Piazzini Vieri, Rosseti Chiara, Bigagli Elisabetta, Luceri Cristina, Bilia Anna Rita, Bergonzi Maria Camilla
Department of Chemistry, University of Florence, Sesto Fiorentino, Florence, Italy.
NEUROFARBA, Department of Neurosciences, Psychology, Drug Research and Child Health, Section of Pharmacology and Toxicology, University of Florence, Florence, Italy.
Planta Med. 2017 Oct;83(14-15):1184-1193. doi: 10.1055/s-0043-110052. Epub 2017 May 4.
The present study explores the potential of nanoemulsion, a lipid drug delivery system, to improve solubility and oral absorption of extract. The optimized formulation contained 40 mg/mL of commercial extract (4 % w/w) and it was composed of 2.5 g labrasol (20 %) as the oil phase, 1.5 g cremophor EL as the surfactant, and 1 g labrafil as the cosurfactant (mixture surfactant/cosurfactant, 20 %).The system was characterized by dynamic light scattering, transmission electron microscopy, and HPLC-DAD analyses in order to evaluate size, homogeneity, morphology, and encapsulation efficiency. Physical and chemical stabilities were assessed during 40 days at 4 °C and 3 months at 25 °C. Stability in simulated gastric fluid followed by simulated intestinal conditions was also considered. permeation studies were performed to determine the suitability of the prepared nanoemulsion for oral delivery. Different models such as the parallel artificial membrane permeability assay and Caco-2 cell lines were applied.The nanoemulsion showed a good solubilizing effect of the extract, with a pronounced action also on its permeability, in respect to a saturated aqueous solution. The Caco-2 test confirmed the parallel artificial membrane permeability assay results and they revealed the suitability of the prepared nanoemulsion for oral delivery.
本研究探讨了脂质药物递送系统纳米乳剂改善提取物溶解度和口服吸收的潜力。优化后的制剂含有40mg/mL的市售提取物（4%w/w），由2.5g Labrasol（20%）作为油相、1.5g聚氧乙烯蓖麻油（Cremophor EL）作为表面活性剂和1g Labrafil作为助表面活性剂组成（表面活性剂/助表面活性剂混合物，20%）。该系统通过动态光散射、透射电子显微镜和HPLC-DAD分析进行表征，以评估粒径、均匀性、形态和包封率。在4℃下评估40天以及在25℃下评估3个月期间的物理和化学稳定性。还考虑了在模拟胃液随后模拟肠道条件下的稳定性。进行渗透研究以确定所制备的纳米乳剂用于口服给药的适用性。应用了不同的模型，如平行人工膜通透性试验和Caco-2细胞系。与饱和水溶液相比，纳米乳剂对提取物显示出良好的增溶作用，对其渗透性也有显著影响。Caco-2试验证实了平行人工膜通透性试验的结果，表明所制备的纳米乳剂适用于口服给药。
