Spray drying formulation of albendazole microspheres by experimental design. In vitro-in vivo studies

• Published in: Drug development and industrial pharmacy Vol. 41; no. 2; pp. 244 - 252
• Main Authors: García, Agustina, Leonardi, Darío, Piccirilli, Gisela N., Mamprin, María E., Olivieri, Alejandro C., Lamas, María C.
• Format: Journal Article
• Language: English
• Published: England Informa Healthcare USA, Inc 01-02-2015; Informa Healthcare
• Subjects: Administration, Oral; Albendazole; Albendazole - administration & dosage; Albendazole - pharmacokinetics; Animals; Area Under Curve; Biological Availability; biomaterials; Carboxymethylcellulose Sodium - administration & dosage; Chemistry, Pharmaceutical - methods; Chitosan - administration & dosage; Drug Delivery Systems; Drug Stability; In Vitro Techniques; Male; Microscopy, Electron, Scanning; Microspheres; oral drug release; Pectins - administration & dosage; Rats; Rats, Wistar; spray drying; Albendazole; biomaterials; oral drug release; microspheres; spray drying
• ISSN: 0363-9045; 1520-5762
• DOI: 10.3109/03639045.2013.858737

Abstract
Both an experimental design and optimization techniques were carried out for the development of chitosan-pectin-carboxymethylcellulose microspheres to improve the oral absorption of albendazole as a model drug. The effect of three different factors (chitosan, pectin and carboxy methyl cellulose concentrations) was studied on five responses: yield, morphology, dissolution rate at 30 and 60 min, and encapsulation efficiency of the microspheres. During the screening phase, the factors were evaluated in order to identify those which exert a significant effect. Simultaneous multiple response optimizations were then used to find out experimental conditions where the system shows the most adequate results. The optimal conditions were found to be: chitosan concentration, 1.00% w/v, pectin concentration 0.10% w/v and carboxymethylcellulose concentration 0.20% w/v. The bioavailability of the loaded drug in the optimized microspheres was evaluated in Wistar rats which showed an area under curve (AUC) almost 10 times higher than the pure drug.