Incorporation of 10-hydroxycamptothecin nanocrystals into zein microspheres
Incorporation of 10-hydroxycamptothecin nanocrystals into zein microspheres
复制标题
将 10-羟基喜树碱纳米晶体掺入玉米醇溶蛋白微球中
DOI：
10.1016/j.ces.2016.08.029
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发表时间：
2016-11-22
影响因子：
4.7
通讯作者：
Jiang, Yanbin
中科院分区：
文献类型：
--
作者：
Liu, Guijin;Li, Shaomin;Jiang, Yanbin
以玉米醇溶蛋白为载体，羟基喜树碱（HCPT）为模型药物，将药物喜树碱（DNC）掺入到颗粒载体中，制备DNC给药系统。首次分别采用超临界抗溶剂法（SAS）和内置式超声透析法（BUDP）制备了羟基喜树碱NC-玉米醇溶蛋白微球（HCPT NC-Zein MS），但所得产物的微观结构并不理想。将SAS工艺与BUDP工艺相结合，将SAS工艺制备的HCPT与玉米醇溶蛋白共沉淀物分散于乙醇-水溶液中作为BUDP的透析液，得到了理想的HCPT NC-Zein MS。采用总体期望函数（DF）对各处方进行定量评价，并根据DF极差分析结果，优化HCPT NC-玉米醇溶蛋白MS。在优化条件下，制备出平均粒径为1.10 ± 0.12 μ m、载药量为5.98%、包封率为95.68%的HCPT NC-玉米醇溶蛋白MS。SEM、FT-IR、XRD和DSC等表征表明，HCPT NC成功地嵌入到玉米醇溶蛋白微球内部。详细讨论了HCPT NC-玉米醇溶蛋白质谱的形成机理和工艺参数的影响。HCPT NC-玉米醇溶蛋白MS成功地维持了HCPT的释放速率，在最初的20 h内，HCPT快速释放约50%，随后的释放趋势遵循零级动力学，在82 h内达到70%。(C)2016爱思唯尔有限公司版权所有。
Incorporation of drug nanocrystal (DNC) into a particulate carrier to form the DNC delivery system was conducted in this study, where 10-hydroxycamptothecin (HCPT) was selected as the model drug and zein was the carrier. The supercritical anti-solvent (SAS) process or the built-in ultrasonic dialysis process (BUDP) was applied to prepare HCPT NC-loaded zein microspheres (HCPT NC-Zein MS) at first respectively, but the results showed that the products obtained were unsatisfactory in their particle microstructures. Fortunately, by combining the SAS process with BUDP, i.e. the co-precipitation of HCPT and zein prepared using the SAS process was dispersed into ethanol-water as the dialysis solution for BUDP, the results showed that desirable HCPT NC-Zein MS were obtained. The formulations were evaluated quantitatively by an overall desirability function (DF), and the optimized HCPT NC- Zein MS was prepared according to the range analysis results of DF. Under the optimized conditions, HCPT NC-Zein MS with a mean particle size = 1.10 +/- 0.12 mu m, drug loading=5.98% and encapsulation efficiency=95.68% were obtained. The further characterizations of SEM, FT-IR, XRD and DSC demonstrated that HCPT NC was successfully incorporated into the interior of zein microspheres. The effects of the process parameters and the formation mechanism of HCPT NC-Zein MS were discussed in detail. Furthermore, it is presented that HCPT NC-Zein MS sustained HCPT release rate successfully, where about 50% HCPT was fast released in the first 20 h, then the release trend followed zero order kinetics and reached 70% in 82 h. (C) 2016 Elsevier Ltd. All rights reserved.