with vehicle (P less than .001).Although there are currently no direct comparative studies with other tretinoin formulations, a phase 3 study with micronized tretinoin 0.05% aqueous gel reported a reduction in inflammatory lesions of 36% by week 12 (P less than 0.001 versus vehicle).23 A comparative study of this micronized tretinoin 0.05% gel and tretinoin 0.1% microsphere gel failed to show non-inferiority, although numerically the reduction in inflammatory lesions was greater with the higher concentration formulation of tretinoin.24 Safety The potential to cause irritation has been a major concern with tretinoin, and other retinoids; it appears to be dose-dependent. Micronized tretinoin 0.05% lotion in a novel polymeric matrix was very well tolerated, with a low incidence of dryness, pain (including stinging, burning, or pain), and erythema of 4%, 3%, and 1%, respectively (Figure 8). The same concentration of tretinoin (0.5%) formulated in an aqueous gel, of a similar concentration (0.04%) formulated in a microsphere reported higher incidences of skin irritation (16%, 8% and 7%, and 12%, 10%, and 6%, respectively) in two separate studies.23 A higher concentration of tretinoin (0.1%) formulated in a microsphere reported dry skin, skin burning, and erythema in 30%, 15%, and 18% of patients.

CONCLUDING REMARKS

The use of retinoids in the treatment of acne is well-established. However, efficacy in inflammatory lesions and local irritation have limited use. A number of formulation advances have been deployed to address these limitations. The most recent is the introduction of a novel polymeric matrix containing micronized tretinoin (tretinoin 0.05% lotion) and a number of formulation advances, including emulsifying agents and mineral oil. Efficacy against inflammatory lesions appears much greater than that reported previously, and tolerability better.

DISCLOSURES

Dr. Kircik has received compensation from JDD for his editorial support and has served either as an investigator, speaker, consultant, or advisory board member for Ortho Dermatologics. Dr. Draelos is a researcher for Ortho Dermatologics. Dr. Berson is consultant/adviser for Allergan, Galderma, Ortho Dermatologics, Almirall, Ferndale, Johnson & Johnson, L’Oreal, Aclaris, P&G, Dermira, Sienna, Revance, and Sonoma.

ACKNOWLEDGMENT

This research was supported by a grant from Ortho Dermatologics.

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AUTHOR CORRESPONDENCE

Leon H. Kircik MD wedoderm@yahoo.com
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