文献类型：期刊文章

作　　者：张毅[1,2] 詹颖[1,2] 庞宁[1,2] 刘瑜洁[1,2] 程士轩[1,2] 李骥[1,2] 杜祎甜[1,2] 齐宪荣[1,2]

机构地区：[1]北京大学医学部药学院药剂学系,北京100191 [2]北京大学医学部分子药剂学与新释药系统北京市重点实验室,北京100191

出　　处：《Journal of Chinese Pharmaceutical Sciences》

基　　金：NSFC(Grant No.81473156,81673365);Fangzheng Foundation for funding of the work

年　　份：2017

卷　　号：26

期　　号：8

起止页码：574-581

语　　种：中文

收录情况：CAB、CAS、CSCD、CSCD2017_2018、DOAJ、EMBASE、IC、JST、SCOPUS、ZGKJHX、普通刊

摘　　要：10-Hydroxycamptothecin （HCPT） is a broad-spectrum anticancer drug, while its low solubility and instability severely limit its application. In this study, HCPT nanosuspension （HCPT-NSP）, also known as nanocrystal, was prepared by micro-precipitation combined with high-pressure homogenization method. This nanosuspension was characterized by size, shape, zeta potential, drug loading efficiency and in vitro drug release behavior. Preferred formulation and process showed that particle size was （129.8±13.9） nm, PDI was 0.20±0.07, and drug loading efficiency was 36.5%±9.5%. Moreover, HCPT nanocrystal concentration reached （1.35±0.2） mg/mL in HCPT-NSP, which was more than 1000-fold higher than that of HCPT. Transmission electron microscopy （TEM） results showed that the nanosuspension was short rod in shape. X-ray powder diffraction （XRD）, thermogravimetric analysis （TGA）, derivative thermogravimetric analysis （DTA） and differential scanning calorimetry （DSC） further elaborated the crystal state of the HCPT. The drug concentration-time curve of HCPT-NSP in rats was in accordance with the three-compartment model, showing prolonged half-life. Taken together, our data suggested that HCPT-NSP was a promising drug delivery system.

关 键 词：10-HYDROXYCAMPTOTHECIN NANOSUSPENSION Nanocrystal  High-pressure homogenization  PHARMACOKINETICS

分 类 号：R943] R965[药学类]