Ethylcellulose-Based Matrix-Type Microspheres: Influence of Plasticizer RATIO as Pore-Forming Agent

• Published in: AAPS PharmSciTech 2011-12, Vol.12 (4), p.1127-1135
• Main Authors: Sengel-Turk, C. Tuba, Hascicek, Canan, Gonul, Nursin
• Format: Article
• Language: English
• Subjects: Biochemistry; Biomedical and Life Sciences; Biomedicine; Biotechnology; Chemistry, Pharmaceutical; Citrates - chemistry; Diltiazem - chemistry; Drug Carriers; Drug Compounding; Ethylene Glycols - chemistry; Indexing in process; Kinetics; Microspheres; Particle Size; Pharmacology/Toxicology; Pharmacy; Plasticizers - chemistry; Porosity; Research Article; Solubility; Surface Properties; Technology, Pharmaceutical - methods; Transition Temperature
• ISSN: 1530-9932; 1530-9932
• DOI: 10.1208/s12249-011-9680-4

In this study, ethylcellulose (EC)-based microsphere formulations were prepared without and with triethyl citrate (TEC) content of 10% and 30% by water-in-oil emulsion-solvent evaporation technique. Diltiazem hydrochloride (DH) was chosen as a hydrophilic model drug and used at different drug/polymer ratios in the microspheres. The aim of the work was to evaluate the influence of plasticizer ratio on the drug release rate and physicochemical characteristics of EC-based matrix-type microspheres. The resulting microspheres were evaluated for encapsulation efficiency, particle size and size distribution, surface morphology, total pore volume, thermal characteristics, drug release rates, and release mechanism. Results indicated that the physicochemical properties of microspheres were strongly affected by the drug/polymer ratio investigated and the concentration of TEC used in the production technique. The surface morphology and pore volume of microspheres significantly varied based on the plasticizer content in the formulation. DH release rate from EC-based matrix-type microspheres can be controlled by varying the DH to polymer and plasticizer ratios. Glass transition temperature values tended to decrease in conjunction with increasing amounts of TEC. Consequently, the various characteristics of the EC microspheres could be modified based on the plasticized ratio of TEC.