title: Development and evaluation of a calcium alginate based oral ceftriaxone sodium formulation.
abstract: The purpose of this work was to develop a multiparticulate system exploiting the pH-sensitive property and biodegradability of calcium alginate beads for intestinal delivery of ceftriaxone sodium (CS). CS was entrapped in beads made of sodium alginate and sodium carboxymethylcellulose (CMC), acacia, HPMC K4M and HPMC K15M as drug release modifiers. Beads were prepared using calcium chloride as a cross-linking agent, followed by enteric coating with cellulose acetate phthalate (CAP). The beads were then evaluated for entrapment efficiency using HPLC, in vitro drug release examined in simulated gastric fluid (pH 1.2) and simulated intestinal fluid (pH 6.8), swellability, particle size and surface characterization using optical microscopy, scanning electron microscopy (SEM), and atomic force microscopy (AFM). Thermal gravimetric analysis (TGA) was utilized to check the polymer matrix strength and thermal stability. The drug entrapment efficiency of the optimized formulation was determined to be 75 ± 5 %. Swelling properties of drug-loaded beads were found to be in a range of 0.9-3.4. Alginate beads coated with CAP and containing CMC as a second polymer exhibited sustained release. The drug release followed first-order kinetics via non-Fickian diffusion and erosion mechanism. The particle size of the beads was between 1.04 ± 0.20 and 2.15 ± 0.36 mm. TGA, AFM, and SEM data showed composition and polymer-dependent variations in cross-linking, thermal stability, surface structure, morphology, and roughness. The physico-chemical properties of the developed formulation indicate suitability of the formulation to deliver CS orally.
authors.affiliation: Industrial Pharmacy Division, Department of Pharmacy Practice, College of Pharmacy and Pharmaceutical Sciences, The University of Toledo, 3000 Arlington Avenue, MS1013, Toledo, OH USA.
authors.forename: Nachiket
authors.initials: N
authors.lastname: Patel
authors.affiliation: Industrial Pharmacy Division, Department of Pharmacy Practice, College of Pharmacy and Pharmaceutical Sciences, The University of Toledo, 3000 Arlington Avenue, MS1013, Toledo, OH USA.
authors.forename: Darshan
authors.initials: D
authors.lastname: Lalwani
authors.affiliation: Department of Science and Mathematics, Cedarville University, 251 N Main St., Cedarville, OH USA.
authors.forename: Steven
authors.initials: S
authors.lastname: Gollmer
authors.affiliation: Department of Pharmaceutical Sciences, School of Pharmacy, Cedarville University, 251 N Main St., Cedarville, OH USA.
authors.forename: Elisha
authors.initials: E
authors.lastname: Injeti
authors.affiliation: Department of Pharmacology, College of Pharmacy and Pharmaceutical Sciences, University of Toledo, 3000 Arlington Avenue, MS1013, Toledo, OH USA.
authors.forename: Youssef
authors.initials: Y
authors.lastname: Sari
authors.affiliation: Industrial Pharmacy Division, Department of Pharmacy Practice, College of Pharmacy and Pharmaceutical Sciences, The University of Toledo, 3000 Arlington Avenue, MS1013, Toledo, OH USA.
authors.forename: Jerry
authors.identifier: 0000-0003-4855-2405
authors.initials: J
authors.lastname: Nesamony
keywords: Atomic force microscopy; Calcium alginate; Ceftriaxone sodium; Controlled release; Ionotropic gelation; Thermogravimetric analysis