Payab Shahriar, Davaran Soodabeh, Tanhaei Ali, Fayyazi Behnam, Jahangiri Azin, Farzaneh Amir, Adibkia Khosro
a Drug Applied Research Center and Faculty of Pharmacy, Tabriz University of Medical Sciences , Tabriz , Iran.
b Student Research Committee and Faculty of Pharmacy, Tabriz University of Medical Sciences , Tabriz , Iran.
Artif Cells Nanomed Biotechnol. 2016;44(1):362-9. doi: 10.3109/21691401.2014.953250. Epub 2014 Sep 2.
The aim of the present research was to fabricate triamcinolone acetonide (TA)-Eudragit(®) RS100 nanostructures using the electrospraying method.
The physicochemical properties of the electrosprayed formulations as well as drug release patterns were assessed. The particle size and morphology were evaluated using scanning electron microscopy. X-ray crystallography and differential scanning calorimetry were also conducted to investigate the crystallinity and polymorphic alterations of the drug in the formulations. Probable chemical interactions between the drug and the carrier during the preparation process were analyzed using FT-IR spectroscopy. The drug release kinetic was also considered to predict the release mechanism.
Increasing the concentration of injected polymer solution resulted in the formation of more fibers and fewer beads, with the particle diameter ranging from 60 nm to a few micrometers based on the drug: polymer ratio. The drug crystallinity was notably decreased during the electrospraying process; however, no interaction between drug and polymer was detected. The electrosprayed formulations with 1:10 drug: polymer ratio showed an almost similar drug release rate compared to the pure drug, while those with 1:5 ratio revealed slower release profiles. The release data were best fitted to the Weibull model, so that the corresponding shape factor values of the Weibull model were less than 0.75, indicating the diffusion controlled release mechanism.
Our findings revealed that TA loaded Eudragit(®) RS100 nanofibers and nanobeads were properly prepared by the electrospraying method, which is a simple, surfactant-free and cost effective technique for producing drug: polymer nanostructures.
本研究旨在采用电喷雾法制备曲安奈德(TA)-Eudragit® RS100纳米结构。
评估了电喷雾制剂的物理化学性质以及药物释放模式。使用扫描电子显微镜评估粒径和形态。还进行了X射线晶体学和差示扫描量热法研究制剂中药物的结晶度和多晶型变化。使用傅里叶变换红外光谱分析制备过程中药物与载体之间可能的化学相互作用。还考虑了药物释放动力学以预测释放机制。
增加注入聚合物溶液的浓度会导致形成更多的纤维和更少的珠子,根据药物与聚合物的比例,粒径范围为60纳米至几微米。在电喷雾过程中药物结晶度显著降低;然而,未检测到药物与聚合物之间的相互作用。药物与聚合物比例为1:10的电喷雾制剂与纯药物相比显示出几乎相似的药物释放速率,而比例为1:5的制剂显示出较慢的释放曲线。释放数据最适合威布尔模型,因此威布尔模型的相应形状因子值小于0.75,表明为扩散控制释放机制。
我们的研究结果表明,通过电喷雾法可以成功制备负载TA的Eudragit® RS100纳米纤维和纳米珠,这是一种用于制备药物-聚合物纳米结构的简单、无表面活性剂且具有成本效益的技术。