Cationic Analog of Deoxycholate as an Oral Delivery Carrier for Ceftriaxone

Lee, Seulki; Kim, Sang Kyoon; Lee, Dong Yun; Park, Kyeongsoon; Kumar, Tadiparthi Suresh; Chae, Su Young; Byun, Youngro

doi:10.1002/jps.20478

Cited by 26 publications

(15 citation statements)

References 23 publications

(22 reference statements)

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“…This is due to the fact that ceftriaxone sodium, a third-generation cephalosporin is highly water-soluble but cannot be absorbed orally due to its acid labile nature and poor permeability across the GI epithelia. To overcome this situation, the drug must be incorporated into delivery systems that provide greater stability in the gastric fluids and also release the dose in a sustained manner (Lee et al 2005 ).…”

Section: Introductionmentioning

confidence: 99%

Development and evaluation of a calcium alginate based oral ceftriaxone sodium formulation

et al. 2016

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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.

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Section: Introductionmentioning

confidence: 99%

Development and evaluation of a calcium alginate based oral ceftriaxone sodium formulation

et al. 2016

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“…One attempt aimed at increasing its functional lipophilicity through the formation of ion pairs by coupling with positively charged bile acids (12,17). Another aimed at using absorption enhancers for increasing its membrane permeability (18).…”

Section: Introductionmentioning

confidence: 99%

Enhanced Antibacterial Effect of Ceftriaxone Sodium-Loaded Chitosan Nanoparticles Against Intracellular Salmonella typhimurium

2012

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Abstract. The aim of the present study was to utilize chitosan (CS) nanoparticles for the intracellular delivery of the poorly cell-penetrating antibiotic, ceftriaxone sodium (CTX). In vitro characterization of (CTX-CS) nanoparticles was conducted leading to an optimized formula that was assessed for its biocompatibility to blood (hemolysis test) and cells (MTT assay). Progressively, confocal laser scanning microscopy (CLSM), cellular uptake (microfluorimetry), and antibacterial activity of the nanoparticles were investigated in two cell lines: Caco-2 and macrophages J774.2 pre-infected with Salmonella typhimurium. Results showed that the optimized formula had size 210 nm, positive zeta potential (+30 mV) and appreciable entrapment efficiency for CTX (45%) and included a biphasic release pattern. The nanoparticles were biocompatible and were internalized by cells as verified by CLSM whereas microfluorimetry indicated substantial cellular uptake. Moreover, the CTX-chitosan nanoparticles showed a significant reduction in the count of intracellular S. typhimurium in Caco-2 and macrophages J774.2. This reduction was significantly higher than that obtained in case of placebo nanoparticles, CTX, and CTX-chitosan solutions and might be attributed to enhanced endocytic uptake of the nanoaprticles and antibacterial effect of the chitosan polymer. In conclusion, the results provide evidence for the potential use of chitosan nanoparticles to enhance the intracellular delivery and antibacterial effect of CTX in enterocytes and macrophages.

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“…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.…”

Section: Accepted Manuscriptmentioning

confidence: 96%

“…Thus, at physiological pH, CTX possesses two negative charges and is highly hydrophilic (Zhang et al, 2005a). It has a low octanol/water partition coefficient (log P = -2.1 ± 0.2) (Lee et al, 2005). Consequently, it is poorly absorbed through mucosal membranes, which explains why the only pharmaceutical form is injectable.…”

Section: Introductionmentioning

confidence: 98%

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

Kauss

Marchivie

Phoeung

et al. 2017

European Journal of Pharmaceutical Sciences

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Cationic Analog of Deoxycholate as an Oral Delivery Carrier for Ceftriaxone

Cited by 26 publications

References 23 publications

Development and evaluation of a calcium alginate based oral ceftriaxone sodium formulation

Development and evaluation of a calcium alginate based oral ceftriaxone sodium formulation

Enhanced Antibacterial Effect of Ceftriaxone Sodium-Loaded Chitosan Nanoparticles Against Intracellular Salmonella typhimurium

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

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