• 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>RSC Advances >Atorvastatin calcium loaded PCL nanoparticles: development, optimization, in vitro and in vivo assessments
【24h】

Atorvastatin calcium loaded PCL nanoparticles: development, optimization, in vitro and in vivo assessments

机译：阿托伐他汀钙载PCL纳米粒子：开发，优化，体外和体内评估

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

The aim of the present study was to prepare atorvastatin calcium (ATR) loaded poly(epsilon-caprolactone) nanoparticles (ALPNs) to enhance the oral bioavailability, efficacy and safety profile of drug. ALPNs were prepared by a nanoprecipitation technique while formulation and process parameters were optimized using a central composite factorial design. The optimized ALPNs were investigated through in vitro (solid state characterization, morphological, drug release study and stability study) analysis and in vivo (pharmacokinetic, efficacy and safety study) behaviour in rats. The optimized ALPNs having 197 +/- 5 nm particle size, 0.213 +/- 0.012 polydispersity index and 75.6 +/- 3.2% entrapment efficiency, did not exhibit any physicochemical interaction of the drug with the carrier. The X-ray diffraction, differential scanning calorimetry and electron diffraction pattern has substantiated the amorphous character of ATR encapsulated in nanoparticles. The smooth and homogeneous spherical shape of the nanoparticles was evidenced in morphological analyses. The in vitro drug release profile of ALPNs showed a 96 h sustained release and the pharmacokinetic profile in rats exhibited significant enhancement in bioavailability, (C)max and mean resident time of the drug. ALPNs exhibited similar efficacy (plasma lipid profile and glucose level) and markedly improved biochemical safety profiles (creatinine, blood urea nitrogen, creatinine kinase, lactate dehydrogenase and aspartate amino transferase) of rat plasma at a 50% reduced dose compared to orally administered ATR.
机译：本研究的目的是阿托伐他汀钙（ATR）加载的聚（ε-己内酯）的纳米颗粒（ALPNs）准备以增强药物的口服生物利用度，效能和安全性。通过纳米沉淀技术制备ALPN，同时使用中央综合因子设计优化配方和工艺参数。通过体外（固态表征，形态学，药物释放研究和稳定性研究）分析和大鼠体内（药代动力学，疗效和安全性研究）进行了优化的ALPN。具有197 +/- 5nm粒径的优化AlPN，0.213 +/- 0.012多分散指数和75.6 +/- 3.2％的夹带效率，没有表现出药物与载体的任何物理化学相互作用。 X射线衍射，差示扫描量热法和电子衍射图案证实了封装在纳米颗粒中的ATR的无定形特征。在形态学分析中证明了纳米颗粒的光滑和均匀的球形形状。 ALPN的体外药物释放曲线显示出96小时的持续释放，大鼠的药代动力学谱表现出显着提高生物利用度，（C）药物的最大和平均居民时间。 ALPNS表现出类似的功效（血浆脂质曲线和葡萄糖水平），并明显改善了大鼠等离子体的生物化学安全谱（肌酐，血尿尿素，肌酐激酶，乳酸脱氢酶和天冬氨酸氨基转移酶），与口服给药的剂量减少50％。

著录项

  • 来源
    《RSC Advances》 |2016年第20期|共13页
  • 作者

    Kumar Nagendra; Chaurasia Sundeep; Patel Ravi R.; Khan Gayasuddin; Kumar Vikas; Mishra Brahmeshwar;

  • 作者单位

    Banaras Hindu Univ Indian Inst Technol Dept Pharmaceut Varanasi 221005 Uttar Pradesh India;

    Banaras Hindu Univ Indian Inst Technol Dept Pharmaceut Varanasi 221005 Uttar Pradesh India;

    Banaras Hindu Univ Indian Inst Technol Dept Pharmaceut Varanasi 221005 Uttar Pradesh India;

    Banaras Hindu Univ Indian Inst Technol Dept Pharmaceut Varanasi 221005 Uttar Pradesh India;

    Banaras Hindu Univ Indian Inst Technol Dept Pharmaceut Varanasi 221005 Uttar Pradesh India;

    Banaras Hindu Univ Indian Inst Technol Dept Pharmaceut Varanasi 221005 Uttar Pradesh India;

  • 收录信息
  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类 化学;
  • 关键词

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