Taste-masked nanoparticles containing Saquinavir for pediatric oral administration

Author(s)

Krieser, Katherine ^[1] ; Emanuelli, Juliana ^[2] ; Daudt, Renata Moschini ^[3] ; Bilatto, Stanley ^[4] ; Willig, Julia Biz ^{[1, 2]} ; Guterres, Silvia Staniscuaski ^{[1, 2]} ; Pohlmann, Adriana Raffin ^{[2, 5]} ; Buffon, Andreia ^[1] ; Correa, Daniel Souza ^[4] ; Kulkamp-Guerreiro, Irene Clemes ^{[1, 2]}

Affiliation

^[1] Univ Fed Rio Grande do Sul UFRGS, Fac Farm, Ave Ipiranga 2572, BR-90610000 Porto Alegre, RS - Brazil

^[2] Univ Fed Rio Grande do Sul, Programa Posgrad Ciencias Farmaceut, Ave Ipiranga 2572, BR-90610000 Porto Alegre, RS - Brazil

^[3] Univ Fed Rio Grande do Sul, Dept Engn Quim, Rua Engenheiro Luiz Englert S-N, BR-90040040 Porto Alegre, RS - Brazil

^[4] Embrapa Instrumentacao, Lab Nacl Nanotecnol Agronegocio LNNA, BR-13560970 Sao Carlos, SP - Brazil

^[5] Univ Fed Rio Grande do Sul, Inst Quim, Dept Quim Organ, CP15003, Av Bento Goncalves 9500, BR-91501970 Porto Alegre, RS - Brazil

• Document type: Journal article
• Source: Materials Science & Engineering C-Materials for Biological Applications; v. 117, DEC 2020.
• Web of Science Citations: 0

Abstract

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 (R) 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 (R) 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. (AU)

• FAPESP's process: 17/12174-4 - Development of hybrid polymer nanofibers for agricultural applications
• Grantee: Daniel Souza Corrêa
• Support Opportunities: Regular Research Grants