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Stabilization of Etoricoxib Nanosuspension Using Acacia chundra Gum and Copolymers: Preparation, Characterization, and In Vitro Cytotoxic Study
ASSAY and Drug Development Technologies ( IF 1.6 ) Pub Date : 2021-07-12 , DOI: 10.1089/adt.2020.1054
Rishabha Malviya 1, 2 , Rajendra Awasthi 3 , Pramod Kumar Sharma 1 , Susheel Kumar Dubey 4
Affiliation  

Present communication deals with the stabilization of etoricoxib nanosuspension using Acacia chundra gum and its acrylamide-grafted and carboxymethylated copolymers. Acrylamide grafting and carboxymethylation of A. chundra gum were carried out and synthesized copolymers were characterized. Ultrasound-assisted solvent—antisolvent method was utilized to co-precipitate the stabilizers over etoricoxib nanoprecipitates. A 32 full factorial design was used to evaluate the effect of independent variables, that is, the concentration of drug and stabilizer over the dependent variables, that is, particle size (PS), and entrapment efficiency (EE%) of nanoparticles. The effect of process parameters over super saturation, nucleation, and PS were studied and the role of mixing and ultrasound radiation was correlated. FTIR, DSC, and 1H NMR analysis showed a significant difference between the copolymers. The application of stabilizers leads to the synthesis of small, spherical, no aggregated, and composite nanoparticles. PS growth analysis after 45 days showed no sign of “Ostwald repining” and aggregation. Optimized formulations prepared using A. chundra gum (formulation K9), acrylamide-grafted (formulation A8), and carboxymethylated (formulation C1) copolymers showed t80% in 190, 270, and 170 min, respectively. Cytotoxic studies showed that the formulation A8 had better control over cell growth than the pure drug against MCF-7 cell line. The results indicated that the A. chundra gum and its acrylamide and carboxymethylated copolymers can be easily synthesized and utilized for the fabrication of stabilized nanosuspension.

中文翻译:

使用金合欢胶和共聚物稳定依托考昔纳米混悬剂:制备、表征和体外细胞毒性研究

目前的交流涉及使用金合欢树胶及其丙烯酰胺接枝和羧甲基化共聚物稳定依托考昔纳米混悬剂。进行了A. chundra胶的丙烯酰胺接枝和羧甲基化,并对合成的共聚物进行了表征。超声辅助溶剂-反溶剂法用于在依托考昔纳米沉淀物上共沉淀稳定剂。一个 3 2全因子设计用于评估自变量的影响,即药物和稳定剂的浓度对因变量的影响,即粒径(PS)和纳米粒子的包封率(EE%)。研究了工艺参数对过饱和、成核和 PS 的影响,并将混合和超声辐射的作用相关联。FTIR、DSC 和1 H NMR 分析显示共聚物之间存在显着差异。稳定剂的应用导致小、球形、无聚集和复合纳米粒子的合成。45 天后的 PS 生长分析显示没有“Ostwald repining”和聚集的迹象。使用A. chundra制备的优化配方胶(配方 K9)、丙烯酰胺接枝(配方 A8)和羧甲基化(配方 C1)共聚物分别在 190、270 和 170 分钟内显示出80 % 的t 。细胞毒性研究表明,制剂 A8 比针对 MCF-7 细胞系的纯药物对细胞生长具有更好的控制。结果表明, A. chundra胶及其丙烯酰胺和羧甲基化共聚物可以很容易地合成并用于制备稳定的纳米悬浮液。
更新日期:2021-07-14
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