Acyclovir is an effective antiviral drug which suffers from limited water solubility and low bioavailability. However, it is possible to eliminate these limitations by forming inclusion complexes with cyclodextrins. In this study, we have reported the electrospinning of polymer-free and free-standing acyclovir/cyclodextrin nanofibers for the first time. This is a promising approach for developing a fast-dissolving delivery system of an antiviral drug molecule. Here, hydroxypropyl-beta-cyclodextrin (HP-βCD) was used as both complexation agent and electrospinning matrix. The acyclovir/HP-βCD system was prepared by incorporating ~ 7 % (w/w) of acyclovir into the highly concentrated aqueous solution of HP-βCD (180 %, w/v). The control sample of acyclovir/polyvinylpyrrolidone (PVP) nanofiber were also generated using ethanol/water (3/1, v/v) solvent system and the same initial acyclovir (7 %, w/w) content. Due to the inclusion complexation, acyclovir/HP-βCD nanofibers provided better encapsulation and so loading efficiency. The loading efficiency of acyclovir/HP-βCD nanofibers was determined as ~ 98 %, while it was ~ 66 % for acyclovir/PVP nanofibers. It was found that acyclovir/HP-βCD nanofibers contained some crystalline form of acyclovir. Even so, it showed faster dissolving/release and faster disintegration profiles compared to acyclovir/PVP nanofibers which had higher amount of crystalline acyclovir. The inclusion complexation property and high water solubility of HP-βCD (> 2000 mg/mL) ensured the fast-dissolving property of acyclovir/HP-βCD nanofibers. Briefly, acyclovir/HP-βCD nanofibers are quite promising alternative to the polymeric based system for the purpose of fast-dissolving oral drug delivery. The enhanced physicochemical properties of drug molecules and the use of water during whole process can make drug/cyclodextrin nanofibers a favorable dosage formulation for the desired treatments.

阿昔洛韦是一种有效的抗病毒药物，其水溶性有限且生物利用度较低。但是，可以通过与环糊精形成包合物来消除这些限制。在这项研究中，我们首次报道了无聚合物和独立的无环鸟苷/环糊精纳米纤维的静电纺丝。这是开发抗病毒药物分子的快速溶解递送系统的有前途的方法。在这里，羟丙基-β-环糊精（HP-βCD）既用作络合剂又用作电纺丝基质。通过将约7％（w / w）的阿昔洛韦掺入高浓度的HP-βCD水溶液（180％，w / v）中，制备无环鸟苷/HP-βCD系统。阿昔洛韦/聚乙烯吡咯烷酮（PVP）纳米纤维的对照样品也使用乙醇/水（3/1，v / v）溶剂系统和相同的初始阿昔洛韦（7％，w / w）含量。由于包合物的络合，无环鸟苷/HP-βCD纳米纤维提供了更好的封装效果，从而提高了装载效率。无环鸟苷/HP-βCD纳米纤维的负载效率确定为〜98％，而无环鸟苷/ PVP纳米纤维的负载效率为〜66％。发现无环鸟苷/HP-βCD纳米纤维含有一些无环鸟苷的结晶形式。即便如此，与具有较高结晶阿昔洛韦含量的阿昔洛韦/ PVP纳米纤维相比，它仍显示出更快的溶解/释放和更快的崩解特性。HP-βCD的包裹体络合性能和高水溶性（> 2000 mg / mL）确保了阿昔洛韦/HP-βCD纳米纤维的快速溶解性能。简而言之，为了快速溶解口服药物的递送，无环鸟苷/HP-βCD纳米纤维是聚合物系统的非常有前途的替代品。药物分子增强的理化性质和在整个过程中使用水可使药物/环糊精纳米纤维成为用于所需治疗的有利剂型。