Development and Characterization of Synthetic Chalcones-Loaded Eudragit RS 100 Microparticles for Oral Delivery

• Published in: Journal of the Brazilian Chemical Society Vol. 28; no. 6; pp. 1074 - 1080
• Main Authors: Kleemann, Cristian, dos Santos, Talitha, Tavares, Luciana, Pizzolatti, Moacir, de Campos, Angela
• Format: Journal Article
• Language: English; Portuguese
• Published: Sociedade Brasileira de Química 01.06.2017
• Subjects: CHEMISTRY, MULTIDISCIPLINARY; chalcones; RP-HPLC; release control; microparticles; drug delivery system
• ISSN: 0103-5053; 1678-4790
• DOI: 10.21577/0103-5053.20160263

Eudragit® RS100 microspheres of two chalcones were prepared by solvent evaporation technique. A simple and rapid high-performance liquid chromatography (HPLC) method was developed and validated to determine the encapsulation efficiency, drug loading and release profiles of these chalcones in a microparticulate system. The mean EE values for the two chalcones-loaded microparticles were 98.8 ± 1.3% and 99.5 ± 0.9%. Scanning electron microscope (SEM) studies showed that one chalcone-loaded microspheres are spherical and smooth appearance whereas the other chalcone-loaded microspheres showed irregular particles and a rough surface. The analysis of the second chalcone by thermogravimetric analysis (TGA) showed a higher thermal stability compared to the first chalcone. Drug release profiles were determined at pH 7.4 phosphate buffered saline (100 mmol L-1) with sodium lauryl sulfate (0.5%). The systems prepared with Eudragit® showed 78 and 95% of the two chalcones were released after 24 hours. The experimental results indicated that the prepared polymeric microspheres may be useful for potential applications.