Ethoxy acetalated dextran nanoparticles for drug delivery: A comparative study of formulation methods

IF 5.2 2区 医学 Q1 PHARMACOLOGY & PHARMACY International Journal of Pharmaceutics: X Pub Date : 2023-02-24 DOI:10.1016/j.ijpx.2023.100173
Mira Behnke , Paul Klemm , Philipp Dahlke , Blerina Shkodra , Baerbel Beringer-Siemers , Justyna Anna Czaplewska , Steffi Stumpf , Paul M. Jordan , Stephanie Schubert , Stephanie Hoeppener , Antje Vollrath , Oliver Werz , Ulrich S. Schubert
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引用次数: 4

Abstract

Dextran-based polymers, such as ethoxy acetalated dextran (Ace-DEX), are increasingly becoming the focus of research as they offer great potential for the development of polymer-based nanoparticles as drug delivery vehicles. Their major advantages are the facile synthesis, straightforward particle preparation and the pH-dependent degradation of the particles that can be fine-tuned by the degree of acetalation of the polymer. In this study we have shown that Ace-DEX can not only compete against the commonly used and FDA-approved polymer poly(lactic-co-glycolic acid) (PLGA), but even has the potential to outperform it in its encapsulation properties, e.g., for the herein used anti-inflammatory leukotriene biosynthesis inhibitor BRP-187. We used three different methods (microfluidics, batch nanoprecipitation and emulsion solvent evaporation) for the preparation of BRP-187-loaded Ace-DEX nanoparticles to investigate the influence of the formulation technique on the physicochemical properties of the particles. Finally, we evaluated which production method offers the greatest potential for achieving the demands for a successful translation from research into pharmaceutical production by fulfilling the basic requirements, such as reaching a high loading capacity of the particles and excellent reproducibility while being simple and affordable.

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给药用醋酸乙氧基葡聚糖纳米颗粒:配方方法的比较研究
基于葡聚糖的聚合物,如乙氧基乙酰化葡聚糖(Ace-DEX),越来越成为研究的焦点,因为它们为开发基于聚合物的纳米颗粒作为药物递送载体提供了巨大的潜力。它们的主要优点是易于合成、直接制备颗粒以及颗粒的pH依赖性降解,这些降解可以通过聚合物的缩醛化程度进行微调。在这项研究中,我们已经表明Ace-DEX不仅可以与常用的和美国食品药品监督管理局批准的聚合物聚乳酸-乙醇酸(PLGA)竞争,而且甚至有可能在其包封性能方面优于它,例如,对于本文使用的抗炎白三烯生物合成抑制剂BRP-187。我们使用三种不同的方法(微流体、分批纳米沉淀和乳液溶剂蒸发)制备BRP-187负载的Ace-DEX纳米颗粒,以研究配方技术对颗粒物理化学性质的影响。最后,我们评估了哪种生产方法最有潜力通过满足基本要求来实现从研究成功转化为药物生产的需求,例如达到颗粒的高负载能力和优异的再现性,同时简单且价格合理。
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来源期刊
International Journal of Pharmaceutics: X
International Journal of Pharmaceutics: X Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science
CiteScore
6.60
自引率
0.00%
发文量
32
审稿时长
24 days
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