Budesonide Loaded PLGA Nanoparticles for Targeting the Inflamed Intestinal Mucosa-Pharmaceutical Characterization and Fluorescence Imaging
Budesonide Loaded PLGA Nanoparticles for Targeting the Inflamed Intestinal Mucosa-Pharmaceutical Characterization and Fluorescence Imaging
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DOI：
10.1007/s11095-015-1852-6
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发表时间：
2016-05-01
影响因子：
3.7
通讯作者：
Lehr, Claus-Michael
中科院分区：
文献类型：
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作者：
Ali, Hussain;Weigmann, Benno;Lehr, Claus-Michael
本研究采用油/水（O/W）乳化蒸发法制备布地奈德PLGA纳米粒，评价其治疗炎症性肠病（IBD）的特异性靶向疗效。纳米颗粒的大小，形状和体外药物释放曲线进行了表征。通过差示扫描量热法（DSC）和X射线粉末衍射（XPRD）进行固态表征。为了评估纳米颗粒的靶向效率，在体内确定了健康和发炎结肠中的颗粒定位研究。这些数据由冷冻切片补充，纳米颗粒的尺寸为200 +/-05nm，具有光滑的球形形状。包封率约为85 +/-3.5%，这是通过直接和间接方法发现的。布地奈德从纳米粒中的释放显示出双相释放曲线，具有初始突释，然后持续释放。XPRD数据显示，聚合物基质中的药物以结晶状态存在。通过体内成像系统评估纳米颗粒在炎症组织中的积聚，发现与健康组相比，颗粒在炎症部位大量积聚，该研究表明，负载布地奈德的PLGA纳米颗粒是一种有效的靶向药物递送系统，可将药物递送至炎症肠粘膜。
The purpose of this study was to evaluate the specifically targeted efficiency of budesonide loaded PLGA nanoparticles for the treatment of inflammatory bowel disease (IBD).The nanoparticles were prepared by an oil/water (O/W) emulsion evaporation technique. The nanoparticles were characterized for their size, shape and in vitro drug release profile. Solid state characterization was carried out by differential scanning calorimetry (DSC) and X-ray Power diffraction (XPRD). In order to evaluate the targeted efficiency of nanoparticles, a particle localization study in the healthy and in the inflamed colon was determined in vivo. These data were complemented by cryo-sections.Nanoparticles were 200 +/- 05 nm in size with a smooth and spherical shape. The encapsulation efficiency was around 85 +/- 3.5%, which was find-out by both, direct and indirect methods. Release of budesonide from the nanoparticles showed a biphasic release profile with an initial burst followed by sustained release. XPRD data revealed that the drug in the polymer matrix existed in crystalline state. Nanoparticles accumulation in inflamed tissues was evaluated by in-vivo imaging system and it was found that particles are accumulated in abundance at the site of inflammation when compared to the healthy group.The study demonstrates that the budesonide loaded PLGA nanoparticles are an efficient delivery system for targeted drug delivery to the inflamed intestinal mucosa.