Han Xintong, Yan Qiusi, Gao Ning, Kang Yan, Li Na, Zou Aihua
The Education Ministry Key Lab of Resource Chemistry, Joint International Research Laboratory of Resource Chemistry, Shanghai Key Laboratory of Rare Earth Functional Materials, College of Chemistry and Materials Science, Shanghai Normal University, 100 Guilin RD, Shanghai 200234, China.
School of Chemistry and Molecular Engineering, East China University of Science and Technology, Shanghai 200237, China.
Langmuir. 2025 Feb 11;41(5):3278-3290. doi: 10.1021/acs.langmuir.4c04187. Epub 2025 Jan 27.
Ascorbyl tetraisopalmitate (VC-IP) is a novel form of ascorbic acid characterized by reduced water solubility due to complete acylation with palmitate. This study investigated the potential cosmetic application of VC-IP when encapsulated in lyotropic liquid crystal nanoparticles (VC-IP LCNPs) by using a high-pressure homogenization (HPH) method. The particle size, zeta potential, and polydispersity index (PDI) of the obtained VC-IP LCNPs were determined as 158.8 ± 3.2 nm, -35.1 ± 2.8 mV, and 0.12 ± 0.02, respectively. The drug loading (DL%) of the VC-IP LCNPs was approximately 35.1%. Morphological changes in LCNPs, transitioning from a sponge phase to vesicles, confirmed the successful loading of VC-IP, as demonstrated by transmission electron microscopy (Cryo-TEM) and small-angle X-ray scattering (SAXS) experiments. The sustained release of VC-IP was also observed through the Franz transdermal diffusion test, indicating that VC-IP LCNPs facilitated the sustained-release effect of VC-IP into the skin. VC-IP LCNPs exhibited good biocompatibility, showing nontoxicity to HaCaT cells and zebrafish embryos. Raman distribution imaging confirmed that VC-IP successfully penetrated the stratum corneum and reached the dermis. In assessments of whitening effects, VC-IP LCNPs significantly the reduced reactive oxygen species (ROS) content in zebrafish and melanin areas in the heads of zebrafish. Furthermore, VC-IP LCNPs effectively inhibited tyrosinase activity and the proliferation of A375 cells compared with pure VC-IP. Additionally, VC-IP LCNPs significantly reduced the melanin area in the heads of zebrafish. Therefore, the developed VC-IP LCNPs present a promising carrier for the enhanced application of active ingredients, such as VC-IP in whitening products.
四异棕榈酸抗坏血酸酯（VC - IP）是一种新型抗坏血酸形式，其特点是由于被棕榈酸完全酰化而水溶性降低。本研究通过高压均质（HPH）法研究了包裹在溶致液晶纳米颗粒（VC - IP LCNPs）中的VC - IP的潜在化妆品应用。所得VC - IP LCNPs的粒径、zeta电位和多分散指数（PDI）分别测定为158.8±3.2 nm、-35.1±2.8 mV和0.12±0.02。VC - IP LCNPs的载药量（DL%）约为35.1%。通过透射电子显微镜（冷冻透射电镜，Cryo - TEM）和小角X射线散射（SAXS）实验表明，LCNPs从海绵相转变为囊泡的形态变化证实了VC - IP的成功负载。通过Franz透皮扩散试验还观察到VC - IP的持续释放，表明VC - IP LCNPs促进了VC - IP向皮肤的持续释放作用。VC - IP LCNPs表现出良好的生物相容性，对HaCaT细胞和斑马鱼胚胎无毒。拉曼分布成像证实VC - IP成功穿透角质层并到达真皮。在美白效果评估中，VC - IP LCNPs显著降低了斑马鱼中的活性氧（ROS）含量以及斑马鱼头部的黑色素区域。此外，与纯VC - IP相比，VC - IP LCNPs有效抑制了酪氨酸酶活性和A375细胞的增殖。另外，VC - IP LCNPs显著减少了斑马鱼头部的黑色素区域。因此，所开发的VC - IP LCNPs为美白产品中增强活性成分（如VC - IP）的应用提供了一种有前景的载体。
