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首页> 外文期刊>Pharmaceutics >Fabrication of Transgelosomes for Enhancing the Ocular Delivery of Acetazolamide: Statistical Optimization, In Vitro Characterization, and In Vivo Study
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Fabrication of Transgelosomes for Enhancing the Ocular Delivery of Acetazolamide: Statistical Optimization, In Vitro Characterization, and In Vivo Study

机译：用于增强乙酰唑胺的眼递送的外胚层：统计优化，体外特征和体内研究的制备

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Acetazolamide (ACZ) is a potent carbonic anhydrase inhibitor that is used for the treatment of glaucoma. Its oral administration causes various undesirable side effects. This study aimed to formulate transgelosomes (TGS) for enhancing the ocular delivery of ACZ. ACZ-loaded transfersomes were formulated by the ethanol injection method, using phosphatidylcholine (PC) and different edge activators, including Tween 80, Span 60, and Cremophor RH 40. The effects of the ratio of lipid to surfactant and type of surfactant on % drug released after 8 h (Q 8h ) and entrapment efficiency (EE%) were investigated by using Design-Expert software. The optimized formula was formulated as TGS, using poloxamers as gelling agents. In vitro and in vivo characterization of ACZ-loaded TGS was performed. According to optimization study, F8 had the highest desirability value and was chosen as the optimized formula for preparing TGS. F8 appeared as spherical elastic nanovesicles with Q 8h of 93.01 ± 3.76% and EE% of 84.44 ± 2.82. Compared to a free drug, TGS exhibited more prolonged drug release of 71.28 ± 0.46% after 8 h, higher ex vivo permeation of 66.82 ± 1.11% after 8 h and a significant lowering of intraocular pressure (IOP) for 24 h. Therefore, TGS provided a promising technique for improving the corneal delivery of ACZ.
机译：乙酰唑胺（ACZ）是一种有效的碳酸酐酶抑制剂，用于治疗青光眼。其口服给药导致各种不良副作用。该研究旨在配制转基因体（TGS）以增强ACZ的眼部递送。通过磷脂酰胆碱（PC）和不同的边缘活化剂，包括乙醇注射方法，包括吐温80，跨度60和Cremophor RH 40的乙醇注射方法配制。脂质与表面活性剂的效果和％药物的表面活性剂的效果通过使用设计专家软件研究了8小时（Q 8H）和熵效率（EE％）后释放。优化的配方用衍生物作为胶凝剂配制为Tgs。在体外和体内表征ACZ负载的TGS。根据优化研究，F8具有最高的效率值，并选择作为制备TGS的优化配方。 F8出现为球形弹性纳米粒子，Q 8H为93.01±3.76％，EE％84.44±2.82。与游离药物相比，8小时后，Tgs在8小时后表现出更长的71.28±0.46％的延长药物释放，在8小时后较高66.82±1.11％和眼压（IOP）显着降低24小时。因此，TGS提供了一种有助于改善ACZ的角膜传递的技术。

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