Reduction of Ultraviolet- and Heat-Induced Aging Using Betulin-Loaded Arginine-Caprylate Self-Assembly: Randomized Double-Blind Clinical Trials.

IF 2.8 4区医学 Q3 DERMATOLOGY

Skin Research and Technology Pub Date : 2026-05-01 DOI:10.1111/srt.70361

Koo Chul Kwon, Mi Jung Kim, Sang A Yoon

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引用次数: 0

Abstract

Background: Betulin exhibits potent antibacterial, anti-inflammatory, and antioxidant properties, effectively preventing ultraviolet (UV)- and heat-induced skin aging. Its limited solubility in cosmetic solvents restricts its application.

Methods: To enhance betulin's applicability, a self-assembled nanocarrier, arginine-caprylate ion pair loaded with betulin (B-ACS), was developed. Structural properties, loading efficiency, skin permeability, and antioxidant activity were assessed. UVB-induced damage was examined in human keratinocytes (HaCaT; n = 3) by measuring inflammatory cytokines and matrix metalloproteinases (MMPs) via ELISA. Three-dimensional reconstructed human skin models were exposed to UVA (10 J/cm²) to evaluate collagen and aquaporin-3 protection. A pilot randomized, double-blind, placebo-controlled clinical trial (n = 12, 2 weeks) assessed 3 % (w/w) B-ACS cream on UV- and infrared-induced skin damage.

Results: B-ACS showed a particle size of 236.9 ± 10.3 nm, 98.3 ± 1.3 % encapsulation efficacy, and superior reactive oxygen species (ROS) scavenging (IC50 = 4.87 ppm) compared to free betulin (IC50 = 8.26 ppm). In HaCaT cells, B-ACS significantly reduced UVB-induced inflammatory cytokine and MMP expressions (p < 0.05). In reconstructed skin, it prevented UVA-induced collagen and aquaporin-3 degradation. Clinically, 3% B-ACS cream significantly improved elasticity (1.69-fold), brightness (2.59-fold), and pigmentation (1.91-fold); transepidermal water loss (TEWL) and heat-aging markers decreased 1.39-fold and 1.63-fold versus placebo, respectively (p < 0.05).

Conclusion: B-ACS enhances betulin's solubility and delivery, offering potent efficacy against UV- and heat-induced aging.

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利用白桦素负载的精氨酸-辛酸盐自组装减少紫外线和热诱导的衰老：随机双盲临床试验。

背景：桦木素具有有效的抗菌、抗炎和抗氧化特性，能有效防止紫外线和热致皮肤老化。它在化妆品溶剂中的溶解度有限，限制了它的应用。方法：为提高桦木素的适用性，制备了一种自组装的纳米载体——载桦木素精氨酸-辛酸离子对（B-ACS）。对其结构性能、负载效率、透皮性和抗氧化活性进行了评估。通过ELISA检测炎症因子和基质金属蛋白酶（MMPs），检测uvb诱导的人角化细胞（HaCaT, n = 3）损伤。三维重建人体皮肤模型暴露于UVA （10 J/cm2）下，以评估胶原蛋白和水通道蛋白-3的保护作用。一项随机、双盲、安慰剂对照的临床试验（n = 12, 2周）评估了3% (w/w) B-ACS乳膏对紫外线和红外线诱导的皮肤损伤的影响。结果：B-ACS的粒径为236.9±10.3 nm，包封率为98.3%±1.3%，对活性氧（ROS）的清除能力（IC50 = 4.87 ppm）优于游离白桦素（IC50 = 8.26 ppm）。在HaCaT细胞中，B-ACS显著降低uvb诱导的炎症细胞因子和MMP的表达（p < 0.05）。在重建皮肤中，它可以阻止uva诱导的胶原蛋白和水通道蛋白-3降解。临床上，3% B-ACS乳膏可显著改善弹性（1.69倍）、亮度（2.59倍）和色素沉着（1.91倍）；经皮失水（TEWL）和热老化指标分别比安慰剂降低1.39倍和1.63倍（p < 0.05）。结论：B-ACS增强了白桦素的溶解度和传递能力，具有抗紫外线和热老化的作用。

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来源期刊

Skin Research and Technology 医学-皮肤病学

CiteScore

3.30

自引率

9.10%

发文量

审稿时长

6-12 weeks

期刊介绍： Skin Research and Technology is a clinically-oriented journal on biophysical methods and imaging techniques and how they are used in dermatology, cosmetology and plastic surgery for noninvasive quantification of skin structure and functions. Papers are invited on the development and validation of methods and their application in the characterization of diseased, abnormal and normal skin. Topics include blood flow, colorimetry, thermography, evaporimetry, epidermal humidity, desquamation, profilometry, skin mechanics, epiluminiscence microscopy, high-frequency ultrasonography, confocal microscopy, digital imaging, image analysis and computerized evaluation and magnetic resonance. Noninvasive biochemical methods (such as lipids, keratin and tissue water) and the instrumental evaluation of cytological and histological samples are also covered. The journal has a wide scope and aims to link scientists, clinical researchers and technicians through original articles, communications, editorials and commentaries, letters, reviews, announcements and news. Contributions should be clear, experimentally sound and novel.