Witt Sandra, Scheper Thomas, Walter Johanna-Gabriela
Institut für Technische Chemie Hannover Leibniz Universität Hannover Hannover Germany.
Eng Life Sci. 2019 Aug 12;19(10):658-665. doi: 10.1002/elsc.201800214. eCollection 2019 Oct.
Cancer is a worldwide increasing burden and its therapy is often challenging and causes severe side effects in healthy tissue. If drugs are loaded into nanoparticles, side effects can be reduced, and efficiency can be increased via the enhanced permeability and retention effect. This effect is based on the fact that nanoparticles with sizes from 10 to 200 nm can accumulate in tumor tissue due to their leaky vasculature. In this work, we produced polycaprolactone (PCL) in the sizes 1.8, 5.4, and 13.6 kDa and were able to produce spherical shaped nanoparticles with mean diameters of 64 ± 19 nm out of the PCL and 45 ± 8 nm out of the PCL reproducibly. By encapsulation of paclitaxel the diameter of that nanoparticles did not increase, and we were able to encapsulate 73 ± 7 fmol paclitaxel per 1000 particles in the PCL-nanoparticles and 35 ± 8 fmol PTX per 1000 PCL-nanoparticles. Furthermore, we coupled the aptamer S15 to preformed PCL-nanoparticles resulting in particles with a hydrodynamic diameter of 153 nm. This offers the opportunity to use these nanoparticles for targeted drug delivery.
癌症是一种在全球范围内负担日益加重的疾病，其治疗往往具有挑战性，且会对健康组织造成严重副作用。如果将药物负载到纳米颗粒中，通过增强的渗透和滞留效应，可以减少副作用并提高疗效。这种效应基于这样一个事实，即尺寸在10至200纳米之间的纳米颗粒由于肿瘤组织血管渗漏而能够在其中积聚。在这项工作中，我们制备了分子量为1.8、5.4和13.6千道尔顿的聚己内酯（PCL），并且能够分别从PCL中可重复地制备出平均直径为64±19纳米和45±8纳米的球形纳米颗粒。通过包裹紫杉醇，纳米颗粒的直径并未增加，并且我们能够在PCL纳米颗粒中每1000个颗粒包裹73±7飞摩尔紫杉醇，在PCL纳米颗粒中每1000个颗粒包裹35±8飞摩尔紫杉醇。此外，我们将适配体S15偶联到预先形成的PCL纳米颗粒上，得到了流体动力学直径为153纳米的颗粒。这为将这些纳米颗粒用于靶向药物递送提供了机会。
