Huang Weidong, Yang Yaoyao, Zhao Biwei, Liang Gangqiang, Liu Shiwei, Liu Xian-Li, Yu Deng-Guang
School of Chemistry and Chemical Engineering, Hubei Polytechnic University, Huangshi 435003, China.
Hubei Key Laboratory of Mine Environmental Pollution Control and Remediation, Hubei Polytechnic University, Huangshi 435003, China.
Pharmaceutics. 2018 Aug 2;10(3):115. doi: 10.3390/pharmaceutics10030115.
Enhancing the dissolution of insoluble active ingredients comprises one of the most important issues in the pharmaceutical and biomaterial fields. Here, a third generation solid dispersion (3rd SD) of ferulic acid was designed and fabricated by a modified coaxial electrospinning process. A traditional second generation SD (2nd SD) was also prepared by common one-fluid blending electrospinning and was used as a control. With poly(vinyl alcohol) as the fiber matrix and polyvinylpyrrolidone K10 as an additive in the 3rd SDs, the two electrospinning processes were investigated. The prepared 2nd and 3rd SDs were subjected to a series of characterizations, including X-ray diffraction (XRD), scanning electron microscope (SEM), hydrophilicity and in vitro drug dissolving experiments. The results demonstrate that both SDs were monolithic nanocomposites and that the drugs were amorphously distributed within the matrix. However, the 3rd SDs had better morphology with smaller size, narrower size distribution, and smaller water contact angles than the 2nd SDs. Dissolution tests verified that the 3rd SDs could release their loaded cargoes within 60 s, which was over three times faster than the 2nd SDs. Therefore, a combined strategy based on the modified coaxial electrospinning and the logical selections of drug carriers is demonstrated for creating advanced biomaterials.
提高难溶性活性成分的溶出度是制药和生物材料领域最重要的问题之一。在此,通过改进的同轴静电纺丝工艺设计并制备了阿魏酸第三代固体分散体(3rd SD)。还通过普通的单流体共混静电纺丝制备了传统的第二代固体分散体(2nd SD)并用作对照。以聚乙烯醇为纤维基质,聚乙烯吡咯烷酮K10为3rd SD中的添加剂,研究了这两种静电纺丝工艺。对制备的2nd和3rd SD进行了一系列表征,包括X射线衍射(XRD)、扫描电子显微镜(SEM)、亲水性和体外药物溶出实验。结果表明,两种固体分散体均为整体纳米复合材料,药物以无定形形式分布在基质中。然而,3rd SD比2nd SD具有更好的形态,尺寸更小、尺寸分布更窄且水接触角更小。溶出试验证实,3rd SD可在60秒内释放其负载的药物,比2nd SD快三倍以上。因此,展示了一种基于改进的同轴静电纺丝和合理选择药物载体的联合策略,用于制备先进的生物材料。