Department of Fiber and Polymer Technology, School of Engineering Sciences in Chemistry, Biotechnology, and Health, Royal Institute of Technology, Teknikringen 56-58, Stockholm, SE-100 44, Sweden.
Department of Materials and Environmental Chemistry, Stockholm University, Svante Arrhenius väg 16C, Stockholm, 10691, Sweden.
Drug Deliv Transl Res. 2024 Dec;14(12):3452-3466. doi: 10.1007/s13346-024-01573-2. Epub 2024 Mar 26.
Polyelectrolyte complexes (PECs) are polymeric structures formed by the self-assembly of oppositely charged polymers. Novel biomaterials based on PECs are currently under investigation as drug delivery systems, among other applications. This strategy leverages the ability of PECs to entrap drugs under mild conditions and control their release. In this study, we combined a novel and sustainably produced hemicellulose-rich lignosulphonate polymer (EH, negatively charged) with polyethyleneimine (PEI) or chitosan (CH, positively charged) and agar for the development of drug-releasing PECs. A preliminary screening demonstrated the effect of several parameters (polyelectrolyte ratio, temperature, and type of polycation) on PECs formation. From this, selected formulations were further characterized in terms of thermal properties, surface morphology at the microscale, stability, and ability to load and release methylene blue (MB) as a model drug. EH/PEI complexes had a more pronounced gel-like behaviour compared to the EH/CH complexes. Differential scanning calorimetry (DSC) results supported the establishment of polymeric interactions during complexation. Overall, PECs' stability was positively affected by low pH, ratios close to 1:1, and the addition of agar. PECs with higher EH content showed a higher MB loading, likely promoted by stronger electrostatic interactions. The EH/CH formulation enriched with agar showed the best sustained release profile of MB during the first 30 h in a pH-dependent environment simulating the gastrointestinal tract. Overall, we defined the conditions to formulate novel PECs based on a sustainable hemicellulose-rich lignosulphonate for potential applications in drug delivery, which promotes the valuable synergy between sustainability and the biomedical field.
聚电解质复合物（PECs）是通过带相反电荷的聚合物自组装形成的聚合物结构。基于 PEC 的新型生物材料目前正在作为药物输送系统等应用进行研究。该策略利用 PEC 在温和条件下包埋药物并控制其释放的能力。在这项研究中，我们将一种新型且可持续生产的富含半纤维素的木质素磺酸盐聚合物（EH，带负电荷）与聚乙烯亚胺（PEI）或壳聚糖（CH，带正电荷）和琼脂结合，开发了释放药物的 PEC。初步筛选表明了几种参数（聚电解质比、温度和聚阳离子类型）对 PEC 形成的影响。在此基础上，对选定的配方从热性能、微观表面形貌、稳定性以及负载和释放亚甲蓝（MB）作为模型药物的能力等方面进行了进一步的表征。与 EH/CH 复合物相比，EH/PEI 复合物具有更明显的凝胶状行为。差示扫描量热法（DSC）结果支持在复合物形成过程中建立聚合物相互作用。总体而言，PEC 的稳定性受到低 pH 值、接近 1:1 的比例以及琼脂添加的积极影响。EH 含量较高的 PEC 表现出更高的 MB 负载量，这可能是由于更强的静电相互作用所致。在模拟胃肠道的 pH 依赖性环境中，在最初的 30 小时内，富含琼脂的 EH/CH 制剂显示出 MB 最佳的持续释放特性。总体而言，我们确定了基于可持续富含半纤维素的木质素磺酸盐的新型 PEC 的配方条件，为药物输送中的潜在应用提供了条件，促进了可持续性和生物医学领域之间的宝贵协同作用。
