School of Bioscience and Bioengineering, South China University of Technology, Guangzhou 510006, China.
Molecules. 2022 Sep 26;27(19):6328. doi: 10.3390/molecules27196328.
Psoriasis is a chronic inflammatory skin disorder accompanied by excessive keratinocyte proliferation. Erianin (Eri) is an ideal drug candidate for inhibiting proliferation and inducing apoptosis in the treatment of psoriasis. However, Eri's poor water solubility and low penetration activity across the skin hinder its application in local medicine. In this study, we developed a novel photo-responsive dendritic mesoporous silica nanoparticle-based carrier to deliver erianin, improved its bioavailability, and achieved sustained-release effects. Spiropyran (SP), 3-aminopropyltriethoxysilane (APTES), and perfluorodecyltriethoxysilane (PFDTES) were conjugated to the outer surface, which allowed Eri to be released in response to UV radiation. The physicochemical properties of photo-responsive dendritic mesoporous silica nanoparticles (Eri-DMSN@FSP) were characterized via multiple techniques, such as using a Fourier-transform infrared spectrometer, a high-resolution transmission electron microscope, and nuclear magnetic resonance (NMR) spectroscopy. The anti-proliferative properties and light-triggered release of erianin-loaded photo-responsive dendritic mesoporous silica nanoparticles were assessed via the MTT assay and a drug release study in vitro. Erianin-loaded photo-responsive dendritic mesoporous silica nanoparticles (UV) exhibit a significantly enhanced HaCat cell-inhibiting efficacy compared to other formulations, as demonstrated by their extremely low cell viability of 10.0% (concentration: 500 mg/mL), indicating their capability to release a drug that responds to UV radiation. The cellular uptake of photo-responsive dendritic mesoporous silica nanoparticles (DMSN@FSP) was observed via confocal laser scanning microscopy (CLSM). These experimental results show that Eri-DMSN@FSP could be effectively endocytosed into cells and respond to ultraviolet light to release Eri, achieving a more effective psoriasis treatment. Therefore, this drug delivery system may be a promising strategy for addressing the question of Eri's delivery and psoriasis therapy.
银屑病是一种慢性炎症性皮肤病,伴有角质形成细胞过度增殖。杨梅素(Eri)是一种理想的药物候选物,可用于抑制增殖并诱导银屑病细胞凋亡。然而,Eri 的水溶性差,穿过皮肤的渗透活性低,阻碍了其在局部药物中的应用。在这项研究中,我们开发了一种新型光响应树枝状介孔硅纳米粒子载体来递送杨梅素,提高其生物利用度,并实现了持续释放效果。螺吡喃(SP)、3-氨丙基三乙氧基硅烷(APTES)和全氟癸基三乙氧基硅烷(PFDTES)被接枝到外表面,使 Eri 能够响应紫外线辐射而释放。通过傅里叶变换红外光谱仪、高分辨率透射电子显微镜和核磁共振(NMR)光谱等多种技术对光响应树枝状介孔硅纳米粒子(Eri-DMSN@FSP)的理化性质进行了表征。通过 MTT 测定和体外药物释放研究评估了载杨梅素的光响应树枝状介孔硅纳米粒子的抗增殖性能和光触发释放。与其他制剂相比,载杨梅素的光响应树枝状介孔硅纳米粒子(UV)对 HaCat 细胞的抑制效果显著增强,其细胞活力极低,为 10.0%(浓度:500mg/mL),表明其能够释放对紫外线有反应的药物。通过共聚焦激光扫描显微镜(CLSM)观察光响应树枝状介孔硅纳米粒子(DMSN@FSP)的细胞摄取。这些实验结果表明,Eri-DMSN@FSP 可以有效地被细胞内吞,并对紫外线光响应释放 Eri,从而实现更有效的银屑病治疗。因此,这种药物传递系统可能是解决 Eri 传递和银屑病治疗问题的一种有前途的策略。