Department of Pharmaceutics, Virginia Commonwealth University, Richmond, VA 23298, USA.
Department of Ophthalmology, Virginia Commonwealth University, Richmond, VA 23298, USA; Department of Pathology, Virginia Commonwealth University, Richmond, VA 23298, USA.
Exp Eye Res. 2024 Jun;243:109902. doi: 10.1016/j.exer.2024.109902. Epub 2024 Apr 18.
Nitrogen mustard (NM) is a potent vesicating chemical warfare agent that is primarily absorbed through skin, inhalation, or ocular surface. Ocular exposure of NM can cause acute to chronic keratopathy which can eventually lead to blindness. There is a current lack of effective countermeasures against ocular exposure of NM despite their imperative need. Herein, we aim to explore the sustained effect of Dexamethasone sodium phosphate (DSP)-loaded polymeric nanoparticles (PLGA-DSP-NP) following a single subconjunctival injection in the management and prevention of corneal injury progression upon exposure to NM. DSP is an FDA approved corticosteroid with proven anti-inflammatory properties. We formulated PLGA-DSP-NP with zinc chelation ion bridging method using PLGA polymer, with particles of approximately 250 nm and a drug loading of 6.5 wt%. Under in vitro sink conditions, PLGA-DSP-NP exhibited a sustained drug release for two weeks. Notably, in NM injured cornea, a single subconjunctival (SCT) injection of PLGA-DSP-NP outperformed DSP eyedrops (0.1%), DSP solution, placebo NP, and saline, significantly mitigating corneal neovascularization, ulceration, and opacity for the two weeks study period. Through PLGA-DSP-NP injection, sustained DSP release hindered inflammatory cytokine recruitment, angiogenic factors, and endothelial cell proliferation in the cornea. This strategy presents a promising localized corticosteroid delivery system to effectively combat NM-induced corneal injury, offering insights into managing vesicant exposure.
氮芥(NM)是一种有效的糜烂性化学战剂,主要通过皮肤、吸入或眼表面吸收。NM 眼部暴露可导致急性至慢性角膜炎,最终导致失明。尽管对 NM 眼部暴露有迫切的需求,但目前仍缺乏有效的对策。在此,我们旨在探索单眼结膜下注射负载二磷酸地塞米松(DSP)的聚合物纳米粒(PLGA-DSP-NP)在 NM 暴露后管理和预防角膜损伤进展的持续效果。DSP 是一种经 FDA 批准的具有抗炎特性的皮质类固醇。我们使用 PLGA 聚合物通过锌螯合离子桥接法制备 PLGA-DSP-NP,其粒径约为 250nm,载药量为 6.5wt%。在体外溶出条件下,PLGA-DSP-NP 可在两周内持续释放药物。值得注意的是,在 NM 损伤的角膜中,单次眼结膜下(SCT)注射 PLGA-DSP-NP 优于地塞米松滴眼液(0.1%)、DSP 溶液、安慰剂 NP 和生理盐水,可显著减轻角膜新生血管、溃疡和混浊,在两周的研究期间。通过 PLGA-DSP-NP 注射,持续释放的 DSP 抑制了角膜中炎症细胞因子募集、血管生成因子和内皮细胞增殖。该策略为有效治疗 NM 诱导的角膜损伤提供了一种有前景的局部皮质类固醇递送系统,为处理糜烂性暴露提供了新的思路。