Department of Pharmacy, State University of Maringá (UEM), Maringá, Paraná 87020-900, Brazil.
i3S - Institute for Research and Innovation in Health, University of Porto, Rua Alfredo Allen, 208, 4200-135 Porto, Portugal; INEB - Institute of Biomedical Engineering, University of Porto, Rua Alfredo Allen, 208, 4200-135 Porto, Portugal.
Int J Pharm. 2020 May 30;582:119336. doi: 10.1016/j.ijpharm.2020.119336. Epub 2020 Apr 15.
Excessive exposure to solar radiation induces injurious effects on human skin. Our previous study evidenced that protocatechuic acid (P0) and ethyl protocatechuate (P2) act against photodamage and photoaging. The present study aimed to develop solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) for topical delivery of P0 or P2, as a strategy for photoprotection. Lipid nanoparticles exhibited mean particle size, polydispersity index, zeta potential and association efficiency between 200 and 400 nm, 0.160 to 0.460, -2.2 to -5.2 mV, and 60% to 80%, respectively. The formulations were stable for 3 months when stored at 4C and 25C/60% RH. SLNs/NLCs-P0 showed minor cytotoxicity effects compared with SLNs/NLCs-P2, in HaCat (keratinocytes) and HFF-1 (fibroblasts) cell lines. Additionally, bare NLCs exhibited less cytotoxicity effect, compared with bare SLNs. NLCs exhibited a controlled in vitro release of P0 and P2, and were able to protect the compounds against UVB degradation. Ex vivo permeability study showed that NLCs modulated P0 and P2 retention profiles on human skin layers. Furthermore, histological analysis of skin showed that NLCs-P0 did not cause morphological alterations, while NLCs-P2 showed a potential irritation effect in the skin structure. Based on these results, NLCs were considered a potential dermatological nanocarrier for P0 delivery.
过度暴露于太阳辐射会对人类皮肤造成伤害。我们之前的研究表明，原儿茶酸（P0）和 3-乙基-原儿茶酸（P2）可对抗光损伤和光老化。本研究旨在开发固体脂质纳米粒（SLN）和纳米结构脂质载体（NLC），以用于 P0 或 P2 的局部递送，作为一种光保护策略。脂质纳米粒的平均粒径、多分散指数、Zeta 电位和结合效率分别为 200-400nm、0.160-0.460、-2.2 至-5.2mV 和 60%-80%。当在 4°C 和 25°C/60%RH 下储存时，制剂在 3 个月内稳定。与 SLN/NLC-P2 相比，SLN/NLC-P0 对 HaCat（角质形成细胞）和 HFF-1（成纤维细胞）细胞系的细胞毒性较小。此外，与裸 SLN 相比，裸 NLC 的细胞毒性较小。NLC 表现出对 P0 和 P2 的控制释放，并且能够保护化合物免受 UVB 降解。体外透皮研究表明，NLC 调节了 P0 和 P2 在人皮肤层中的保留情况。此外，皮肤组织学分析表明，NLC-P0 不会引起皮肤形态改变，而 NLC-P2 显示出对皮肤结构的潜在刺激性影响。基于这些结果，NLC 被认为是 P0 递送的潜在皮肤科纳米载体。
