Bhupinder Kaur, Newton Maria J
Department of Pharmaceutics, Rayat-Bahra Institute of Pharmacy, Rayat-Bahra University, Punjab. India.
Recent Pat Drug Deliv Formul. 2017;11(2):132-146. doi: 10.2174/1872211311666170117123403.
The fractionated coconut oil based Solid Lipid Nanoparticles (SLNs) of Acyclovir (ACV) were fabricated in two batches by using Glyceryl mono stearate (GMS) and Lipoid S75 (Fat free soybean phospholipids with 70% phosphatidylcholine-Lipoid GmbH, Germany). The research was focused on developing ACV-SLN by using high pressure hot-homogenization technique. The ingredients were used in different concentrations and ratios to identify the best formulation design.
The GMS with Fractionated coconut oil and Lipoid S75 with Fractionated coconut oil were used in various concentrations in formulation design to assess the impact on the fabrication and evaluation of SLNs. The SLNs were subjected to various characterization techniques such as XRD (X-Ray Diffraction), FTIR (Fourier transform infrared study), master sizer analysis and zeta potential. The mean particle size was determined by master sizer and zeta sizer. Transmission Electron Microscopy (TEM) was used as a tool to analyze the morphology and other features. The zeta potential and drug Entrapment Efficiency (EE%) were also determined. The drug release time profile was studied in vitro study with the utilization of dialysis membrane technique as well as by wistar rat skin. The most recent patents related to the current research topic were also discussed.
The Zeta potential of the best formulation from GMS batch GNE5 was found to be -2.62mV as the preparation was very viscous with low zeta potential. The better results of Lipoid S75 batch LS4 were found to be 23.23mV which was within the recommended range. The formulations prepared with Lipoid S75, LS4 showed narrow distribution size of 53.46nm and the uniformity was found to be 14.1. The formulation LS4 demonstrated the lowest distribution with of 6.8, 14.5, 139.1nm respectively amongst all the formulations.
SLN dispersions exhibited the average size in nano range. SLNs with small particle size found to have predetermined encapsulation efficiency and relatively high loading capacity and predetermined in vitro drugrelease profile. The lipoid S and Pluronic F68 nanoparticles are found to be superior to Conventional GMSand tween 80 nanoparticles in terms of particles size, stability and zetapotential.
使用单硬脂酸甘油酯（GMS）和Lipoid S75（含70%磷脂酰胆碱的无脂大豆磷脂，德国Lipoid GmbH公司）分两批制备基于分馏椰子油的阿昔洛韦（ACV）固体脂质纳米粒（SLNs）。该研究聚焦于采用高压热均质技术开发ACV-SLN。使用不同浓度和比例的成分来确定最佳配方设计。
在配方设计中使用不同浓度的GMS与分馏椰子油以及Lipoid S75与分馏椰子油，以评估其对SLNs制备和评估的影响。对SLNs进行各种表征技术，如XRD（X射线衍射）、FTIR（傅里叶变换红外研究）、粒度分析仪分析和zeta电位测定。通过粒度分析仪和zeta粒度仪测定平均粒径。使用透射电子显微镜（TEM）作为工具分析形态和其他特征。还测定了zeta电位和药物包封率（EE%）。利用透析膜技术以及通过Wistar大鼠皮肤进行体外研究，考察药物释放时间曲线。还讨论了与当前研究主题相关的最新专利。
GMS批次GNE5的最佳配方的zeta电位为-2.62mV，因为该制剂非常粘稠且zeta电位较低。Lipoid S75批次LS4的较好结果为23.23mV，在推荐范围内。用Lipoid S75制备的LS4配方显示出窄分布尺寸为53.46nm，均匀度为14.1。在所有配方中，LS4配方的分布分别最低，为6.8、14.5、139.1nm。
SLN分散体呈现纳米级的平均尺寸。发现粒径小的SLNs具有预定的包封效率、相对较高的载药量和预定的体外药物释放曲线。在粒径、稳定性和zeta电位方面，Lipoid S和普朗尼克F68纳米粒优于传统的GMS和吐温80纳米粒。
