姜黄素口服纳米乳的制备及其在原位结直肠癌中的应用  

Preparation of Curcumin Oral Nanoemulsion and Its Application in Orthotopic Colorectal Cancer

作　　者：李婧伊 王杰 王瑞[1] LI Jingyi;WANG Jie;WANG Rui(School of Pharmacy,Shanghai University of Traditional Chinese Medicine,Shanghai 201203)

机构地区：[1]上海中医药大学中药学院,上海201203

出　　处：《中国医药工业杂志》2023年第4期554-561,576,共9页Chinese Journal of Pharmaceuticals

摘　　要：采用纳米乳化技术改善难溶性中药姜黄素(1)的溶解性及口服吸收行为,实现原位结直肠癌的高效治疗。使用高能剪切法制备了1纳米乳,粒径为(98.79±1.08)nm,透射电镜观测结果显示其呈圆球状。经体外模拟消化后,仍有(71.03±2.93)%的1溶于水相中。进一步的离体肠吸收试验和药动学试验结果显示,纳米乳可促进1的肠道吸收,主要吸收部位为十二指肠,且呈现吸收快、消除慢的药代动力学特征,口服相对生物利用度为313.50%。在原位结直肠癌裸鼠模型中,1纳米乳口服后可有效抑制结直肠癌的肿瘤生长,剥离所得的肿瘤组织质量约为磷酸盐缓冲液处理组的23.91%,说明1纳米乳在原位结直肠癌方面具有良好的治疗前景。Nanoemulsification technology was applied to improve the solubility and oral absorption behaviors of the insoluble Chinese medicine curcumin(1),achieving an efficient therapeutic effect for colorectal cancer.The nanoemulsion loaded with 1 was prepared through high-shear emulsification.The observation of transmission electron microscopy showed that the 1 nanoemulsion was spherical,and its particle size was(98.79±1.08)nm.After in vitro simulated digestion,(71.03±2.93)%of 1 was still dissolved in the aqueous phase.Moreover,intestinal absorption and pharmacokinetic experiments in vivo revealed that the nanoemulsion could promote the intestinal absorption of 1,especially in the duodenum segment.The 1-loaded nanoemulsion also exhibited the pharmacokinetic characteristics of fast absorption and slow elimination,and the relative oral bioavailability of 1 was improved to 313.50%.In the orthotopic nude mouse models of colorectal cancer,1 nanoemulsion could effectively inhibit the tumor growth after oral administration.The weight of harvested tumor tissue in the 1 nanoemulsion treatment group was about 23.91%of that in the phosphate buffer treatment group,indicating that 1 nanoemulsion had an excellent therapeutic prospect in treating orthotopic colorectal cancer.

关 键 词：姜黄素 纳米乳 口服吸收 生物利用度 结直肠癌 

分 类 号：R979.1[医药卫生—药品]