Arana Lide, Salado Clarisa, Vega Sandra, Aizpurua-Olaizola Oier, Arada Igor de la, Suarez Tatiana, Usobiaga Aresatz, Arrondo José Luis R, Alonso Alicia, Goñi Félix M, Alkorta Itziar
Unidad de Biofísica (CSIC, UPV/EHU), and Departamento de Bioquímica y Biología Molecular, Universidad del País Vasco (UPV/EHU), P.O. Box 644, 48080 Bilbao, Spain.
Innoprot, Parque Tecnológico de Bizkaia, Edificio 502, Ibaizabal Bidea, 48160 Elexalde Derio, Spain.
Colloids Surf B Biointerfaces. 2015 Nov 1;135:18-26. doi: 10.1016/j.colsurfb.2015.07.020. Epub 2015 Jul 17.
Solid lipid nanoparticles (SLN) composed of long-chain fatty acids (palmitic acid, stearic acid or arachidic acid), Epikuron 200 (purified phosphatidylcholine), and bile salts (cholate, taurocholate or taurodeoxycholate) have been prepared by dilution of a microemulsion. A total of five different systems were prepared, and characterized by photon correlation spectroscopy, transmission electron microscopy, differential scanning calorimetry, and infrared spectroscopy. The SLN formulation showing optimal properties (lowest size and polydispersity index and highest zeta potential) was obtained with stearic acid and taurodeoxycholate as cosurfactant. This formulation was loaded with Calendula officinalis extract, a natural compound used on ophthalmic formulations given its anti-inflammatory, emollient, and wound repairing activity. Calendula-loaded SLN preparations were characterized in order to determine loading capacity and entrapment efficiency. In vitro cytotoxicity and wound healing efficacy of Calendula-loaded SLN compared to that of a free plant extract were evaluated on a conjunctival epithelium cell line WKD. Our results suggest that this SLN formulation is a safe and solvent-free Calendula extract delivery system which could provide a controlled therapeutic alternative for reducing disease-related symptoms and improving epithelium repair in ocular surface.
由长链脂肪酸(棕榈酸、硬脂酸或花生酸)、Epikuron 200(纯化的磷脂酰胆碱)和胆盐(胆酸盐、牛磺胆酸盐或牛磺去氧胆酸盐)组成的固体脂质纳米粒(SLN)已通过微乳液稀释法制备。总共制备了五种不同的体系,并通过光子相关光谱、透射电子显微镜、差示扫描量热法和红外光谱进行了表征。以硬脂酸和牛磺去氧胆酸盐作为助表面活性剂获得了具有最佳性能(最低尺寸和多分散指数以及最高zeta电位)的SLN制剂。该制剂负载了金盏花提取物,鉴于其抗炎、润肤和伤口修复活性,金盏花提取物是一种用于眼科制剂的天然化合物。对负载金盏花的SLN制剂进行了表征,以确定其负载能力和包封效率。在结膜上皮细胞系WKD上评估了负载金盏花的SLN与游离植物提取物相比的体外细胞毒性和伤口愈合功效。我们的结果表明,这种SLN制剂是一种安全且无溶剂的金盏花提取物递送系统,可为减轻疾病相关症状和改善眼表上皮修复提供一种可控的治疗选择。