当前位置: X-MOL 学术Mater. Today Chem. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
The glucocorticoid derivative with the phthalimide group cationic nanocrystal for ophthalmic application: a design space development approach
Materials Today Chemistry ( IF 6.7 ) Pub Date : 2020-12-24 , DOI: 10.1016/j.mtchem.2020.100396
M.C.C. Peters , I.F. de Oliveira , M.G.M. Machado , D.C. Ferreira , M.H.A. Zanin , N. Bou-Chacra

The glucocorticoid derivative of budesonide with a phthalimide group is a drug candidate to treat inflammatory eye diseases; nevertheless, it presents low water solubility. Drug nanocrystals have been proposed to overcome this hurdle. The development of an innovative ophthalmic anti-inflammatory nanosuspension was performed using a design space approach. We obtained the particle size reduction of this glucocorticoid derivative on a nanometer scale (approximately 165.0 nm), applying wet bead milling on a super reduced scale. The design of experiment supported the optimization of the formula evaluating the parameters that influence reducing the particle size and also allowed determining the design space. Considering the two statistical models developed and the size range obtained, we proposed that the optimized formulation for the glucocorticoid derivative nanosuspension may be 1.0 wt% glucocorticoid derivative and 0.092 wt% cetylpyridinium chloride. This formulation was characterized by the morphological, physical–chemical, and mucoadhesive in vitro test and showed potential for ophthalmic use with reduced frequency of product application, improved efficiency, and safety, which may promote better patient compliance.



中文翻译:

用于眼科应用的具有邻苯二甲酰亚胺基团阳离子纳米晶体的糖皮质激素衍生物:一种设计空间开发方法

布地奈德带有邻苯二甲酰亚胺基团的糖皮质激素衍生物是治疗炎性眼病的候选药物。但是,它具有低水溶性。已经提出了药物纳米晶体来克服这一障碍。使用设计空间方法进行了创新性眼科消炎性纳米混悬剂的开发。我们以纳米尺寸(约165.0 nm)实现了这种糖皮质激素衍生物的粒径减小,并以超减小的尺寸进行了湿珠磨。实验设计支持公式的优化,以评估影响减小粒径的参数,还可以确定设计空间。考虑到开发的两个统计模型和获得的大小范围,我们提出,糖皮质激素衍生物纳米悬浮液的最佳配方可以为1.0 wt%的糖皮质激素衍生物和0.092 wt%的十六烷基氯化吡啶鎓。这种配方的特征是形态,物理化学和粘膜粘附体外测试表明,该产品具有降低眼科产品使用频率,降低产品应用频率,提高效率和安全性的潜力,从而可以提高患者的依从性。

更新日期:2020-12-24
down
wechat
bug