Institute of Pharmaceutical Technology and Buchmann Institute for Molecular Life Sciences, Goethe University, Frankfurt am Main, Germany; Helmholtz-Institute for Pharmaceutical Research Saarland (HIPS), Department of Drug Delivery (DDEL), Saarland University, Saarbruecken, Germany.
Institute of Pharmaceutical Technology and Buchmann Institute for Molecular Life Sciences, Goethe University, Frankfurt am Main, Germany; Helmholtz-Institute for Pharmaceutical Research Saarland (HIPS), Department of Drug Delivery (DDEL), Saarland University, Saarbruecken, Germany.
Int J Pharm. 2019 Feb 10;556:363-371. doi: 10.1016/j.ijpharm.2018.12.026. Epub 2018 Dec 18.
Controlled release of hydrophilic drugs from carriers is still faced with problems due to the poor compatibility of such substances with slowly degradable polymers leading to challenges regarding fabrication as well as undesired burst release of the encapsulated drugs. In this context, coaxial electrospinning being capable of simultaneously using two different solvent systems provides a promising strategy. However, the coaxial electrospinning process is extremely complex and numerous parameters might impact the incorporation as well as release kinetics of the drugs. To address this gap, we fabricated coaxial fibers for controlled co-delivery of two different drugs: bovine serum albumin as a model protein and acyclovir as a small molecule. Controlled release of both embedded drugs was achieved, and drug release profiles could be modulated through modifying spinning techniques as well as compositions and process parameters of the core fluid. Especially, the interactions of the co-incorporated drugs were found to be of key significance for affecting drug distribution within the fibers, and thus ultimately impacting drug release kinetics. Based on our findings, key factors for influencing drug encapsulation and release kinetics from coaxial fibers could be identified, providing a valuable guidance for rational development of coaxial fiber-based drug carriers.
亲水药物从载体中的控制释放仍然面临问题,因为这些物质与缓慢降解的聚合物的兼容性差,导致在制造方面以及封装药物的不希望的突释方面存在挑战。在这种情况下,能够同时使用两种不同溶剂系统的同轴静电纺丝提供了一种有前途的策略。然而,同轴静电纺丝过程非常复杂,许多参数可能会影响药物的掺入和释放动力学。为了解决这一差距,我们制造了用于两种不同药物的共递送的同轴纤维:牛血清白蛋白作为模型蛋白和阿昔洛韦作为小分子。实现了两种嵌入式药物的控制释放,并且可以通过改变纺丝技术以及芯液的组成和工艺参数来调节药物释放曲线。特别是,共掺入药物的相互作用对于影响纤维内药物分布从而最终影响药物释放动力学具有关键意义。基于我们的发现,可以确定影响同轴纤维中药物包封和释放动力学的关键因素,为基于同轴纤维的药物载体的合理开发提供了有价值的指导。