A Comparative Study of an In Vitro Release Patterns of Ceftaroline Fosamil from Chemically-Prepared Coated Hydroxyapatite Nanoparticles -

Abstract

This research aimed to chemically synthesize four different sized hydroxyapatite (HA) compound nanoparticles, then coating them with trehalose sugar. After that, a drug release study in an in vitro model was achieved to evaluate the release of ceftaroline fosamil drug from HA different sized coated powders in a simulated body fluid.Calcium nitrate tetrahydrate and diammonium hydrogen phosphate were employed by sol-gel method and wet chemical method to produce the four different sized nanoparticles of hydroxyapatite compound. Identification of the produced HA nanoparticles was implemented using FTIR spectroscopy and X-ray diffraction. Additionally, scanning electron microscopy was utilized to check the morphology and particle size of the synthesized nanoparticles. These nanoparticles were coated by trehalose disaccharide. An in vitro release study was carried out to evaluate the release of ceftaroline fosamil, a low bacterial resistant 5th generation cephalosporin antibiotic, from the four HA coated nanoparticles, at a temperature of 37 OC for 4.5 hours with a time interval of 7.5 minutes, employing simulated body fluid as a releasing medium. The U.V. spectroscopy at I»max of 245.2 nm was used to check the loading amounts and to follow the release of ceftaroline from the synthesized coated HA nanoparicles. The loading percents of ceftaroline on the four identified HA nanoparticles were 59.6% w/w, 53.35% w/w, 38.21% w/w and 32.23% w/w. A percent of 75.84% w/w ceftaroline fosamil was released within 37.5 minutes from the coated hydroxyapatite nanoparticles that was formulated by sol-gel method with sintering for 12 hours. This release remained with a median of 74.95% w/w till the end of the 3rd hour, after that it started to decrease.The release of ceftaroline from HA nanoparticles that was formulated by sol-gel method with sintering for 12 hours, was the fastest to reach the steady state and the highest one during the study time than all other releases, so it is considered effective for futuristic therapeutic uses. The trehalose coating was expected to greatly diminish the hydroxyapatite-ceftaroline ionic interactions, resulting in increased drug release proficiency.