title: Formulation and Characterization of Polysaccharide Microparticles for Pulmonary Delivery of Sodium Cromoglycate.
abstract: Sodium cromoglycate (SC) is an antiasthmatic and antiallergenic drug commonly used for chronic inhalation therapy; however, many daily intakes are required due to the fast drug clearance from airways. For these reasons, SC polymeric particles for inhalatory administration with adequate aerosolization and mucoadhesive properties were designed to prolong the drug residence time in the site of action. Sodium carboxymethylcellulose (CMCNa), sodium hyaluronate, and sodium alginate were selected to co-process SC by spray drying. The influence of these polysaccharides on the spray drying process and powder quality was evaluated (among others, morphology, size, moisture content, hygroscopicity, flowability, densities, liquid sorption, and stability). In vitro aerosolization, drug release, and mucoadhesion performance were also studied. Particularly, a novel method to comparatively evaluate the interaction between formulations and mucin solution (mucoadhesion test) was proposed as a rapid methodology to measure adhesion properties of inhalable particles, being the results as indicative of clearance probability. Among all the studied formulations, the powder based on SC and CMCNa exhibited the best mucoadhesion and aerosolization performance, the highest process yield and adequate moisture content, hygroscopicity, and stability. SC-CMCNa formulation arose as a promising inhalatory system to reduce the daily intakes and to increase the patient compliance.
authors.affiliation: Department of Biology, Biochemistry and Pharmacy, Universidad Nacional del Sur, San Juan 670, (8000), Bahía Blanca, Argentina.|Department of Chemical Engineering-PLAPIQUI, Universidad Nacional del Sur-CONICET, Camino La Carrindanga Km. 7, (8000), Bahía Blanca, Argentina.
authors.forename: Loreana
authors.initials: L
authors.lastname: Gallo
authors.affiliation: Department of Chemical Engineering-PLAPIQUI, Universidad Nacional del Sur-CONICET, Camino La Carrindanga Km. 7, (8000), Bahía Blanca, Argentina.
authors.forename: Verónica
authors.initials: V
authors.lastname: Bucalá
authors.affiliation: Department of Biology, Biochemistry and Pharmacy, Universidad Nacional del Sur, San Juan 670, (8000), Bahía Blanca, Argentina. vrrigo@plapiqui.edu.ar.|Department of Chemical Engineering-PLAPIQUI, Universidad Nacional del Sur-CONICET, Camino La Carrindanga Km. 7, (8000), Bahía Blanca, Argentina. vrrigo@plapiqui.edu.ar.
authors.forename: María Verónica
authors.initials: MV
authors.lastname: Ramírez-Rigo
mesh_terms: D000280:Administration, Inhalation; D000464:Alginates / Q000737:chemistry; D002266:Carboxymethylcellulose Sodium / Q000737:chemistry; D004205:Cromolyn Sodium / Q000008:administration & dosage / Q000737:chemistry*; D004339:Drug Compounding; D020723:Glucuronic Acid / Q000737:chemistry; D006603:Hexuronic Acids / Q000737:chemistry; D006801:Humans; D008168:Lung / Q000187:drug effects*; D011134:Polysaccharides / Q000737:chemistry*; D017155:Wettability
chemical_list: D000464:Alginates; D006603:Hexuronic Acids; D011134:Polysaccharides; D020723:Glucuronic Acid; D002266:Carboxymethylcellulose Sodium; D004205:Cromolyn Sodium
keywords: inhaled particles; mucoadhesion; polysaccharides; sodium cromoglycate; spray drying