川陈皮素纳米乳的理化性质及其在小鼠体内的分布

Characteristics of nobiletin-loaded nanoemulsion and its in vivo distribution in mice

本文制备了川陈皮素纳米乳(NOB-NE),考察了纳米乳载药前后的理化特性、稳定性及其在小鼠体内的分布情况。制得的川陈皮素纳米乳的粒径、表观黏度和pH值分别为(15.5±2.9)nm,(3.10±0.33)mPa.s,6.56±0.05,且稳定性好。小鼠各组织中川陈皮素的浓度采用HPLC法进行测定。纳米乳静脉注射给药后,脑和肾中药物浓度增加最为显著(P<0.01),同时靶向效率增大。结果显示,制得的NOB-NE质量稳定,且可改变药物在小鼠体内的分布,增强了药物的脑和肾靶向性。

The purpose of this study was to prepare the nobiletin-loaded nanoemulsions （NOB-NE） and study its in vivo distribution in mice. The characteristics and stability of the unloaded and drug-loaded nanoemulsions were investigated. The size, apparent viscosity and pH value of NOB-NE were respectively （ 15.5 ±2.9） nm, （3. 10 ±0.33 ） mPa·s and 6. 56±0.05, which were all higher than those of unloaded nanoemulsions. The zeta potential of unloaded and drug-loaded nanoemulsions carried negative charge. The NOB-NE after diluted by 5% glucose solution was stable in 8 h, and there was no significant difference in the size, content and diluted stability of its preconcentrate in long-term storage. The concentration of nobiletin in plasma and tissues was determined by HPLC after intravenous administration of NOB-NE. Based on AUC0-1, MRT and C the nanoemulsions delivered more nobiletin into the brain and kidney compared to those of nobiletin solution. The brain and kidney targeting efficiency was improved. In addition, the results fitting using SAAM II software show that the higher drug concentration of the NOB-NE in the brain might be owed to the quicker transport rate from the blood to the brain, and that in the kidney relate to the probable accumulation effect. These results indicate that the in vivo distribution of NOB-NE with consistent quality in mice could be changed and its brain and kidney targeting absorption capability was enhanced comparing with nobiletin solution.