Department of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard, Hamdard Nagar, New Delhi, India.
Int J Nanomedicine. 2012;7:5705-18. doi: 10.2147/IJN.S35329. Epub 2012 Nov 9.
Chitosan (CS) nanoparticles of thymoquinone (TQ) were prepared by the ionic gelation method and are characterized on the basis of surface morphology, in vitro or ex vivo release, dynamic light scattering, and X-ray diffractometry (XRD) studies. Dynamic laser light scattering and transmission electron microscopy confirmed the particle diameter was between 150 to 200 nm. The results showed that the particle size of the formulation was significantly affected by the drug:CS ratio, whereas it was least significantly affected by the tripolyphosphate:CS ratio. The entrapment efficiency and loading capacity of TQ was found to be 63.3% ± 3.5% and 31.23% ± 3.14%, respectively. The drug-entrapment efficiency and drug-loading capacity of the nanoparticles appears to be inversely proportional to the drug:CS ratio. An XRD study proves that TQ dispersed in the nanoparticles changes its form from crystalline to amorphous. This was further confirmed by differential scanning calorimetry thermography. The flat thermogram of the nanoparticle data indicated that TQ formed a molecular dispersion within the nanoparticles. Optimized nanoparticles were evaluated further with the help of scintigraphy imaging, which ascertains the uptake of drug into the brain. Based on maximum concentration, time-to-maximum concentration, area-under-curve over 24 hours, and elimination rate constant, intranasal TQ-loaded nanoparticles (TQ-NP1) proved more effective in brain targeting compared to intravenous and intranasal TQ solution. The high drug-targeting potential and efficiency demonstrates the significant role of the mucoadhesive properties of TQ-NP1.
壳聚糖（CS）纳米粒的百里醌（TQ）是由离子凝胶法制备的，并根据表面形态、体外或离体释放、动态光散射和 X 射线衍射（XRD）研究进行了表征。动态激光光散射和透射电子显微镜证实粒径在 150 至 200nm 之间。结果表明，制剂的粒径显著受药物与 CS 的比例影响，而受三聚磷酸钠与 CS 的比例影响最小。TQ 的包封效率和载药量分别为 63.3%±3.5%和 31.23%±3.14%。纳米粒的药物包封效率和载药量似乎与药物与 CS 的比例成反比。XRD 研究证明，TQ 在纳米粒中分散，其形态从结晶态变为无定形态。差示扫描量热法进一步证实了这一点。纳米粒数据的平坦热谱表明，TQ 在纳米粒内形成了分子分散。优化后的纳米粒进一步通过闪烁成像进行评估，这确定了药物进入大脑的摄取情况。基于最大浓度、达到最大浓度的时间、24 小时内的曲线下面积和消除速率常数，与静脉内和鼻内 TQ 溶液相比，鼻内 TQ 载药纳米粒（TQ-NP1）在脑靶向方面更有效。高药物靶向潜力和效率表明 TQ-NP1 的黏膜黏附特性发挥了重要作用。
