Clinical Evidence of Cell-Targeted Topical Therapy for Treating Skin Dyspigmentation

August 2021 | Volume 20 | Issue 8 | Original Article | 865 | Copyright © August 2021


Published online July 30, 2021

Zoe Diana Draelos MDa, Frederick W. Woodin Jr. BS MAb

aDermatology Consulting Services, PLLC., High Point, NC
bZO Skin Health, Inc., Irvine, CA

Abstract
Background: New development of cell-targeted therapies to enable site-specific skin tissue drug delivery may reduce off-target effects, decrease unwanted toxicities, and enhance drug efficacy. These efforts have led to several targeting strategies that modulate active product delivery to include small molecule-, nucleic acid-, peptide-, antibody-, and cell-based strategies. Tissue specific cell-targeting strategies such as these may be useful in cosmetic dermatologic applications.
Objective: The aim of this 16-week clinical trial of a skin brightening composition containing melanocyte cell-targeted biodelivery was to assess its effectiveness in restoring the skin complexion evenness by modulating melanocyte activity in a cohort of 50 Fitzpatrick type I–VI subjects with moderate to severe dyspigmentation.
Results: Data from expert grading, skin surface colorimetry, and subject self-assessments reflected significant improvement in facial skin tone as early as 2 weeks after treatment initiation, with continual improvement through week 16. The most dramatic pigmentation improvement, based on investigator assessments, was a statistically significant improvement in skin brightness at week 2 that progressed to week 8 with significant improvement in skin evenness and brightness. By weeks 12 and 16, progressive levels of significant improvement in skin evenness and brightening became apparent. Colorimetry demonstrated progressive improvement in skin dyspigmentation starting at 2 weeks and continuing to week 16. Subject self-assessment data supported similar improvements in skin dyspigmentation.
Conclusion: These results demonstrate the ability of a cell-targeted topical therapy to achieve improvements in skin pigmentation through site-specific suppression of melanocyte activity.

J Drugs Dermatol. 2021;20(8):865-867. oi:10.36849/JDD.6037

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INTRODUCTION

The evolution of site-specific cell-targeted drug delivery systems chemically programmed to bind with a single cellular receptor have recently emerged as enablers toward delivering topical skin therapy. New technologies now afford the opportunity to promote enhanced skin repair by employing cell-targeted biodelivery systems capable of delivering therapeutic bioactive constituents to specific cellular receptors that minimize off-target delivery to maximize treatment efficacy of skin dyspigmentation conditions.

An array of technologies has been employed over the last century to interfere at various stages of the melanogenesis process to mitigate melanin production. The prevailing limitation with these existing technologies resides in their non-specific and off-targeting characteristics that limits efficacy. Therefore, it could be envisioned that technologies that can directly target the melanocyte to suppress melanocyte hyperactivity could provide for a more effective treatment method toward addressing skin dyspigmentation issues. The recent scientific advancement of a cell-targeted encapsulation technology that binds solely to the melanocortin 1 (MC1) receptors of melanocyte cells due to the presence of site-specific surface ligands affords such an opportunity to overcome off-target delivery. The technology exclusively binds with the MC1 receptors to deliver melanogenesis suppressing bioactive constituents directly into melanocyte cells through endocytosis, where the encapsulate is then metabolized within the melanocytes to release a bioactive peptide that suppresses tyrosinase expression.1

Structural changes occur to the melanocytes in photoaged skin, including nuclear heterogeneity, abundant cytoplasmic organelles, and elongation of dendrites.2 This research demonstrates the effectiveness of a cell-targeted encapsulated technology that targets the MC1 receptor to down-regulate melanogenesis in human skin, disregarding any changes that may occur to the melanocytes due to intrinsic or extrinsic aging.