Shang Qing, Huang Sijin, Zhang Aixin, Feng Jia, Yang Song
a Chemical and Pharmaceutical Engineering Institute , Hebei University of Science and Technology , Hebei , China.
J Biomater Sci Polym Ed. 2017 Nov;28(16):1874-1887. doi: 10.1080/09205063.2017.1354677. Epub 2017 Jul 19.
To improve the bioavailability of ibuprofen (IBU), we developed a novel binary complex of poly(PEGMA-co-MAA) hydrogel and IBU-loaded PLGA nanoparticles (IBU-PLGA NPs@hydrogels) as an oral intestinal targeting drug delivery system (OIDDS). The IBU-loaded PLGA NPs and pH-sensitive hydrogels were obtained via the solvent evaporation method and radical polymerization, respectively. The final OIDDS was obtained by immersing the hydrogel chips in the IBU-loaded PLGA NPs solutions (pH 7.4) for 3 d. The size distribution and morphology of cargo-free NPs were studied by laser granularity analyzer and transmission electron microscope (TEM). The inner structures of the pH-sensitive hydrogel chips were observed with an S-4800 scanning electron microscope (SEM). The distribution states of IBU in the OIDDS were also studied with X-ray diffraction (XRD) and differential scanning calorimetry (DSC). TEM photographs illustrated that the PLGA NPs had a round shape with an average diameter about 100 nm. Fourier transform infrared spectrum (FTIR) confirmed the synthesis of poly(PEGMA-co-MAA) hydrogel. The SEM picture showed that the final hydrogel had 3D net-work structures. Moreover, the poly(PEGMA-co-MAA) hydrogel showed an excellent pH-sensitivity. The XRD and DSC curves suggested that IBU distributed in the OIDDS with an amorphous state. The cumulated release profiles indicated that the final OIDDS could release IBU in alkaline environment (e.g. intestinal tract) at a sustained manner. Therefore, the novel OIDDS could improve the oral bioavailability of IBU, and had a potential application in drug delivery.
为提高布洛芬（IBU）的生物利用度，我们开发了一种新型的聚（聚乙二醇甲基丙烯酸酯 - 共 - 甲基丙烯酸）水凝胶与载有IBU的聚乳酸 - 羟基乙酸共聚物纳米粒（IBU - PLGA NPs@水凝胶）的二元复合物，作为口服肠道靶向给药系统（OIDDS）。载有IBU的PLGA纳米粒和pH敏感水凝胶分别通过溶剂蒸发法和自由基聚合反应制备。最终的OIDDS是通过将水凝胶芯片浸泡在载有IBU的PLGA NPs溶液（pH 7.4）中3天获得的。通过激光粒度分析仪和透射电子显微镜（TEM）研究了无载药纳米粒的尺寸分布和形态。用S - 4800扫描电子显微镜（SEM）观察了pH敏感水凝胶芯片的内部结构。还通过X射线衍射（XRD）和差示扫描量热法（DSC）研究了IBU在OIDDS中的分布状态。TEM照片表明PLGA纳米粒呈圆形，平均直径约为100 nm。傅里叶变换红外光谱（FTIR）证实了聚（聚乙二醇甲基丙烯酸酯 - 共 - 甲基丙烯酸）水凝胶的合成。SEM图片显示最终的水凝胶具有三维网络结构。此外，聚（聚乙二醇甲基丙烯酸酯 - 共 - 甲基丙烯酸）水凝胶表现出优异的pH敏感性。XRD和DSC曲线表明IBU以无定形状态分布在OIDDS中。累积释放曲线表明最终的OIDDS能够在碱性环境（如肠道）中持续释放IBU。因此，这种新型的OIDDS可以提高IBU的口服生物利用度，并在药物递送方面具有潜在应用。
