School of Materials Science and Engineering, University of Shanghai for Science and Technology, Shanghai, People's Republic of China.
Int J Nanomedicine. 2011;6:3271-80. doi: 10.2147/IJN.S27468. Epub 2011 Dec 13.
The objective of this investigation was to develop a new type of solid dispersion in the form of core-sheath nanofibers using coaxial electrospinning for poorly water-soluble drugs. Different functional ingredients can be placed in various parts of core-sheath nanofibers to improve synergistically the dissolution and permeation properties of encapsulated drugs and to enable drugs to exert their actions.
Using acyclovir as a model drug, polyvinylpyrrolidone as the hydrophilic filament-forming polymer matrix, sodium dodecyl sulfate as a transmembrane enhancer, and sucralose as a sweetener, core-sheath nanofibers were successfully prepared, with the sheath part consisting of polyvinylpyrrolidone, sodium dodecyl sulfate, and sucralose, and the core part composed of polyvinylpyrrolidone and acyclovir.
The core-sheath nanofibers had an average diameter of 410 ± 94 nm with a uniform structure and smooth surface. Differential scanning calorimetry and x-ray diffraction results demonstrated that acyclovir, sodium dodecyl sulfate, and sucralose were well distributed in the polyvinylpyrrolidone matrix in an amorphous state due to favoring of second-order interactions. In vitro dissolution and permeation studies showed that the core-sheath nanofiber solid dispersions could rapidly release acyclovir within one minute, with an over six-fold increased permeation rate across the sublingual mucosa compared with that of crude acyclovir particles.
The study reported here provides an example of the systematic design, preparation, characterization, and application of a novel type of solid dispersion consisting of multiple components and structural characteristics.
本研究旨在通过同轴静电纺丝技术制备一种新型的核壳结构纳米纤维固体分散体，用于改善难溶性药物的溶解和渗透性能。不同的功能成分可以放置在核壳纳米纤维的不同部位，协同提高包封药物的溶解和渗透性能，并使药物发挥作用。
以阿昔洛韦为模型药物，聚乙烯吡咯烷酮为亲水性纤维形成聚合物基质，十二烷基硫酸钠为跨膜增强剂，三氯蔗糖为甜味剂，成功制备了核壳结构纳米纤维，其中壳层部分由聚乙烯吡咯烷酮、十二烷基硫酸钠和三氯蔗糖组成，芯层部分由聚乙烯吡咯烷酮和阿昔洛韦组成。
核壳纳米纤维的平均直径为 410±94nm，具有均匀的结构和光滑的表面。差示扫描量热法和 X 射线衍射结果表明，由于二级相互作用的有利影响，阿昔洛韦、十二烷基硫酸钠和三氯蔗糖在聚乙烯吡咯烷酮基质中以无定形状态均匀分布。体外溶解和渗透研究表明，核壳纳米纤维固体分散体在一分钟内可迅速释放阿昔洛韦，与粗阿昔洛韦颗粒相比，透过舌下黏膜的渗透速率提高了六倍以上。
本研究为多组分、结构特征的新型固体分散体的系统设计、制备、表征和应用提供了一个范例。
