Akyüz Lalehan, Duman Fatih, Kaya Murat
Aksaray University, Faculty Of Technical Vocational, Department Of Chemistry Technology, Aksaray, Turkey.
Erciyes University, Faculty Of Science, Department Of Biology, Kayseri, Turkey.
Turk J Pharm Sci. 2017 Apr;14(1):34-39. doi: 10.4274/tjps.95867. Epub 2017 Apr 15.
This study aimed to prepare chitosan-flurbiprofen micro-nano spheres as environmentally friendly for drug releasing by spray-drying method without any cross-linking agent. It was also aimed to reveal the favorable binding geometries of chitosan and flurbiprofen using molecular modeling.
In this study, flurbiprofen was encapsulated with chitosan using spray-drying technique. The used chitosan, flurbiprofen and obtained spheres were characterized via fourier transmission infrared spectrometer (FT-IR), thermogravimetric analysis (TGA), X-ray diffractometer and scanning electron microscopy (SEM). Drug entrapment efficiency was carried out for determination of the drug amount in the micro-nano spheres. release studies of CS-FP spheres were also examined in the simulated biological fluid at pH 7.4. Encapsulation process of flurbiprofen was combined with the docking studies to investigate the possible binding sites of the chitosan.
FT-IR results confirmed that H-bonding system was formed between chitosan and drug. CS-FP spheres with spherical shape were observed by SEM. TGA analysis results showed that thermal stabilities of flurbiprofen and chitosan were decreased after the encapsulation process. The spheres were used for releasing studies in simulated biological fluids. All these analysis results clearly showed that encapsulation was successfully carried out with 73.28% efficiency. Molecular modeling studies showed that CS-FP stable complexes was formed through a hydrogen bonding system between OH group of the drug molecule and chitosan hydroxyl (OH) group with a binding energy of -3.90 kcal/mol. Our computational results supported to spectroscopic results obtained by FTIR.
This study proved that micro-nano spheres can be prepared without using cross-linking agent by spray-drying method. The results of the drug releasing studies showed that release of encapsulated flurbiprofen was completed within 48h. The results of docking analysis can be suggested for the design of new drug carrier systems with chitosan.
本研究旨在通过喷雾干燥法制备壳聚糖 - 氟比洛芬微纳米球,用于药物释放,且不使用任何交联剂,使其对环境友好。同时,旨在通过分子建模揭示壳聚糖与氟比洛芬的有利结合几何结构。
在本研究中,采用喷雾干燥技术用壳聚糖包裹氟比洛芬。通过傅里叶透射红外光谱仪(FT - IR)、热重分析(TGA)、X射线衍射仪和扫描电子显微镜(SEM)对所用的壳聚糖、氟比洛芬及得到的微纳米球进行表征。测定药物包封率以确定微纳米球中的药物含量。还在pH 7.4的模拟生物流体中对壳聚糖 - 氟比洛芬微纳米球进行释放研究。将氟比洛芬的包封过程与对接研究相结合,以研究壳聚糖可能的结合位点。
FT - IR结果证实壳聚糖与药物之间形成了氢键体系。通过SEM观察到呈球形的壳聚糖 - 氟比洛芬微纳米球。TGA分析结果表明,包裹过程后氟比洛芬和壳聚糖的热稳定性降低。这些微纳米球用于模拟生物流体中的释放研究。所有这些分析结果清楚地表明包封成功进行,包封率为73.28%。分子建模研究表明,壳聚糖 - 氟比洛芬稳定复合物是通过药物分子的OH基团与壳聚糖羟基(OH)基团之间的氢键体系形成的,结合能为 - 3.90千卡/摩尔。我们的计算结果支持了FTIR获得的光谱结果。
本研究证明通过喷雾干燥法无需使用交联剂即可制备微纳米球。药物释放研究结果表明,包封的氟比洛芬在48小时内释放完毕。对接分析结果可为设计新型壳聚糖药物载体系统提供参考。