Calcium alginate multi-unit oral dosage form for delayed release of celecoxib

Segale, Lorena; Mannina, Paolo; Giovannelli, Lorella; Pattarino, Franco

doi:10.1016/j.jddst.2015.02.001

Cited by 13 publications

(9 citation statements)

References 35 publications

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“…The excipients selected for the self-emulsifying phase were Labrasol, a liquid component with self-emulsifying and solubility enhancer properties, and D- α -tocopheryl polyethylenglycol 1000 succinate as coemulsifying and absorption enhancer agent ( Table 1 ). The composition of the self-emulsifying phase was the same used in a previous work [ 34 ].…”

Section: Resultsmentioning

confidence: 99%

“…All the formulations contain high amount of drug ( Table 2 ) homogeneously distributed in the excipient matrix and the differences among their drug content were not significant except for CAlCh 400 slightly lower than the others ( p < 0.001). The percentage of celecoxib in the beads exceeds the theoretical value and this is due to the loss of Labrasol during the curing time [ 34 ], justifiable considering the high affinity between this excipient and water which drives it out of the beads into the gelling bath.…”

Section: Resultsmentioning

confidence: 99%

“…Calcium alginate beads were prepared by gelation method using calcium ions as cross-linking agent. In detail, a 1.5% (w/w) sodium alginate aqueous solution was mixed with a drug loaded self-emulsifying phase in 4 : 1 ratio and added drop by drop to a 100 mM CaCl 2 solution [ 34 ]. The self-emulsifying phase was prepared mixing weighed amounts of Labrasol and TPGS at 50°C and dissolving celecoxib in the excipient solution.…”

Section: Methodsmentioning

confidence: 99%

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Calcium Alginate and Calcium Alginate-Chitosan Beads Containing Celecoxib Solubilized in a Self-Emulsifying Phase

et al. 2016

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In this work alginate and alginate-chitosan beads containing celecoxib solubilized into a self-emulsifying phase were developed in order to obtain a drug delivery system for oral administration, able to delay the drug release in acidic environment and to promote it in the intestinal compartment. The rationale of this work was linked to the desire to improve celecoxib therapeutic effectiveness reducing its gastric adverse effects and to favor its use in the prophylaxis of colon cancer and as adjuvant in the therapy of familial polyposis. The systems were prepared by ionotropic gelation using needles with different diameters (400 and 600 μm). Morphology, particle size, swelling behavior, and in vitro drug release performance of the beads in aqueous media with different pH were investigated. The experimental results demonstrated that the presence of chitosan in the formulation caused an increase of the mechanical resistance of the bead structure and, as a consequence, a limitation of the bead swelling ability and a decrease of the drug release rate at neutral pH. Alginate-chitosan beads could be a good tool to guarantee a celecoxib colon delivery.

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Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

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Calcium Alginate and Calcium Alginate-Chitosan Beads Containing Celecoxib Solubilized in a Self-Emulsifying Phase

et al. 2016

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“…Celecoxib (CX), a selective cyclooxygenase-2 inhibitor non-steroidal anti-inflammatory drug (NSAID), is the drug of choice for chronic inflammatory diseases. However, its erratic absorption, reduced aqueous solubility and bioavailability require the administration of high doses (200-400 mg twice a day) to achieve the desired outcomes [1]. The longterm use of high doses results in serious gastrointestinal tract (GIT)-related side effects including bleeding, ulcerations, heart burn, discomfort, and perforations [1,2].…”

Section: Introductionmentioning

confidence: 99%

Fabrication and Characterization of Celecoxib-Loaded Chitosan/Guar Gum-Based Hydrogel Beads

et al. 2023

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The aim of this study was to fabricate celecoxib-loaded chitosan/guar gum (CS/GG) single (SC) and dual (DC) crosslinked hydrogel beads using the ionotropic gelation approach. The prepared formulations were evaluated for entrapment efficiency (EE%), loading efficiency (LE%), particle size and swelling studies. The performance efficiency was assessed by in vitro drug release, ex-vivo mucoadhesion, permeability, ex-in vivo swelling and in vivo anti-inflammatory studies. The EE% was found to be ~55% and ~44% for SC5 and DC5 beads, respectively. The LE% was ~11% and ~7% for SC5 and DC5 beads, respectively. The beads showed a matrix-like network with thick fibers. The particle size of beads ranged from ~2.74 to 1.91 mm. About 74% and 24% celecoxib was released from SC and DC hydrogel beads, respectively, within 24 h. The SC formulation showed higher %swelling and permeability than the DC counterpart, while the %mucoadhesion was relatively higher for DC beads. During the in vivo study, a significant decrease in the inflammation of the rat paw and inflammatory markers including C-reactive proteins (CRP) and interleukin-6 (IL-6) was observed following treatment with the prepared hydrogel beads; however, the SC formulation showed better therapeutic efficiency. In conclusion, celecoxib-loaded crosslinked CS/GG hydrogel beads can provide sustained drug release and act as potential candidates for managing inflammatory conditions.

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“…The inhibition of isoform COX-2 helps in reducing the number of inflammation mediators [ 1 ]. CLB is highly effective in the treatment of osteo and rheumatoid arthritis [ 2 , 3 ] when compared to other NSAIDs such as naproxen and diclofenac. It is also used in the treatment of ankylosing spondylitis, colonic polyps and menstrual cramps.…”

Section: Introductionmentioning

confidence: 99%

Development of stealth liposomal formulation of celecoxib: In vitro and in vivo evaluation

et al. 2022

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Celecoxib (CLB) is a highly hydrophobic selective cyclo-oxygenase inhibitor with high plasma protein binding and undergoes extensive hepatic metabolism. CLB is highly effective in the treatment of osteo and rheumatoid arthritis as first line therapy but produces severe gastro-intestinal toxicities and cardiovascular side effects. In this research, stealth liposomes of CLB were developed with the intention to reduce the side effects and increase the accumulation of drug in the sites of inflammation. Stealth liposomes were prepared by thin film hydration technique using distearoylphosphatidylcholine and PE-PEG 2000 with variable amounts of cholesterol and characterized. The effects of various lipids such as hydrogenated soy phosphatidylcholine, dipalmitoyl phosphatidylcholine, distearoylphosphatidylcholine and cholesterol content on % drug encapsulation was investigated. The optimized stealth liposomes were characterized by FT-IR and DSC for possible drug excipients interaction. Pharmacokinetics, pharmacodynamics and biodistribution studies were carried out for the stealth liposomes. The results revealed that the stealth liposomes reduced the inflammation to the larger magnitude and have also sustained the magnitude when compared to free drug along with maximum analgesic response. Higher elimination half-life, AUC, MRT and lowered clearance rate denotes the extended bioavailability of the drug in blood. Biodistribution studies revealed that stealth liposomes extend the circulation time of liposomes in blood by decreasing opsonisation and be less concentrated in kidney, thereby reducing the toxicities to RES and renal organs and facilitate the drug accumulation in the area of inflammation. Our results indicated that CLB, without the requirement of modifications to enhance solubilisation, can be encapsulated and released from liposomal formulations. This new-fangled drug delivery approach may be used to circumvent the low bioavailability and toxic side effects of oral CLB formulations.

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Calcium alginate multi-unit oral dosage form for delayed release of celecoxib

Cited by 13 publications

References 35 publications

Calcium Alginate and Calcium Alginate-Chitosan Beads Containing Celecoxib Solubilized in a Self-Emulsifying Phase

Calcium Alginate and Calcium Alginate-Chitosan Beads Containing Celecoxib Solubilized in a Self-Emulsifying Phase

Fabrication and Characterization of Celecoxib-Loaded Chitosan/Guar Gum-Based Hydrogel Beads

Development of stealth liposomal formulation of celecoxib: In vitro and in vivo evaluation

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