Mirzaeei Shahla, Berenjian Kaveh, Khazaei Rasol
Pharmaceutical Sciences Research Center, School of Pharmacy, Kermanshah University of Medical Sciences, Kermanshah, Iran.
Nano Drug Delivery Research Center, School of Pharmacy, Kermanshah University of Medical Sciences, Kermanshah, Iran.
Adv Pharm Bull. 2018 Mar;8(1):21-27. doi: 10.15171/apb.2018.003. Epub 2018 Mar 18.
The poor bioavailability of drugs in the ocular delivery systems is an important issue and development of delivery systems with prolonged release profile could be in a major importance. This study aims to develop an ocular delivery system using electrospun nanofibers to be a candidate insert for delivery of triamcinolone acetonide. For this purpose, three different chitosan-based formulations were prepared by electrospinning method, and electrospun nanofibers were compared to a formulation comprising hydrophobic polymers (Eudragit S100 and Zein). The electrospun nanofibers were characterized by SEM and FTIR analyses. The release profile and release kinetic models of all the formulations were also examined. The SEM photographs of electrospun nanofibers revealed that among the four designed formulations, formulation obtained by electrospinning of chitosan and PVP possessed the best quality and the minimum size (120 ±30 nm) , which resulted the most uniform and bead-free nanofibers. This formulation also possessed the prolonged release profile of triamcinolone acetonide and was the only electrospun nanofiber following the zero-order kinetic profile. Due to the small diameter and uniformity of this formulation, the prolonged and well controlled release profile, it could be taken into account as a candidate to overcome the drawbacks of the commonly used ocular delivery systems and be used as ocular insert. This study confirmed the ability of electrospun nanofibers to be used as ocular inserts for delivery of ophthalmic drugs.
眼部给药系统中药物的生物利用度低是一个重要问题，开发具有长效释放特性的给药系统可能至关重要。本研究旨在开发一种使用电纺纳米纤维的眼部给药系统，作为醋酸曲安奈德给药的候选插入物。为此，通过电纺丝法制备了三种不同的壳聚糖基制剂，并将电纺纳米纤维与一种包含疏水聚合物（Eudragit S100和玉米醇溶蛋白）的制剂进行了比较。通过扫描电子显微镜（SEM）和傅里叶变换红外光谱（FTIR）分析对电纺纳米纤维进行了表征。还研究了所有制剂的释放曲线和释放动力学模型。电纺纳米纤维的SEM照片显示，在四种设计的制剂中，通过壳聚糖和聚乙烯吡咯烷酮（PVP）电纺得到的制剂质量最佳且尺寸最小（120±30nm），形成的纳米纤维最均匀且无珠粒。该制剂还具有醋酸曲安奈德的长效释放特性，是唯一符合零级动力学曲线的电纺纳米纤维。由于该制剂直径小、均匀性好、释放曲线长效且可控，可被视为克服常用眼部给药系统缺点并用作眼部插入物的候选者。本研究证实了电纺纳米纤维用作眼部插入物以递送眼科药物的能力。
