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纳米脂质体对诊断超声能量水平的抗癌药物的增强释放。

Enhanced release of anticancer agents from nanoliposomes in response to diagnostic ultrasound energy levels.

机构信息

Department of Speech and Hearing Sciences, University of Illinois at Urbana-Champaign, Champaign, IL 61820, USA.

出版信息

Pharm Dev Technol. 2012 May-Jun;17(3):383-8. doi: 10.3109/10837450.2010.546407. Epub 2011 Jan 11.

Abstract

The efficacy of diagnostic ultrasound is explored for the release of anticancer agents loaded inside liposomes. Diagnostic ultrasound energy levels employed in the study were at a frequency of 7.5 MHz and the highest power intensity which is a function of the pulse repetition time. Design of Experiments was used to formulate the Ultrasound sensitive nanoliposome (USNL) by varying the lipid ratios and the intensity settings of ultrasound energy. Doxorubicin was loaded into the USNL and the release was compared to conventional Doxil liposomes. The USNLs released increasing amounts of drug in response to increasing irradiation times while the drug release was not significant when the Non-USNLs (Doxil liposomes) were exposed to ultrasound energy levels. In vitro studies to test the cytotoxicity of the formulations showed that the USNLs significantly inhibited cell survival of SCC9, squamous oral cancer cells, as compared to the Non-USNLs. We hypothesize that the drug is released due to increased membrane permeability during exposure to ultrasound energy levels, where the lipid composition and energy levels play a key role in determining the efficacy of diagnostic ultrasound energy as a tool for drug delivery.

摘要

研究了诊断超声在释放载于脂质体内部的抗癌剂方面的效果。研究中使用的诊断超声能水平频率为 7.5MHz,最大功率强度是脉冲重复时间的函数。通过改变脂质比率和超声能量的强度设置,使用实验设计来制备超声敏感纳米脂质体(USNL)。将阿霉素载入 USNL,并将其释放与常规多柔比星脂质体进行比较。USNL 在响应增加的辐照时间时释放出越来越多的药物,而当非 USNL(多柔比星脂质体)暴露于超声能水平时,药物释放则不显著。体外研究测试制剂的细胞毒性表明,与非 USNL 相比,USNL 显著抑制了 SCC9、鳞状口腔癌细胞的存活。我们假设药物是由于在暴露于超声能水平期间膜通透性增加而释放的,其中脂质组成和能水平在确定诊断超声能作为药物递送工具的效果方面起着关键作用。

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