Department of Pharmaceutics, Institute of Technology, Banaras Hindu University, Varanasi, Uttar Pradesh, India.
Colloids Surf B Biointerfaces. 2011 Oct 15;87(2):280-8. doi: 10.1016/j.colsurfb.2011.05.030. Epub 2011 May 26.
In the present study eugenol loaded solid lipid nanoparticles (SLN) was prepared and characterized for particle size, polydispersity index, zeta potential, encapsulation efficiency, in vitro release and in vivo antifungal activity. Effect of addition of liquid lipid (caprylic triglyceride) to solid lipid (stearic acid) on crystallinity of lipid matrix of SLN was determined by using Fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC) and X-ray diffraction (XRD) techniques. Transmission electron microscopy (TEM) was carried out to determine the morphology of SLN. In vivo antifungal activity of eugenol loaded lipid nanoparticles was evaluated by using a model of oral candidiasis in immunosuppressed rats. Particle size results showed that d(90) of SLN(1) (single lipid matrix) and SLN(2) (binary lipid matrix) was 332±14.2 nm and 87.8±3.8 nm, respectively. Polydispersity index was found to be in the range of 0.27-0.4 which indicate moderate size distribution. Encapsulation efficiency of SLN(2) (98.52%) was found to be more than that of SLN(1) (91.80%) at same lipid concentration (2%, w/v). Increasing of the solid lipid concentration from 2% (w/v) to 4% (w/v) resulted in increase in encapsulation efficiency and the particle size. SLN(2) shows faster release of eugenol than that of SLN(1) due to smaller size and presence of liquid lipid which provide less barriers to the diffusion of drug from matrix. TEM study reveals the spherical shape of SLN. FT-IR, DSC and XRD results indicate less crystallinity of SLN(2) than that of SLN(1). In vivo studies show no significant difference in log cfu value of all the groups at 0 day. At 8th day, log cfu value of group treated with saline (control), standard antifungal agent, eugenol solution, SLN(1) and SLN(2) was found to be 3.89±.032, 2.69, 3.39±.088, 3.19±.028 and 3.08±0.124, respectively. The in vivo study results indicate improvement in the antifungal activity of eugenol when administrated in the form of SLN.
在本研究中，制备了负载丁香酚的固体脂质纳米粒（SLN），并对其粒径、多分散指数、Zeta 电位、包封效率、体外释放和体内抗真菌活性进行了表征。采用傅里叶变换红外光谱（FT-IR）、差示扫描量热法（DSC）和 X 射线衍射（XRD）技术，研究了添加液体脂质（辛酸三甘油酯）对 SLN 脂质基质结晶度的影响。通过透射电子显微镜（TEM）确定了 SLN 的形态。采用免疫抑制大鼠口腔念珠菌病模型评价了负载丁香酚的脂质纳米粒的体内抗真菌活性。粒径结果表明，单脂质基质 SLN(1)和双脂质基质 SLN(2)的 d(90)分别为 332±14.2nm 和 87.8±3.8nm。多分散指数在 0.27-0.4 之间，表明粒径分布适中。在相同脂质浓度（2%，w/v）下，SLN(2)（98.52%）的包封效率高于 SLN(1)（91.80%）。随着固体脂质浓度从 2%（w/v）增加到 4%（w/v），包封效率和粒径均增加。由于粒径较小且存在液体脂质，SLN(2)中丁香酚的释放速度快于 SLN(1)，这为药物从基质中扩散提供了较少的障碍。TEM 研究表明 SLN 呈球形。FT-IR、DSC 和 XRD 结果表明，与 SLN(1)相比，SLN(2)的结晶度较低。体内研究结果表明，在第 0 天，所有组的 log cfu 值均无显著差异。在第 8 天，用生理盐水（对照）、标准抗真菌剂、丁香酚溶液、SLN(1)和 SLN(2)处理的组的 log cfu 值分别为 3.89±.032、2.69、3.39±.088、3.19±.028 和 3.08±0.124。体内研究结果表明，以 SLN 的形式给药可提高丁香酚的抗真菌活性。
