a College of Mechanical and Electrical Engineering, Beijing University of Chemical Technology , Beijing , China.
b Beijing Key Laboratory of Advanced Functional Polymer Composites , College of Materials Science and Engineering, Beijing University of Chemical Technology , Beijing , China.
J Biomater Sci Polym Ed. 2019 Mar;30(4):308-321. doi: 10.1080/09205063.2019.1570432. Epub 2019 Feb 9.
How to improve the bioavailability of the Sanguis Draconis (SD) is an important problem in the potential clinical applications. The aim of this study was to develop a drug delivery system to achieve high bioavailability of SD, a drug with poor water solubility. It will promote the research about new formulations of the SD and the other insoluble drugs. In this study, a highly biocompatible hydrophilic polymer, polyvinylpyrrolidone (PVP), was selected as a carrier, mixed with different proportions of SD to produce SD-PVP microfibers by solution electrospinning. By orthogonal experiments, the optimal spinning conditions of the preparation of SD-PVP fibers were investigated. The morphology of different proportions of SD-PVP microfibers was observed by scanning electron microscopy, and the phase characteristics were characterized by Fourier transform infrared spectrometry, X-ray diffraction, and differential scanning calorimetry. The hydrophilic properties of SD-PVP fiber membranes with different SD content were analyzed by the water contact angle assay. In vitro dissolution experiments were carried out to observe the dissolution of drugs in SD-PVP fiber membranes. The results showed that the diameter of SD-PVP fibers increased with the enlargement of SD content. A eutectic mixture was formed after blending PVP and SD, and the hydrogen bonds were formed between the SD and PVP with no chemical reaction occurred. The dispersion of SD in the fiber decreased with the increase of SD content. The higher the content of SD in the fiber, the more hydrophobic the fiber membrane. In vitro dissolution studies revealed that the dissolution content of SD from SD-PVP microfibers was significantly higher than that of the pure or original drug SD. However, as the SD content increased from 15% to 30%, the dissolution of the drug in the SD-PVP fibers decreased. The SD-PVP fiber prepared in this study showed much higher solubility than the original drug in vitro, which has great significance for the development of new dosage forms for the clinical application of SD, and it has a useful reference for the study of similar bioavailability of poorly soluble drugs.
如何提高龙血竭（SD）的生物利用度是其潜在临床应用中的一个重要问题。本研究旨在开发一种药物传递系统，以实现 SD（一种水溶性差的药物）的高生物利用度，从而促进对 SD 及其他难溶性药物新制剂的研究。在这项研究中，选择了一种高度生物相容的亲水性聚合物聚乙烯吡咯烷酮（PVP）作为载体，与不同比例的 SD 混合，通过溶液静电纺丝制备 SD-PVP 微纤维。通过正交实验，考察了制备 SD-PVP 纤维的最佳纺丝条件。通过扫描电子显微镜观察不同比例 SD-PVP 微纤维的形态，通过傅里叶变换红外光谱、X 射线衍射和差示扫描量热法对其相特征进行了表征。通过水接触角测定分析了不同 SD 含量的 SD-PVP 纤维膜的亲水性。进行了体外溶出实验，观察药物在 SD-PVP 纤维膜中的溶出情况。结果表明，随着 SD 含量的增加，SD-PVP 纤维的直径增大。PVP 和 SD 混合后形成共晶混合物，SD 与 PVP 之间形成氢键，没有发生化学反应。随着 SD 含量的增加，SD 在纤维中的分散性降低。纤维中 SD 的含量越高，纤维膜的疏水性越强。体外溶出研究表明，SD-PVP 微纤维中 SD 的溶解含量明显高于纯 SD 或原药 SD。然而，随着 SD-PVP 纤维中 SD 含量从 15%增加到 30%，药物在 SD-PVP 纤维中的溶解量下降。与原药相比，本研究制备的 SD-PVP 纤维在体外具有更高的溶解度，这对 SD 临床应用新剂型的开发具有重要意义，对类似难溶性药物生物利用度的研究也具有有益的参考价值。
