Rocha Kamilla Amaral David, Krawczyk-Santos Anna Paula, Andrade Lígia Marquez, Souza Luana Clara de, Marreto Ricardo Neves, Gratieri Tais, Taveira Stephânia Fleury
Laboratory of Nanosystems and Drug Delivery Devices (NanoSYS), School of Pharmacy, Universidade Federal de Goiás (UFG), Rua 240, Setor Leste Universitário, 74.605-170, Goiânia, GO, Brazil.
Laboratory of Food, Drugs and Cosmetics (LTMAC), University of Brasilia (UnB), Campus Universitário Darcy Ribeiro, Asa Norte, 70.910-900, Brasília, DF, Brazil.
Int J Pharm. 2017 Oct 5;531(1):292-298. doi: 10.1016/j.ijpharm.2017.08.115. Epub 2017 Aug 30.
Voriconazole-loaded nanostructured lipid carriers (VOR-NLC) were developed and drug penetration evaluated in porcine hooves in vitro. Synergistic effect of urea (Ur), selected among other known chemical enhancers according to hoof hydration potential, was also evaluated. VOR-NLC presented a high encapsulation efficiency (74.52±2.13%), approximate mean diameter of 230nm and were positively charged (+27.32±2.74mV). Stability studies indicated they were stable under refrigeration (4±2°C) for up to 150days. SEM images revealed hooves treated with VOR-NLC and VOR-NLC-Ur suffered a disturbance on the surface depicting high roughness and porosity. Permeation data showed a substantial VOR amount retained in superficial hooves sections independent of the formulation used (2.42±0.26; 2.52±0.36 and 2.41±0.60μg/cm for unloaded VOR, VOR-NLC and VOR-NLC-Ur, respectively, p>0.05). Still, successive extractions, revealed the amount of VOR retained in deeper regions was significantly higher when VOR-NLC or VOR-NLC-Ur was used (0.17±0.04, 0.47±0.14 and 0.36±0.07μg/cm for unloaded VOR, VOR-NLC and VOR-NLC-Ur, respectively, p<0.05). Such results indicate NLC are promising formulations for the management of onychomycosis. Further studies in diseased nail plates are necessary.
制备了载伏立康唑的纳米结构脂质载体（VOR-NLC），并在体外评估了其在猪蹄中的药物渗透情况。根据蹄部水合潜力，从其他已知化学增强剂中选择了尿素（Ur），并评估了其协同作用。VOR-NLC具有较高的包封率（74.52±2.13%），平均直径约为230nm，且带正电荷（+27.32±2.74mV）。稳定性研究表明，它们在冷藏（4±2°C）条件下可稳定保存长达150天。扫描电子显微镜图像显示，用VOR-NLC和VOR-NLC-Ur处理的蹄部表面出现紊乱，呈现出高粗糙度和孔隙率。渗透数据显示，无论使用何种制剂，浅表蹄部切片中保留的伏立康唑量基本相同（未负载伏立康唑组、VOR-NLC组和VOR-NLC-Ur组分别为2.42±0.26、2.52±0.36和2.41±0.60μg/cm，p>0.05）。然而，连续萃取显示，当使用VOR-NLC或VOR-NLC-Ur时，更深区域保留的伏立康唑量显著更高（未负载伏立康唑组、VOR-NLC组和VOR-NLC-Ur组分别为0.17±0.04、0.47±0.14和0.36±0.07μg/cm，p<0.05）。这些结果表明，纳米结构脂质载体是治疗甲癣的有前景的制剂。有必要对患病甲板进行进一步研究。
