Efficacy of Heparinoid Cream Containing Pseudo-Ceramide for Remission of Atopic Dermatitis

Abstract

Purpose: Atopic dermatitis (AD) is characterized by chronic inflammation, which frequently recurs, is exacerbated, and enters remission. A maintenance remission period is important for AD patients. We developed a formulation for use during AD remission, containing heparinoid and pseudo-ceramide that forms a lamellar structure. We evaluated the allergen permeability and examined the formulation's efficacy in maintaining remission in patients with AD. Materials and Methods: Seventeen AD patients applied a cream containing 0.3% heparinoid and pseudo-ceramide (test cream group, n = 10), or a general cream containing 0.3% heparinoid (control cream group, n = 7) to their arm for four weeks after inducing remission with the application of a steroid cream for two weeks. Results:The lamellar structure of the test cream was confirmed with small-and wide-angle x-ray scattering analysis and observation by transmission electron microscopy. The test cream inhibited the penetration of V8 protease significantly compared to the control cream in vitro. According to AD severity score by dermatologists, the effects remission maintenance of the test cream group were comparable to those of the control cream group. However, the test cream group had a significantly increased skin hydration value compared to the control cream group. A significant decrease in transepidermal water loss, an indicator of skin barrier function, was shown in the test cream group compared to the control cream group. Conclusion:The cream with lamellar structures containing heparinoid and pseudoceramides may inhibit allergen penetration. Moreover, skin properties improved during the remission period; thus, the formulation we developed was suitable for use during the AD remission period.

Combination of a Topical Anti-Inflammatory Drug and a Moisturizer, Both with a Lamellar Structure Containing Synthetic Pseudo-Ceramides, for the Treatment of Patients with Mild-to-Moderate Atopic Dermatitis

“…It should be noted that coatings of formulations with lamellar structure also have a physical barrier function that suppresses allergen entry. 24 Interestingly, the improvement in SC function in the present study was most prominent in the participants with weak barrier function at the outset ( Figure 3A ). These participants experienced a significant decrease in the TEWL and an improved Cer [NP]/[NS] ratio, which is an indicator of epidermal turnover ( Figure 3C ).…”

“… 23 Furthermore, we found that a formulation containing synthetic pseudo-ceramides and a heparinoid that formed a lamellar structure after application and drying exhibited physical barrier function, effectively inhibiting allergen permeation. 24 Our assessment of the above-mentioned heparinoid formulation during AD remission revealed notable improvements in skin hydration and a reduction in the TEWL, accompanied by alleviation of itchiness. Taken together, these observations demonstrated that steroid and heparinoid formulations with a lamellar structure exhibit greater efficacy as therapeutic agents for AD than formulations without a lamellar structure.…”

“… 16 Previous research evaluated the efficacy of steroid and heparinoid formulations that form a lamellar structure after application and drying for the treatment of mild to moderate AD cases, with a significant improvement in stratum corneum function compared to that achieved by formulations without a lamellar structure. 23 , 24 …”

Natural Ingredients of Transdermal Drug Delivery Systems as Permeation Enhancers of Active Substances through the Stratum Corneum

“…Substances applied externally that penetrate the structure of the SC interact with its components. Substances containing compounds that physiologically occur in the SC, such as ceramides, cholesterol and its sulfate, and fatty acids affect the proportions of their counterparts resulting in supplementation of their deficiencies. − Conversely, they may disrupt the natural quantitative balance of lipid components to induce an increase in skin permeability. It has been found that changes in the composition and chain length of fatty acids present in their free forms as well as bound to SC ceramides change their melting point and membrane permeability .…”

Efficacy of Topical Application of a Skin Moisturizer Containing Pseudo-Ceramide and a Eucalyptus Leaf Extract on Atopic Dermatitis: A Review

“…A cream containing heparinoid and P-Cer forms lamellar structures that result in inhibiting allergen penetration with an improvement in SC functions. This cream is effective in maintaining the AD remission period [ 91 ]. The cream with steroids and P-Cer, which also forms a lamellar structure, not only demonstrates anti-inflammatory effects but also significantly improves SC functions [ 88 ].…”