...
  • 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>Journal of pharmaceutical sciences. >Single and double emulsion manufacturing techniques of an amphiphilic drug in PLGA nanoparticles: formulations of mithramycin and bioactivity.
【24h】

Single and double emulsion manufacturing techniques of an amphiphilic drug in PLGA nanoparticles: formulations of mithramycin and bioactivity.

机译：PLGA纳米颗粒中两亲药物的单和双乳剂制造技术：光神霉素的配方和生物活性。

获取原文
获取原文并翻译 | 示例
           
页面导航
  • 摘要
  • 著录项
  • 相似文献
  • 相关主题

摘要

Formulation of hydrophilic compounds in nanoparticles is problematic due to their escape to the external aqueous phase. The certain amphiphilic nature of mithramycin, utilized clinically in cancer, makes its incorporation into nanoparticles an interesting challenge, elucidating the formulation factors of amphiphilics in nanoparticles. We hypothesized that mithramycin nanoparticles could provide more effective therapy of restenosis due to its antiproliferating and potential monocyte inhibition properties. The nanoprecipitation technique (designed for lipophilic compounds) was found preferable, with better encapsulation efficiency, than the emulsification solvent diffusion (ESD) technique (79.3 +/- 3.1% and 40.8 +/- 1.1%, respectively). The double emulsion solvent diffusion (DESD) method, designed for hydrophilic compounds, yielded similar encapsulation efficiency (80%). Nanoparticles size was, 110 +/- 36, 130 +/- 30, and 160 +/- 31 nm, ESD, nanoprecipitation, and DESD techniques, respectively. Mithramycin solution and in nanoparticles significantly inhibited RAW264 macrophages and smooth muscle cells in a dose-dependent relationship, and reduced the number of circulating monocytes in rabbits. However, no inhibition of restenosis was obtained in the rat carotid model following i.v. administration of mithramycin nanoparticles. It can be concluded that PLGA-based polymeric nanoparticles of mithramycin can be formulated by techniques suitable for lipophilic/hydrophilic compounds. The ineffectiveness in the rat restenosis model is probably due to the short depletion period of circulating monocytes and lack of arterial targeting.
机译：由于纳米颗粒中的亲水性化合物逃逸到外部水相中，因此其配制存在问题。临床上用于癌症的光神霉素的某些两亲性质使得将其结合到纳米颗粒中成为一个有趣的挑战，阐明了纳米颗粒中两亲物的组成因素。我们假设，光神霉素纳米粒由于其抗增殖和潜在的单核细胞抑制特性，可以提供更有效的再狭窄治疗。发现纳米沉淀技术（专为亲脂性化合物设计）比乳化溶剂扩散（ESD）技术（分别为79.3 +/- 3.1％和40.8 +/- 1.1％）具有更好的封装效率。专为亲水性化合物设计的双乳液溶剂扩散（DESD）方法产生了相似的封装效率（80％）。纳米颗粒尺寸分别是ESD，纳米沉淀和DESD技术，分别为110 +/- 36、130 +/- 30和160 +/- 31 nm。丝裂霉素溶液和纳米颗粒中的剂量显着抑制RAW264巨噬细胞和平滑肌细胞，并减少了兔中循环单核细胞的数量。然而，在静脉内注射后，在大鼠颈动脉模型中没有获得对再狭窄的抑制作用。纳米霉素的给药。可以得出结论，可以通过适用于亲脂性/亲水性化合物的技术来配制光神霉素的基于PLGA的聚合纳米颗粒。大鼠再狭窄模型的无效性可能是由于循环单核细胞的耗竭期短和缺乏动脉靶向性所致。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱：kefu@zhangqiaokeyan.com

京公网安备：11010802029741号 ICP备案号：京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有

  • 客服微信

  • 服务号