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首页> 外文期刊>Journal of Applied Polymer Science >Irbesartan-loaded electrospun nanofibers-based PVP K90 for the drug dissolution improvement: Fabrication, in vitro performance assessment, and in vivo evaluation
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Irbesartan-loaded electrospun nanofibers-based PVP K90 for the drug dissolution improvement: Fabrication, in vitro performance assessment, and in vivo evaluation

机译：负载厄贝沙坦的静电纺丝纳米纤维基PVP K90用于改善药物溶出度：制备，体外性能评估和体内评估

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摘要

Irbesartan with a low bioavailability is known as a poorly water-soluble drug. The purpose of this investigation is the improvement of physicochemical properties (such as solubility and dissolution rate) of Irbesartan using electrospun nanofibers-based solid dispersion preparation. Nanofibers were prepared using certain weight ratios of the drug and polyvinylpyrrolidone K90 (PVP K90). Then, dissolution studies were carried out. Moreover, selected samples were examined by many different tests such as Fourier transform infra red (FTIR), differential scanning calorimetry (DSC), X-ray diffraction (XRD), high-performance liquid chromatography (HPLC), and scanning electron microscopy (SEM). Though solubility and dissolution rate of all Irbesartan-PVP nanofibers improved, but the best result was obtained through of ENSD5 (3% (w/v) : 7% (w/v)). In sink condition approximately 97% of this sample was released during 60 min. The drug content was among the different batches from 40.55 +/- 1.01 to 245.32 +/- 1.77 g/mL. The maximum saturation solubility was belonged to this sample. According to the results of the thermal analysis and FTIR spectroscopy, there is no chemical reaction between drug and carrier, also samples has not changed during the process. Amorphous structure for nanofibers was confirmed by DSC thermograms and XRD diffractograms and morphological structure of samples were observed by SEM images. Ultimately, in vivo studies were performed in healthy grey rabbits and the results were satisfactory. The drug-polymer nanofibers showed an increase in relative bioavailability than the plain Irbesartan suspension. (c) 2015 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2015, 132, 42212.
机译：生物利用度低的厄贝沙坦是水溶性差的药物。这项研究的目的是使用电纺基于纳米纤维的固体分散体制剂来改善厄贝沙坦的理化性质（例如溶解度和溶解速率）。使用一定重量比的药物和聚乙烯吡咯烷酮K90（PVP K90）制备纳米纤维。然后，进行溶出度研究。此外，通过许多不同的测试对选定的样品进行了检查，例如傅立叶变换红外（FTIR），差示扫描量热法（DSC），X射线衍射（XRD），高效液相色谱（HPLC）和扫描电子显微镜（SEM） ）。尽管所有厄贝沙坦-PVP纳米纤维的溶解度和溶解速率均得到改善，但通过ENSD5可获得最佳结果（3％（w / v）：7％（w / v））。在水槽条件下，60分钟内约有97％的样品被释放。药物含量在40.55 +/- 1.01至245.32 +/- 1.77 g / mL的不同批次中。最大饱和溶解度属于该样品。根据热分析和FTIR光谱的结果，药物与载体之间没有化学反应，样品在此过程中也没有变化。通过DSC热分析图和XRD衍射图确认了纳米纤维的非晶结构，并且通过SEM图像观察了样品的形态结构。最终，在健康的灰兔子中进行了体内研究，结果令人满意。药物聚合物纳米纤维比普通的厄贝沙坦悬浮液显示出相对生物利用度的增加。 （c）2015 Wiley Periodicals，Inc. J. Appl。 Polym。科学2015，132，42212。

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