title: Microencapsulation of sodium alendronate reduces drug mucosal damage in rats.
abstract: Sodium alendronate is an effective treatment for osteoporosis, but its oral administration is associated with adverse gastrointestinal effects. The aim of this work was to evaluate gastroresistant sodium alendronate-loaded microparticles prepared by spray-drying using Eudragit S100 or a blend of Eudragit S100/Methocel E4M. Both formulations presented high encapsulation efficiencies, mean diameters below 17 microm, and similar collapsed shape. Dissolution experiments showed good gastro-resistance for the microparticles at pH 1.2. At pH 6.8, the blended microparticles retarded the drug release. In vivo studies showed that the formulations were able to protect the rat stomachs against ulcer formation by sodium alendronate. In conclusion, the microparticles seems to be promising oral carriers for sodium alendronate.
authors.affiliation: Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Porto Alegre, Brazil.
authors.forename: Letícia
authors.initials: L
authors.lastname: Cruz
authors.forename: Evelise
authors.initials: E
authors.lastname: Assumpção
authors.forename: Sérgio Faloni
authors.initials: SF
authors.lastname: Andrade
authors.forename: Daniela Joyce
authors.initials: DJ
authors.lastname: Conrado
authors.forename: Sílvia Stanisçuaski
authors.initials: SS
authors.lastname: Guterres
authors.forename: Adriana Raffin
authors.initials: AR
authors.lastname: Pohlmann
mesh_terms: D019386:Alendronate / Q000009:adverse effects* / Q000138:chemical synthesis / Q000493:pharmacokinetics; D000818:Animals; D004339:Drug Compounding; D005260:Female; D005753:Gastric Mucosa / Q000187:drug effects* / Q000378:metabolism / Q000473:pathology; D007413:Intestinal Mucosa / Q000187:drug effects* / Q000378:metabolism / Q000473:pathology; D051381:Rats; D017208:Rats, Wistar
chemical_list: D019386:Alendronate