Resveratrol-loaded solid lipid nanoparticles versus nanostructured lipid carriers: evaluation of antioxidant potential for dermal applications.
Resveratrol-loaded solid lipid nanoparticles versus nanostructured lipid carriers: evaluation of antioxidant potential for dermal applications.
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DOI：
10.2147/ijn.s29710
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发表时间：
2012
影响因子：
8
通讯作者：
Ozer O
中科院分区：
文献类型：
--
作者：
Gokce EH;Korkmaz E;Dellera E;Sandri G;Bonferoni MC;Ozer O
自由基氧（ROS）的过量产生是皮肤病变的一个因素。白藜芦醇（RSV）是一种有效的抗氧化剂。固体脂质纳米颗粒（SLN）和纳米结构脂质载体（NLC）可以确保紧密接触，增加药物进入皮肤的吸收量。在本研究中，RSV被加载到SLN和NLC中用于皮肤应用。采用Compritol 888ATO、Myglyol、Poloxamer188和Tween80进行高剪切均质制备纳米颗粒。测定了样品的粒径（PS）、多分散性指数（PI）、ζ电位（ZP）、包封效率（EE）和产率。差示扫描量热分析（DSC）和形态透射电子显微镜（TEM）检查。通过细胞毒性研究优化RSV浓度，并用细胞荧光法监测细胞内ROS的净积累。测定大鼠腹部不同皮肤层RSV的数量。均匀RSV-SLN和RSV-NLC的PS分别为287.2 nm±5.1和110.5 nm±1.3。ZP依次为- 15.3 mV±0.4和- 13.8 mV±0.1。在NLC系统中，药物EE高出18%。透射电镜研究表明，壳模型中的药物与SLN有关，NLC中的脂质熔点略低。在细胞培养研究中，低于50 μM的浓度被确定为适合于SLN和NLC的RSV浓度。在细胞荧光学研究中，RSV-NLC显示较少的荧光，表明较少的ROS产生。离体皮肤研究表明，NLC更有效地将RSV携带到表皮。本研究表明，两种脂质纳米颗粒在浓度为50 μM时均具有抗氧化性能。当两种系统进行比较时，NLC深入皮肤。rsv负载的NLC具有更小的PS和更高的载药量，在皮肤应用方面优于SLN。
Excessive generation of radical oxygen species (ROS) is a contributor to skin pathologies. Resveratrol (RSV) is a potent antioxidant. Solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) can ensure close contact and increase the amount of drug absorbed into the skin. In this study, RSV was loaded into SLN and NLC for dermal applications. Nanoparticles were prepared by high shear homogenization using Compritol 888ATO, Myglyol, Poloxamer188, and Tween80. Particle size (PS), polydispersity index (PI), zeta potential (ZP), drug entrapment efficiency (EE), and production yield were determined. Differential scanning calorimetry (DSC) analysis and morphological transmission electron microscopy (TEM) examination were conducted. RSV concentration was optimized with cytotoxicity studies, and net intracellular accumulation of ROS was monitored with cytofluorimetry. The amount of RSV was determined from different layers of rat abdominal skin. PS of uniform RSV-SLN and RSV-NLC were determined as 287.2 nm ± 5.1 and 110.5 nm ± 1.3, respectively. ZP was −15.3 mV ± 0.4 and −13.8 mV ± 0.1 in the same order. The drug EE was 18% higher in NLC systems. TEM studies showed that the drug in the shell model was relevant for SLN, and that the melting point of the lipid in NLC was slightly lower. Concentrations below 50 μM were determined as suitable RSV concentrations for both SLN and NLC in cell culture studies. RSV-NLC showed less fluorescence, indicating less ROS production in cytofluorometric studies. Ex vivo skin studies revealed that NLC are more efficient in carrying RSV to the epidermis. This study suggests that both of the lipid nanoparticles had antioxidant properties at a concentration of 50 μM. When the two systems were compared, NLC penetrated deeper into the skin. RSV-loaded NLC with smaller PS and higher drug loading appears to be superior to SLN for dermal applications.