Abou-Taleb Basant A, Abdelwahab Ibrahim A
Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, Pharos University in Alexandria, Canal El Mahmoudia Street, Beside, Green Plaza Complex, Alexandria, 21648, Egypt.
Department of Pharmaceutics and Pharmacy Practices, Alexandria University Hospitals, Alexandria University, Alexandria, Egypt.
Sci Rep. 2025 Jun 3;15(1):19430. doi: 10.1038/s41598-025-03418-5.
Acanthamoeba keratitis is the most dangerous ocular-infection that can cause blindness. The propamidine-isethionate (PI) 0.1% eye-drops are used in the treatment, but they have low-bioavailability due to precorneal loss parameters. In-situ-gels are administered as drops into the eye and changed into gel in the cul-de-sac, which may be able to solve these issues. In this study, we demonstrate different nano-ocular delivery-systems formulations of 0.1%PI loaded in-situ-gels using the ideas of pH & temperature-stimulated in-situ-gelation. Pluronic F-127 a thermosensitive-polymer with chitosan as a pH-sensitive polymer that also enhances permeability was utilized as a gelling-agent. Several in-vitro pharmaceutical and antiprotozoal assessments on Acanthamoeba keratitis were assessed for the developed formulations. It was observed that the created PI-chitosan nanoparticles in-situ-gel formulation showed smaller particle-size, higher zeta with a higher %inhibition of amoebae after 24-h incubation compared to other formulations with continuous drug release for 24-h. The PI-CSNPs in-situ-gel formulation offers an effective substitute for traditional BROLENE eye-drops in the management of Acanthamebae, around double the effect based on % amebae inhibition, reached 92%. It can reach the clinical-stage & is appropriate for sustained-ocular-administration for the treatment of Acanthamoeba keratitis.
棘阿米巴角膜炎是最危险的眼部感染疾病,可导致失明。0.1%的依西酸丙脒(PI)滴眼液用于治疗,但由于角膜前损失参数,其生物利用度较低。原位凝胶以滴剂形式滴入眼内,并在结膜囊中转变为凝胶,这可能能够解决这些问题。在本研究中,我们利用pH值和温度刺激原位凝胶化的理念,展示了不同的载有0.1%PI的纳米眼部给药系统原位凝胶制剂。使用具有壳聚糖作为pH敏感聚合物(其还可增强通透性)的热敏聚合物普朗尼克F-127作为胶凝剂。对所开发的制剂进行了几项关于棘阿米巴角膜炎的体外药物和抗原生动物评估。观察到,与其他具有24小时持续药物释放的制剂相比,所制备的PI-壳聚糖纳米颗粒原位凝胶制剂在孵育24小时后显示出更小的粒径、更高的zeta电位以及更高的对变形虫的抑制百分比。PI-CSNPs原位凝胶制剂在棘阿米巴的管理方面为传统的BROLENE滴眼液提供了一种有效的替代品,基于变形虫抑制百分比,其效果约为传统滴眼液的两倍,达到了92%。它可以进入临床阶段,适用于棘阿米巴角膜炎治疗的持续眼部给药。