Preparation of cabazitaxel albumin nanoparticles and evaluation of its biocompatibility in vitro
-
摘要: 目的 制备卡巴他赛白蛋白纳米粒（CBZ-BSA-Gd-NP）以降低药物毒性，并评价其体外生物相容性。 方法 采用生物矿化法制备CBZ-BSA-Gd-NP，对其处方工艺进行优化，对粒径、Zeta电位、载药量等性质进行表征，并采用体外溶血试验考察其体外血液相容性。 结果 制得的纳米粒包封率为63.04%，载药量为10.51%，平均粒径为（166.1±4.7） nm，粒径的多分散系数（PDI）为0.256，Zeta电位为（-18.14±1.16） mV，与卡巴他赛-吐温溶液相比，体外溶血作用显著降低。 结论 该方法操作简便，制备的CBZ-BSA-Gd-NP载药量高，粒径均匀，体外血液相容性好，增加了药物使用的安全性。Abstract: Objective To prepare cabazitaxel albumin nanoparticles(CBZ-BSA-Gd-NP) to reduce drug toxicity,and to evaluate its biocompatibility in vitro. Methods CBZ-BSA-Gd-NP was prepared by biomineralization method.The formulation process was optimized,and the properties such as particle size,Zeta potential and drug loading were characterized.The in vitro hemolysis characteristics were investigated. Results The encapsulation rate of the prepared nanoparticles was 63.04%,the drug loading was about 10.51%.The particle size was (166.1±4.7) nm with the PDI 0.256.The Zeta potential was (-18.14±1.16)mV.The hemolysis effect of CBZ-BSA-Gd-NP in vitro was significantly lower than that of cabazitaxel-Tween solution. Conclusion The preparation method of CBZ-BSA-Gd-NP in this study is simple,with high drug loading,uniform particle size and good blood compatibility in vitro,which will increase the safety for clinical use of the drug.
-
Key words:
- cabazitaxel /
- albumin nanoparticles /
- biocompatibility /
- prostate cancer
-
[1] SIEGEL R L,MILLER K D,JEMAL A.Cancer statistics,2015[J].CA:Cancer J Clin,2015,65(1):5-29. [2] 董隽.激素难治性前列腺癌对多西他赛耐药机制的研究进展[J].中华泌尿外科杂志,2011,32(2):138-140. [3] 马琪,李永红,杨斌,等.前列腺癌化疗安全共识[J].现代泌尿外科杂志,2018,23(2):85-92. [4] 周爱萍,房虹,李长岭,等.去势抗拒前列腺癌治疗新药卡巴他赛[J].中国新药杂志,2013,22(19):2229-2231. [5] LEE K C,MATURO C,RODRIGUEZ R,et al.Nanomedicine-nanoemulsion formulation improves safety and efficacy of the anti-cancer drug paclitaxel according to preclinical assessment[J].J Nanosci Nanotechnol,2011,11(8):6642-6656. [6] 杨恩慈,李苌清,林长征,等.改善紫杉醇水溶性方法的研究进展[J].中南药学,2011,9(8):615-618. [7] 连建豪,陈建明.纳米给药系统在难溶性药物制剂研究中的应用[J].中国新药与临床杂志,2012,31(8):441-446. [8] 王梦迪,何广卫.靶向递药系统白蛋白纳米粒的研究进展[J].安徽医药,2013,17(10):1649-1651. [9] 黄娜,高慧敏,陈两绵,等.金银花与山银花的体外溶血作用分析[J].中国实验方剂学杂志,2017,23(12):6-12. [10] 黄炜忠,蔡泽府,张清民.紫外分光光度法测定注射剂溶血的方法研究[J].今日药学,2016,26(10):713-716. [11] 郝斌,马志方.去势抵抗性前列腺癌化疗及其新进展[J].临床泌尿外科杂志,2015,30(1):83-87. -
点击查看大图
计量
- 文章访问数: 3359
- HTML全文浏览量: 439
- PDF下载量: 417
- 被引次数: 0
下载:
