Krieser Katherine, Emanuelli Juliana, Daudt Renata Moschini, Bilatto Stanley, Willig Julia Biz, Guterres Silvia Stanisçuaski, Pohlmann Adriana Raffin, Buffon Andréia, Correa Daniel Souza, Külkamp-Guerreiro Irene Clemes
Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul (UFRGS), Avenida Ipiranga, 2572, Porto Alegre, RS 90610-000, Brazil.
Programa de Pós-Graduação em Ciências Farmacêuticas, UFRGS, Avenida Ipiranga, 2752, Porto Alegre, RS 90610-000, Brazil.
Mater Sci Eng C Mater Biol Appl. 2020 Dec;117:111315. doi: 10.1016/j.msec.2020.111315. Epub 2020 Aug 4.
This research has aimed to improve the stability and taste-masking properties by developing nanostructured dosage forms containing Saquinavir. Liquid formulations were developed using Eudragit RS100® and Pullulan as polymers. The physicochemical characteristics, stability, in vitro drug release, morphology, mucoadhesion and taste masking capacity were evaluated. The Saquinavir-nanoparticles had average diameters between 136 and 158 nm, with a Span below 1.4. These formulations presented a drug content above 80%, a high encapsulation efficiency (>97%), slightly acidic pH levels, low dynamic viscosity and controlled drug release. Electron microscopy revealed irregular spherical nanoparticles. The formulations prepared with higher amounts of Eudragit RS100® had greater mucoadhesion. Both polymers were able to improve drug stabilization, taste-masking properties and protection against drug cytotoxicity. The Saquinavir-nanoparticles exhibited stability and control releasing properties, thus making it a promising liquid dosage form with taste-masking properties intended for application in pediatric treatment.
本研究旨在通过开发含有沙奎那韦的纳米结构剂型来提高稳定性和掩味性能。使用Eudragit RS100®和支链淀粉作为聚合物开发液体制剂。对其理化特性、稳定性、体外药物释放、形态、粘膜粘附性和掩味能力进行了评估。沙奎那韦纳米颗粒的平均直径在136至158纳米之间，跨度低于1.4。这些制剂的药物含量高于80%，包封效率高（>97%），pH值略呈酸性，动态粘度低，药物释放可控。电子显微镜显示为不规则球形纳米颗粒。用较高量的Eudragit RS100®制备的制剂具有更强的粘膜粘附性。两种聚合物都能够改善药物稳定性、掩味性能并防止药物细胞毒性。沙奎那韦纳米颗粒表现出稳定性和控释特性，因此使其成为一种有前景的具有掩味性能的液体制剂，适用于儿科治疗。
