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研究载药胶束的声致释放阿霉素。

Investigating the acoustic release of doxorubicin from targeted micelles.

机构信息

Chemical Engineering Department, American University of Sharjah, United Arab Emirates.

出版信息

Colloids Surf B Biointerfaces. 2013 Jan 1;101:153-5. doi: 10.1016/j.colsurfb.2012.05.025. Epub 2012 Jun 7.

Abstract

The main problem associated with the administration of anti-cancer medication is that the drug is delivered throughout the body causing undesirable side effects. Therefore, it is important to synthesize drug carriers capable of minimizing the adverse side effects of chemotherapy by preferentially targeting tumor cells both actively (e.g. a folate receptor) and using external stimulus (e.g. ultrasound). In this paper, we report the synthesis of Pluronic P105 micelles with a folate targeting moiety (with a yield of 48%) containing doxorubicin (Dox). We applied low frequency ultrasound as an external stimulus and measured the amount of release of Dox from these folated micelles. The results showed that the percent drug release increases as the power intensity of ultrasound increases. The maximum amount of release (14%) was measured at 5.4 W/cm(2). A power density threshold at approximately 0.55 W/cm(2) exists below which no statistically significant release was observed. This lower threshold suggests that cavitation plays an important role in triggering drug release from targeted micelles.

摘要

与抗癌药物给药相关的主要问题是药物在全身传递会导致不良的副作用。因此,合成能够通过主动靶向肿瘤细胞(例如叶酸受体)并利用外部刺激(例如超声)最小化化疗的不良副作用的药物载体非常重要。在本文中,我们报告了具有叶酸靶向部分(产率为 48%)的 Pluronic P105 胶束的合成,其中包含阿霉素(Dox)。我们应用低频超声作为外部刺激,并测量了这些叶酸胶束中 Dox 的释放量。结果表明,随着超声功率强度的增加,药物释放的百分比增加。在 5.4 W/cm(2) 时测量到最大释放量(14%)。存在一个功率密度阈值约为 0.55 W/cm(2),低于该阈值观察到没有统计学意义的释放。这个较低的阈值表明空化在触发靶向胶束释放药物方面起着重要作用。

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