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.

Alginate hydrogels incorporating neomycin or propolis as potential dressings for diabetic ulcers: Structure, swelling, and antimicrobial barrier properties

“…For those samples, the drug could also interact with the polymeric chains, resulting in a higher gel fraction . Moreover, samples with high cross‐linking density have a higher probability to entrap drug molecules in their structure, resulting in an increased gel fraction . The lowest gel fraction was observed for the F0 sample.…”

Preformulation studies of ceftriaxone for pediatric non-parenteral administration as an alternative to existing injectable formulations

“…Most are based either on CTX complex formation (Lee et al, 2005(Lee et al, , 2006Cho et al, 2004) or on CTX encapsulation in the form of mucin-gelatin mucoadhesive microspheres (Ofokansi et al, 2007), lipospheres (Attama et al, 2009) or alginate encapsulated particles (Debrouse, patent US20090123537 A1, 2007;Patel et al, 2016). Improvement of CTX bioavailability from each of these formulations (except for lipospheres and enteric coated alginate beadsevaluated only in vitro) has been shown in rodents or rabbits after oral or rectal administration.…”

Tailored Hydrogel Microbeads of Sodium Carboxymethylcellulose as a Carrier to Deliver Mefenamic Acid: Transmucosal Administration

“…The thermograms were acquired at a scanning rate of 10°C/minute carried out at a heat limit of 25 -300°C (19,20).…”

“…The bead added in the cylinder was tapped mechanically for 200 times. Next, the tapped volume was recorded and bulk and tapped densities were computed (19).…”