Controlling Morphology and Release Behavior of Sorafenib-Loaded Nanocarriers Prepared by Flash Nanoprecipitation,Industrial & Engineering Chemistry Research

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Controlling Morphology and Release Behavior of Sorafenib-Loaded Nanocarriers Prepared by Flash Nanoprecipitation
Industrial & Engineering Chemistry Research ( IF 3.8 ) Pub Date : 2018-08-24 , DOI: 10.1021/acs.iecr.8b02105
Mingwei Wang ₁ , Shan Lin ₁ , Junyou Wang ₁ , Lei Liu ₁ , Wenjuan Zhou ₁ , Rizwan Bhutto Ahmed ₁ , Aiguo Hu ₂ , Xuhong Guo _{1,

3} , Martien A. Cohen Stuart ₁

Affiliation

Flash nanoprecipitation (FNP) is a recent developed method featuring fast processing and simple equipment for preparing drug-carrier NPs. Herein, we prepared stable sorafenib-loaded NPs with biocompatible amphiphilic poly(ethylene glycol)-block-poly(lactide acid) (PEG-b-PLA) as stabilizing polymer based on FNP. The formed NPs show well-controlled size and high drug loading content compared with nanoparticles from traditional antisolvent precipitation. Moreover, drug/polymer mass ratio (D/P) and stream velocity presented as Reynolds number (Re) show strong effects on particles size and internal morphology. Low D/P ratio and Re number provide core–shell nanoparticles with drug nuclei distributed in PLA matrix, which could release the sorafenib completely but keep the polymer aggregates after the drug release. While high D/P ratio and Re number lead to grained nanoparticles with bigger size and low packing density due to the coprecipitation of the PEG blocks in the structure. The drug release of these particles is fast and typically accompanied by the dissociation of the nanoparticles. Our study demonstrates that the particle internal morphology and solute packing density are crucial factors to manipulate the drug release of the FNP nanoparticles, and the developed strategy could be widely adopted to assess drug release of FNP nanoparticles for further therapeutic applications.

中文翻译：

通过快速纳米沉淀制备的索拉非尼负载的纳米载体的形态和释放行为的控制

快速纳米沉淀（FNP）是最近开发的一种方法，具有制备药物载体NP的快速处理和简单设备的特点。在本文中，我们制备了具有两亲性的生物相容的聚（乙二醇）稳定的索拉非尼加载的NP -嵌段-聚（丙交酯酸）（PEG- b -PLA）作为稳定基于FNP聚合物。与来自传统抗溶剂沉淀的纳米粒子相比，形成的纳米粒子显示出可控的大小和较高的药物载量。此外，以雷诺数（Re）表示的药物/聚合物质量比（D / P）和流速度对颗粒尺寸和内部形态具有强烈影响。低D / P比和Re数量提供了在PLA基质中分布有药物核的核-壳纳米颗粒，它可以完全释放索拉非尼，但在药物释放后仍保持聚合物聚集。由于PEG嵌段在结构中的共沉淀，高D / P比和Re数导致颗粒状纳米颗粒具有更大的尺寸和较低的堆积密度。这些颗粒的药物释放是快速的，并且通常伴随着纳米颗粒的解离。我们的研究表明，颗粒的内部形态和溶质堆积密度是控制FNP纳米颗粒药物释放的关键因素，并且该开发的策略可广泛用于评估FNP纳米颗粒的药物释放，以进一步用于治疗应用。

更新日期：2018-08-24

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