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Stability testing of tacrolimus-loaded poly(ԑ-caprolactone) nanoparticles by physicochemical assays and Raman spectroscopy
Vibrational Spectroscopy ( IF 2.5 ) Pub Date : 2020-09-01 , DOI: 10.1016/j.vibspec.2020.103139
Guilherme dos Anjos Camargo , Amanda Roderjan Cray da Costa Filha , Amanda Martinez Lyra , Andressa Novatski , Jessica Mendes Nadal , Lucas Stori de Lara , Daniele Toniolo Dias , Elizangela Anazilda do Nascimento , Uéslen Rocha Silva , Carlos Jacinto , Paulo Vitor Farago

Abstract Tacrolimus (TAC) or FK506 is a macrolide lactone isolated from the bacterial fermentation of Streptomyces tsukubaensis which belongs to the group of calcineurin inhibitors. Its main mechanism of action is to act on the immune system. In addition, this drug has been widely explored for skin disorders. However, TAC shows high molecular weight, high hydrophobicity, and low water solubility that can limit its ability to effectively permeate through the skin. Hence, it becomes imperative to develop a percutaneous drug delivery system for increasing its permeation in relation to the conventional ointment and for reducing the dose and the adverse effects as erythema, itching, and burning. Therefore, the aim of this work was to investigate the stability of colloidal suspensions of TAC-loaded poly(ԑ-caprolactone) (PCL) nanoparticles that were stored at room temperature for 120 days. In that sense, pH, particle size, polydispersity index (PDI), zeta potential, and Raman spectroscopy were performed. Significant decrease of pH (p 0.05) during the time interval investigated. Zeta potential presented statistically significant difference (p

中文翻译:

通过物理化学分析和拉曼光谱法对负载他克莫司的聚(己内酯)纳米颗粒进行稳定性测试

摘要 他克莫司(TAC) 或FK506 是从筑波链霉菌(Streptomyces tsukubaensis) 的细菌发酵中分离得到的一种大环内酯内酯,属于钙调神经磷酸酶抑制剂组。其主要作用机制是作用于免疫系统。此外,这种药物已被广泛用于治疗皮肤病。然而,TAC 显示出高分子量、高疏水性和低水溶性,这会限制其有效渗透皮肤的能力。因此,必须开发一种经皮给药系统,以增加其相对于传统软膏的渗透性,并减少剂量和红斑、瘙痒和灼痛等不良反应。所以,这项工作的目的是研究在室温下储存 120 天的载有 TAC 的聚(己内酯)(PCL)纳米颗粒的胶体悬浮液的稳定性。从这个意义上说,进行了 pH、粒度、多分散指数 (PDI)、zeta 电位和拉曼光谱。在调查的时间间隔内,pH 值显着降低 (p = 0.05)。Zeta 电位呈现出统计学上的显着差异(p
更新日期:2020-09-01
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