A Novel Microgel Complex Delivers Acne Medicine Deep into Follicles While Demonstrating High Patient Tolerance

February 2015 | Volume 14 | Issue 2 | Original Article | 176 | Copyright © 2015

Jeff Wu PhD, Jeannette Chantalat MBA, Jue-Chen Liu PhD

Johnson & Johnson Consumer Companies, Inc., Skillman, NJ

Abstract

Acne vulgaris is a common skin disease that is difficult to treat due to its multifactorial etiology. The presence of sebum and keratinocytes within the hair follicle often prevent medication from penetrating deep into the follicle where the causal bacteria are to be found. Medications able to penetrate into the follicle are often irritating to the skin. Recently, a technology has been developed that can penetrate sebum and deliver medication deep in the follicle while also being gentle on the skin. This novel microgel complex is therefore a critical next step in the treatment of acne and also an important tool for people who suffer from a lower quality of life due to persistent acne breakouts.

J Drugs Dermatol. 2015;14(2):176-182.

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INTRODUCTION

Acne vulgaris is a common, multifactorial disease involving the pilosebaceous unit of the skin that affects over 17 million people in the United States, most commonly teenagers, but can also affects about 12% of women and 3% of men up to the age of 44.1 Acne presents in a wide variety of ways, including comedones, papules, pustules, and cysts, but all forms of acne cause a lower quality of life due to embarrassment, low self-esteem and impaired social interaction.

Acne vulgaris is difficult to manage due to the exact etiology often varying from person to person. Three main factors influence the formation of acne: hyperactivity of sebaceous glands, changes in follicular keratinization, and the bacteria Propionibacterium acnes.1 Increases in androgen production cause sebaceous glands to become more active, causing an imbalance between production and secretion capacity, resulting in blockage of the follicle.1 Concurrently, maturing keratinocytes are exfoliated into the follicle, which can adhere to each other due to the sebum’s presence, transglutaminase activity, and attractive forces between charges. These mixtures of sebum and dead skin cells are a source of nutrition for bacteria such P. acnes, resulting in inflammation.1

Acne is a complex process that defies a simple solution. Since acne manifests on the surface of the skin, topical agents are a major method of treatment. However, many topical treatments have diminished efficacy due to their inability to penetrate deep into the follicle. Also, many topical treatments, while effective, have harsh, drying or irritating effects on the skin, resulting in poor patient compliance.2 For example 10% benzoyl peroxide (BPO) commonly causes erythema, burning, and irritant dermatitis and can also bleach hair and clothes.3-5

To address these problems, a new acne treatment using a novel microgel complex that penetrates sebum on the skin and around follicles to deliver medication deep into the follicle has been developed. 6 This novel complex has demonstrated the ability to enhance the delivery of medication into follicles in vivo using multiple mechanisms of action, allowing it to target multiple factors that contribute to Acne vulgaris while also demonstrating excellent skin tolerance and high patient compliance.

Properties of the Microgel Complex

The microgel complex has unique sebum solubilizing properties, enhanced skin penetration and rapid antibacterial action without inducing oxidative stress or compromising skin barrier function. The microgel complex contains C12-15 alkyl lactate and cetyl lactate, 2 sebum dissolving components. Compared to other current, typically marketed, single-phase system acne products, acne treatments with the microgel complex are multiple-phase systems. The typical diameter of the microgel droplets was determined to be approximately 10 μm. Each microgel droplet contains the sebum solubilizing components and concentrated levels of salicylic acid (1.6-fold higher versus the external continuous phase) as demonstrated by reverse-phase isocratic high performance liquid chromatography (Agilent HPLC 1100).

In order to demonstrate the ability of the microgel to solubilize sebum, model sebum compositions were formulated with triglycerides, wax esters, squalene, free fatty acids, cholesterol esters, and cholesterol based on the percentages found in human sebum.7 At room temperature, the model sebum is a white waxy substance. Using a precision micropipette, sebum (50 μl) and the test agent or investigative ingredient (100 μl) were added to a 200 μl clear vial. After warming to 32 °C, the vials were visually

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