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10-羟基喜树碱(HCPT)是一种广谱抗癌药,然而由于其溶解性差、不稳定,限制了它的应用.本研究采用微沉淀法联合高压均质法制备羟基喜树碱纳米混悬剂(HCPT-NSP),也称为纳米晶体,显著提高了HCPT的载药量,药物包载率为(36.5士9.5)％,药物浓度达到(1.35士0.2) mg/mL,高于HCPT溶解度的1000倍以上.用动态光散射法(DLS)测定HCPT-NSP粒径为(129.8士13.9) nm.透射电镜(TEM)观察HCPT-NSP呈短杆状晶体.X射线粉末衍射(XRD)和差示扫描量热法(DSC)、热重分析(TGA)、微分热重分析(DTA)结果显示,HCPT在混悬剂中呈短杆状晶体状态.HCPT-NSP以10 mg/kg剂量静注后在体内分布符合三房室模型,与文献中HCPT注射液静脉给药后的药物动力学数据相比,HCPT-NSP的半衰期延长,预示HCPT-NSP是一种很有前景的给药体系.“,”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.