达卡巴嗪长循环脂质体的制备及体内抗肿瘤效应
DOI:
作者:
作者单位:

作者简介:

通讯作者:

基金项目:

四川省科技计划重点研发项目(2017SZ0134)


Preparation of long circulating liposomal dacarbazine and preliminary study on its antitumor effect in vivo
Author:
Affiliation:

Fund Project:

  • 摘要
  • |
  • 图/表
  • |
  • 访问统计
  • |
  • 参考文献
  • |
  • 相似文献
  • |
  • 引证文献
  • |
  • 资源附件
    摘要:

    【摘要】 目的 探讨达卡巴嗪长循环脂质体(PEGylated dacarbazine liposome,PEG-DTIC-LP)的制备及体内抗肿瘤效应。 方法 采用硫酸铵梯度法制备PEG-DTIC-LP,考察其包封率、载药量、形态、粒径、Zeta电位、稳定性、体外释药性等性质。建立荷黑色素瘤小鼠模型,将小鼠分为生理盐水组、空白脂质体组、DTIC溶液组、PEG-DTIC-LP组4组,每组6只,雌雄各半。于第1、3、5、7、9天按10 mg/kg给药剂量给生理盐水组小鼠尾静脉注射生理盐水,空白脂质体组尾静脉注射空白脂质体混悬液,DTIC溶液组尾静脉注射1mg/mL DTIC溶液,PEG-DTIC-LP组尾静脉注射1 mg/mL PEG-DTIC-LP混悬液。以肿瘤体积、小鼠体重、中位生存时间为评价指标,研究PEG-DTIC-LP的抗肿瘤效应。 结果 制备的PEG-DTIC-LP为半透明乳白色有蓝色乳光的液体;包封率为(60.41±2.47)%,载药量为(5.95±0.24)%;平均粒径为190nm,Zeta电位为-53.8mV;放置7天后PEG-DTIC-LP包封率无显著变化(P>0.05),放置14天后包封率下降明显(P<0.05);PEG-DTIC-LP组荷瘤小鼠的肿瘤体积显著小于DTIC组与生理盐水组(P<0.05),但与空白脂质体组比较差异无统计学意义(P>0.05);中位生存时间PEG-DTIC-LP组>空白脂质体组>生理盐水组>DTIC溶液组(P<0.05);PEG-DTIC-LP组体重低于其余三组(P<0.05)。 结论 将达卡巴嗪制备成长循环脂质体有利于提高其抗肿瘤效应。

    Abstract:

    【Abstract】 Objective To prepare PEGylated long circulating dacarbazine liposome(PEG-DTIC-LP),and preliminarily study its antitumor effect in vivo. Methods The liposomes were prepared using the ammonium sulfate gradient method, and its entrapment efficiency, drug loading, morphology under electron microscope, particle size, zeta potential, stability and drug release behavior in vitro were investigated. Establish melanoma bearing mouse models. The antitumor effect of PEG-DTIC-LP was studied using mouse tumor volume, body weight and median survival time as the indicators, and DTIC solution, saline and blank liposomes were used as the control groups. Results PEG-DTIC-LP was a translucent milky white suspension with blue opalescence. The encapsulation efficiency was 60.41±2.47% and the drug loading was 5.95±0.24%. The average particle size was 190 nm, and the zeta potential was -53.8 mV. Compared with three control groups, the tumor volume of mice in PEG-DTIC-LP group was significantly smaller, and the median survival time was longer. Conclusion Long circulating liposome encapsulation is beneficial to improve the antitumor effect of DTIC.

    参考文献
    相似文献
    引证文献
引用本文
分享
文章指标
  • 点击次数:
  • 下载次数:
历史
  • 收稿日期:
  • 最后修改日期:
  • 录用日期:
  • 在线发布日期: 2021-09-30
您是第位访问者
网站版权所有:《西部医学》编辑部     蜀ICP备18038379号-4
地址:四川省成都市武侯区小天竺街75号财富国际18F-1号    邮政编码:610041
电话:028-85570072/85588403 本网站支持 IPv6    E-mail:xbyxqk@163.com
技术支持:北京勤云科技发展有限公司