Controlled and manageable release of antimalarial Artemisone by encapsulation in biodegradable carriers
Controlled and manageable release of antimalarial Artemisone by encapsulation in biodegradable carriers
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DOI：
10.1016/j.eurpolymj.2020.109625
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发表时间：
2020-04-15
影响因子：
6
通讯作者：
Greiner, Andreas
中科院分区：
文献类型：
--
作者：
Bagheri, Amir Reza;Golenser, Jacob;Greiner, Andreas
纳米纤维垫和膜是有利的平台，可以提供作为药物递送技术中的药物载体的独特机会。在这项研究中，青蒿素（ART）加载聚己内酯（16500）-b-α-羟基-ω-甲氧基聚（乙二醇）（5000）（PCL-MPEG）纳米纤维无纺布（NFN）和薄膜成功地生产和用于进行基础研究的控制和延长释放的ART作为一种不溶性（疏水）抗疟药从加载的配方，其中涵盖了广泛的释放动力学。作为这项工作中提出的关键发现，潜在的广泛释放动力学特别适用于治疗由各种青蒿素敏感寄生虫引起的寄生虫病。一般来说，纳米纤维结构表现出突发药物释放行为，特别是在开始的下沉调节，而膜不。因此，开发的NFN可以被用作潜在的药物递送候选人，以提供立即释放的药物分子具有较差的水溶性，如ART，而电影可以采用作为潜在的有效载体，更延迟释放的ART。释放的动力学可以另外调整浸涂NFN与生物相容性涂层剂。通过增加涂布剂的浓度并因此增加纤维结构的厚度，可以观察到由纤维结构形成膜的趋势。NFN在水环境中表现出更高的吸水能力，在酶促条件下表现出更快的降解。这些结果可以解释为什么ART从NFN比从膜中释放得更快。
Nanofiber mats and films are advantageous platforms that can offer unique opportunities as drug carriers in drug delivery technologies. In this research, Artemisone (ART)-loaded polycaprolactone(16500)-b-alpha-hydroxy-omega-methoxy poly(ethylene glycol)(5000) (PCL-MPEG) nanofibrous nonwovens (NFN), and films were successfully produced and used to carry out fundamental research on the controlled and extended release of ART as an insoluble (hydrophobic) antimalarial from the loaded formulations, which cover a wide range of release kinetics. The potential wide range of release kinetics as a key finding presented in this work is specifically suitable for the treatment of parasitic diseases induced by various artemisinin sensitive parasites. Generally, nanofibrous structures demonstrated a burst drug release behavior, particularly at the beginning of sink-conditioning, whereas films do not. Therefore, the developed NFN can be used as potential drug delivery candidates to provide an immediate release for drug molecules having poor water solubility such as ART, whereas films can be employed as potentially effective carriers for more retarded release of ART.The kinetics of the release could be additionally adjusted by dip-coating of NFN with biocompatible coating agents. A tendency to form films from the fibrous structures could be observed by increasing the concentration of coating agents and thus the thickness of the fibrous structures. NFN showed higher water uptake ability in aqueous environment and faster degradation under enzymatic conditions. These results may explain why ART was released quicker from the NFN than from the films.