立方体;持续和改进青光眼治疗眼部给药的一种方法:方框本肯优化、配方、体外表征和体内渗透研究

Shubhangi Aher, Bharati Nimase
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引用次数: 0

摘要

简介:在青光眼中,乙酰唑胺(ACZ)用于降低眼内压(IOP)。低水溶性和角膜渗透性降低是乙酰脞胺的两个特点。本研究旨在提高 ACZ 的眼部给药效果。材料与方法:采用方框-贝肯设计法,利用熔融分散乳化和超声法制成了装有乙酰唑胺的立方体。自变量包括甘油单油脂(GMO)、聚乙烯醇(PVA)和聚羟胺 407(P407)。制备的制剂进行了多分散指数(PDI)、粒度和包埋效率的评估。此外,还对所开发的制剂进行了热分析、体外表征和渗透性测试。结果显示优化配方的 PDI 为 0.23 ± 0.03,平均粒径为 243 ± 4.2 nm,zeta 电位为 -26.1 ± 0.6 mV,夹带效率为 73.99%,在 TEM 下呈立方体结构。体内外渗透研究表明,药物在山羊角膜中的渗透率有所提高。眼刺激试验证实了所制备立方体的安全性、稳定性和通过角膜给药的能力。结论优化后的立方体制剂具有改善青光眼治疗的潜力,有望用于 ACZ 的眼部给药。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Cubosomes; An Approach to Sustain and Improve the Ocular Delivery for Glaucoma Treatment: Box Benhken Optimization, Formulation, In Vitro Characterization and Ex Vivo Permeation Study
Introduction: In glaucoma, acetazolamide (ACZ) is used to lower intraocular pressure (IOP). Low aqueous solubility and decreased corneal permeation are two characteristics of ACZ. This research intends to enhance the ocular delivery of ACZ. Materials and Methods: Using a Box-Behnken design, cubosomes loaded with acetazolamide were made using the Melt dispersion emulsification and sonication method. The independent variables included Glyceryl monoolein (GMO), polyvinyl alcohol (PVA) and Poloxamer 407 (P407. The prepared formulations underwent evaluation for polydispersity index (PDI), particle size and entrapment efficiency. Thermal analysis, in vitro characterisation and permeation were among the additional tests performed on the developed formulation. Results: Optimized formulation showed PDI of 0.23 ± 0.03, mean particle size of 243 ± 4.2 nm, zeta potential of -26.1 ± 0.6 mV, entrapment efficiency of 73.99% and cubic structure under TEM. Drug penetration through goat cornea has increased, according to an ex vivo permeation study. The prepared cubosome safety, stability and ability to be delivered through the cornea were confirmed by the ocular irritation test. Conclusion: The optimized cubosomal formulation has the potential to improve glaucoma treatment and be regarded as promising for ocular delivery of ACZ.
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