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.
Highlights
The oral route of administration is the most convenient, preferable, and desirable method of administering therapeutic agents for systemic effects
The beads were evaluated for entrapment efficiency using HPLC, in vitro drug release examined in simulated gastric fluid and simulated intestinal fluid, swellability, particle size and surface characterization using optical microscopy, scanning electron microscopy (SEM), and atomic force microscopy (AFM)
Chitosan was not used in our optimized formulation because it contributed to a significant increase in particle size and agglomeration after recovering and drying the coated beads
Summary
The oral route of administration is the most convenient, preferable, and desirable method of administering therapeutic agents for systemic effects. (i.p.) injections of this drug in rats attenuated cue-induced cocaine relapse-like behavior (Sari et al 2009; Knackstedt et al 2010). This effect is partly due to upregulation of expression of a major glutamate transporter, which is called glutamate transporter 1 (GLT-1), in several brain regions. It was found that ceftriaxone-attenuated, relapse-like alcohol-drinking behavior was associated with upregulation of GLT-1 and GLT-1 isoforms (GLT-1a and GLT-1b) in male alcohol-preferring rats (Alhaddad et al 2014; Qrunfleh et al 2013; Rao and Sari 2014)
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