Sebe István, Szabó Péter, Kállai-Szabó Barnabás, Zelkó Romána
University Pharmacy Department of Pharmacy Administration, Semmelweis University, Hőgyes Endre Str. 7-9, H-1092 Budapest, Hungary.
University Pharmacy Department of Pharmacy Administration, Semmelweis University, Hőgyes Endre Str. 7-9, H-1092 Budapest, Hungary; Gedeon Richter Plc., Formulation R&D, Gyömrői Str. 19-21, H-1103 Budapest, Hungary.
Int J Pharm. 2015 Oct 15;494(1):516-30. doi: 10.1016/j.ijpharm.2015.08.054. Epub 2015 Aug 22.
Over the past several decades, the formulation of novel nanofiber-based drug delivery systems focusing on specific delivery purposes has been investigated worldwide with a continuous level of interest. The unique structure and properties of nanoscale fibrous systems, such as their high specific-area-to-volume ratio and high porosity and the possibility of controlling their crystalline-amorphous phase transitions, make them a desirable formulation pathway to satisfy the needs of recent pharmaceutical development. Fibrous delivery systems can facilitate the accelerated dissolution and increased solubility of small molecules and can also be useful in controlling drug delivery over time (for local or systemic drug administration). In the latter case, the release periods can be tuned over a wide range (from hours to weeks), e.g., by adjusting the fiber diameter and selecting the appropriate polymers. The solubility of the polymer, the fiber diameter and the fiber structure are the primary parameters affecting drug release. In addition to immediate and sustained release, other release profiles, such as biphasic release, can also be achieved. Chemical conjugation and surface functionalization offer further possibilities for the control of drug release. In the case of small molecules, developments focus mostly on overcoming the unfavorable physicochemical nature of the active agents. By contrast, in the preparation of macromolecule-loaded nanofibers, maximizing the biological activity of the macromolecules presents the greatest challenge. The authors' intent is to provide a comprehensive overview of the key parameters of advanced drug delivery systems of this type.
在过去几十年里，全球范围内都在研究针对特定给药目的的新型纳米纤维基药物递送系统，人们对此的兴趣持续不减。纳米级纤维系统的独特结构和性质，如高比表面积与体积比、高孔隙率以及控制其晶态 - 非晶态相变的可能性，使其成为满足近期药物研发需求的理想制剂途径。纤维递送系统可促进小分子的加速溶解和溶解度增加，也有助于控制药物随时间的释放（用于局部或全身给药）。在后一种情况下，释放期可在很宽的范围内调节（从数小时到数周），例如，通过调整纤维直径和选择合适的聚合物来实现。聚合物的溶解度、纤维直径和纤维结构是影响药物释放的主要参数。除了速释和缓释外，还可实现其他释放模式，如双相释放。化学偶联和表面功能化提供了进一步控制药物释放的可能性。对于小分子，研发主要集中在克服活性剂不利的物理化学性质。相比之下，在制备负载大分子的纳米纤维时，最大化大分子的生物活性是最大的挑战。作者的目的是全面概述这类先进药物递送系统的关键参数。
