Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Health Sciences, Istanbul, Turkey.
Department of Pharmaceutical Technology, Faculty of Pharmacy, Ege University, İzmir Turkey.
Drug Dev Res. 2020 Sep;81(6):716-727. doi: 10.1002/ddr.21677. Epub 2020 May 2.
Ocular allergy is one of the most common disorders of the eye surface. The conventional eye drops lack of therapeutic efficacy due to low ocular bioavailability and decreased drug residence time on eye surface. Hence, the present research work aimed to formulate, optimize, and evaluate the in situ gel for ophthalmic drug delivery. The prepared in situ gel formulations were evaluated for clarity, pH, gelling capacity, viscosity, osmolality, in vitro release study, and kinetic evaluation. ex vivo corneal permeation/penetration study using goat and in vivo studies on rabbits were also performed. Fourier-transformed infrared spectroscopy was also applied to study possible interactions between drug and polymers. The formulations found to be stable, nonirritant, and showed sustained release of the drug for a period of up to 24 hr with no ocular damage. The developed in situ gels loaded with tetrahydrozoline are alternative and promising ocular candidates for the treatment of allergic conjunctivitis.
眼表过敏是最常见的眼部疾病之一。由于眼部生物利用度低和药物在眼表面停留时间减少，常规眼药水缺乏治疗效果。因此，本研究旨在为眼部药物输送设计、优化和评估原位凝胶。对制备的原位凝胶制剂进行澄清度、pH 值、胶凝能力、粘度、渗透压、体外释放研究和动力学评价。还进行了使用山羊的离体角膜渗透/穿透研究和在兔子体内的研究。傅里叶变换红外光谱也用于研究药物和聚合物之间可能的相互作用。研究发现，这些制剂稳定、无刺激性，并能持续释放药物长达 24 小时，且对眼部没有损伤。用四氢唑啉负载的开发的原位凝胶是治疗过敏性结膜炎的替代和有前途的眼部候选药物。
