Taghe Shiva, Mirzaeei Shahla, Ahmadi Arian
Pharmaceutical Sciences Research Center, Rahesh Daru Novine, Kermanshah 6715847141, Iran.
Student Research Committee, Kermanshah University of Medical Sciences, Kermanshah 6715847141, Iran.
Life (Basel). 2023 Mar 30;13(4):913. doi: 10.3390/life13040913.
Conventional anti-infective eye drops are the most common forms of drugs prescribed for the management of topical ocular infections. Despite their convenience, topical eye drops face multiple challenges, including limited bioavailability and repetitive administration. The present study aimed to prepare, evaluate, and compare film-structured and nanofibrous ocular inserts using biocompatible polymers of polyvinyl alcohol (PVA) and polycaprolactone (PCL) to achieve sustained ciprofloxacin Hydrochloride (CIP) delivery. The nanofibrous formulations were prepared by electrospinning and glutaraldehyde crosslinking while the film formulation was prepared by solvent casting. Nanofibrous inserts had mean diameters in the range 330-450 nm. Both film and nanofibrous inserts were strong, although the nanofibers had higher flexibility. In vitro antibacterial efficacy against and was observed for all formulations and cell viability of more than 70% confirmed their non-toxicity. In vitro release studies showed prolonged release of 2 days for the film and 5 days for the nanofibers compared with a 10-h release of CIP from the eye drop. Pharmacokinetic studies of rabbits' eyes showed 4.5-5-folds higher AUC for the nanofiber formulations compared with the eye drop. Thus, prolonged-release film-structured and nanofibrous inserts are suitable carriers for ocular delivery of CIP.
传统抗感染眼药水是治疗局部眼部感染最常用的药物剂型。尽管其使用方便,但局部眼药水面临诸多挑战,包括生物利用度有限和需重复给药。本研究旨在制备、评估和比较使用聚乙烯醇(PVA)和聚己内酯(PCL)等生物相容性聚合物的膜结构和纳米纤维眼部插入物,以实现盐酸环丙沙星(CIP)的持续递送。纳米纤维制剂通过静电纺丝和戊二醛交联制备,而膜制剂通过溶剂浇铸制备。纳米纤维插入物的平均直径在330 - 450纳米范围内。膜和纳米纤维插入物都很坚固,尽管纳米纤维具有更高的柔韧性。所有制剂均观察到对[具体菌种]的体外抗菌效果,且细胞活力超过70%证实其无毒性。体外释放研究表明,与眼药水10小时的释放时间相比,膜制剂的释放时间延长至2天,纳米纤维制剂的释放时间延长至5天。兔眼的药代动力学研究表明,与眼药水相比,纳米纤维制剂的AUC高4.5 - 5倍。因此,长效膜结构和纳米纤维插入物是眼部递送CIP的合适载体。