Shah Hirva A, Patel Rakesh P
Department of Pharmaceutics, Vidyabharti Trust College of Pharmacy, Umrakh Bardoli, Surat, India.
Department of Pharmacecutics, Shree S K Patel College of Pharmaceutical Education and Research, Mehsana, Gujarat, India.
Int J Pharm Investig. 2015 Jan-Mar;5(1):20-7. doi: 10.4103/2230-973X.147229.
The main objective of this study is to formulate polymeric nanoparticles (NPs) loaded with zaltoprofen, an NSAID drug. The optimization, in terms of polymer concentration, stabilizer concentration and pH of the formulation was employed by 3-factor-3-level Box-Behnken experimental design.
The NPs of zaltoprofen were fabricated using chitosan and alginate as polymers by ionotropic gelation. The ionic interaction between the ionic polymers was studied using Fourier transform infrared and differential scanning calorimetry study.
For different formulation the average particle size ranged between 156 ± 1.0 nm and 554 ± 2.8 nm. The drug entrapment ranged between 61.40% ± 3.20% and 90.20% ± 2.47%. The ANOVA results exhibited that all the three factors were significant. The resultant optimized batch was characterized by particle size 156.04 ± 1.4 nm, %entrapment efficacy 88.67% ± 2.0%, zetapotential + 25.3 mV and polydispersity index 0.320. The scanning electron microscopy showed spherical NPs of average size 99.5 nm. The optimized NPs were loaded in carbopol gel, which was subjected to study of drug content, viscosity, spreadability, in vitro drug diffusion and in vivo antiinflammatory test on rats.
This study showed that zaltoprofen NPs prepared using the ratio of polymer CS:AG:1:1.8, stabilizer concentration 0.98% and pH 4.73 was found to be of optimized particle size, maximum drug entrapment. The NPs loaded gel showed controlled release for 12 h following Korsmeryer-peppas model of the diffusion profile. The in vivo antiinflammatory study showed prolonged effect of NPs loaded gel for 10 h.
本研究的主要目的是制备载有非甾体抗炎药扎托洛芬的聚合物纳米粒（NPs）。采用三因素三水平的Box-Behnken实验设计，对聚合物浓度、稳定剂浓度和制剂pH进行优化。
以壳聚糖和海藻酸钠为聚合物，通过离子凝胶法制备扎托洛芬纳米粒。利用傅里叶变换红外光谱和差示扫描量热法研究离子聚合物之间的离子相互作用。
不同制剂的平均粒径在156±1.0nm至554±2.8nm之间。药物包封率在61.40%±3.20%至90.20%±2.47%之间。方差分析结果表明，所有三个因素均具有显著性。最终优化批次的特征为粒径156.04±1.4nm、包封率88.67%±2.0%、zeta电位+25.3mV和多分散指数0.320。扫描电子显微镜显示平均粒径为99.5nm的球形纳米粒。将优化后的纳米粒载入卡波姆凝胶中，对其进行药物含量、粘度、铺展性、体外药物扩散和大鼠体内抗炎试验研究。
本研究表明，采用聚合物CS:AG:1:1.8的比例、稳定剂浓度0.98%和pH 4.73制备的扎托洛芬纳米粒具有优化的粒径和最大的药物包封率。载纳米粒的凝胶按照Korsmeryer-peppas扩散模型显示出12小时的控释效果。体内抗炎研究表明，载纳米粒的凝胶具有10小时的延长作用。
