Nimesulide/cyclodextrin/PEG 6000 ternary complexes: physico-chemical characterization, dissolution studies and bioavailability in rats

Dutet, Julie; Lahiani-Skiba, Malika; Didier, Ludovic; Jezequel, Soizic; Bounoure, F.; Barbot, Cécile; Arnaúd, Philippe; Sarakha, Mohamed

doi:10.1007/s10847-006-9193-z

Cited by 17 publications

(10 citation statements)

References 4 publications

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“…Nimesulide belongs to the class-II biopharmaceutical classification drug with a low solubility and high permeability [17,18]. Nimesulide is a weak inhibitor of prostaglandin synthesis in vitro and it appears to show its effects by a variety of mechanisms like free-radical scavenging, involving in neutrophil myeloperoxidase pathway, phosphodiesterase type IV inhibition, histamine release, tumor necrosis factor-alpha release, cartilage degradation, bradykinin activity, metaloprotease synthesis, platelet aggregation, and synthesis of platelet activity factor [19,20] used the Nimesulide in control drug delivery [21,22]. Nimesulide produces gastric irritation in some cases and shows loss of its inhibitory cyclooxygenase-2 (COX-2) selectivity [23,24].…”

Section: Introductionmentioning

confidence: 99%

Sodium Alginate–locust Bean Gum Ipn Hydrogel Beads for the Controlled Delivery of Nimesulide-Anti-Inflammatory Drug

Madhavi¹,

Babu²,

Maruthi³

et al. 2017

Int J Pharm Pharm Sci

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Objective: The objective of this study was to formulate and evaluate the drug release studies using locust bean gum (LBG) and sodium alginate (NaAlg) and cross-linked with glutaraldehyde for the controlled release (CR) of Nimesulide, an anti-inflammatory drug.Methods: Locust bean gum (LBG) and sodium alginate (NaAlg) blend hydrogel beads were prepared by an extrusion method using glutaraldehyde as a crosslinker. Nimesulide an anti-inflammatory drug was encapsulation within LBG/NaAlg blend hydrogel beads. Morphology, size, encapsulation efficiency and drug release from these hydrogel beads were evaluated by different characterization techniques such as fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), scanning electron microscopy (SEM), x-ray diffraction (X-RD) studies.Results: Drug-loaded hydrogel beads were analyzed by FTIR, which indicates the interaction between drug and polymers. DSC thermograms on drug-loaded microbeads confirmed the polymorphism of Nimesulide and indicated a molecular level dispersion of the drug in the hydrogel beads. SEM confirmed the spherical nature and rough surface of the hydrogel beads produced. X-RD study was performed to understand the crystalline nature of drug after encapsulated into the hydrogel beads and confirmed the complete dispersion of the drug in the polymer matrix. In vitro release studies conducted in pH-7.4 which indicated a dependence of release rate on the amount of drug loading and the amount of LBG/NaAlg, but slow release rates were extended up to 48 h. The cumulative release data were fitted to an empirical equation to compute diffusion exponent (n) which indicated the non-fickian trend for drug release. Conclusion:These results clearly demonstrated that the ability of these newly developed hydrogel beads containing Nimesulide for its sustained release could possibly be advantageous to patient compliance with reduced dosing interval.

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Section: Introductionmentioning

confidence: 99%

Sodium Alginate–locust Bean Gum Ipn Hydrogel Beads for the Controlled Delivery of Nimesulide-Anti-Inflammatory Drug

Madhavi¹,

Babu²,

Maruthi³

et al. 2017

Int J Pharm Pharm Sci

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“…[40][41][42] Dutet et al, and Ravikumar et al, used the nimesulide in control drug delivery. [43,44] Nimesulide produces gastric irritation in some cases and shows loss of its inhibitory cyclooxygenase-2 (COX-2) selectivity. [45,46] Nimesulide is sparingly soluble in water (0.01 mg/mL).…”

Section: Original Articlementioning

confidence: 99%

Preparation and characterization of nimesulide loaded poly (methyl methacrylate)/poly (ethylene oxide) blend microspheres: In vitro release studies

Rao¹,

Mallikarjuna²,

Prasad³

et al. 2013

Asian J Pharm

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P oly (methyl methacrylate)/poly (ethylene oxide) (PMMA/PEO) blend microspheres were prepared by solvent evaporation technique using poly (vinyl alcohol) (PVA) as a stabilizer. Nimesulide, an arthritis drug was successfully loaded into these microspheres. The effect of experimental variables such as ratio of ploy (methyl methacrylate) to poly (ethylene oxide) on nimesulide encapsulation efficiency, release rate, size, and morphology of the microspheres has been investigated. Nimesulide loaded microspheres were analyzed using Fourier transform infrared (FTIR), differential scanning calorimetry (DSC), X-ray diffraction (X-RD), and scanning electron micrograph (SEM). FTIR spectroscopy was used to explain the blending of polymers. DSC and X-RD techniques were used to investigate the crystalline nature of the drug after encapsulation. DSC and X-RD results indicated a nonuniform dispersion of nimesulide in the PMMA/PEO blend matrix. SEMs indicated the formation of spherical microspheres with distinct size. Nimesulide was successfully encapsulated up to 85% in the polymeric matrices. In vitro dissolution experiments performed in pH 7.4 buffer medium indicated a controlled release of nimesulide from blend microspheres up to 12 h.

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“…To overcome these disadvantages, increasing the aqueous solubility is an important goal. Different efforts have been made to improve the aqueous solubility of NIM, such as hotropic solubilization [3], use of surfactants [4,5], cosolvents methods [6], ternary solid dispersions [7] or by complexing NIM with cyclodextrins, where these inclusion complexes have been shown to improve the stability, solubility, dissolution rate, and bioavailability of the drug [8][9][10][11].…”

Section: Introductionmentioning

confidence: 99%

“…Cyclodextrins, with hydrophobic inner cavities and hydrophilic outer surfaces, are capable of interacting with a large variety of hydrophobic or hydrophilic guest molecules to form non-covalent inclusion complexes [13]. Natural CDs especially -CD have been widely used in the early stages of pharmaceutical applications because of their availability and their cavity size, suitable for wide range of drugs in the form of binary systems or ternary systems (supported with polymers) [7,14]. However, the low aqueous solubility and nephrotoxicity of -CD limit its use especially in parenteral route of drug delivery.…”

Section: Introductionmentioning

confidence: 99%

Nimesulide Apparent Solubility Enhancement with Natural Cyclodextrins and their Polymers

Joudieh¹,

Lahiani-Skiba²,

Bon³

et al. 2008

LDDD

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The object of this work is to investigate physicochemical characteristics and inclusion behavior of binary systems based on cyclodextrin polymer (Poly-CD) or native cyclodextrins (CDs) with a poorly water-soluble, nonsteroidal anti-inflammatory drug, nimesulide (NIM) chemically, N-(4-nitro-2-phenoxyphenyl)methanesulfonamide. Our formulations were studied in solution and solid-state. Drug-cyclodextrin solid binary systems were prepared by the freezedrying method. Phase solubility study was used to evaluate the interaction in solution, between NIM/CDs and NIM/(Poly-CD). The stability constants of NIM/CDs and NIM/(Poly-CD) complexes were calculated using the phase solubility method. The apparent solubility of NIM was enhanced especially with Poly--CD (up to78-fold) in neutral aqueous solutions without any organic solvents or surfactants. Copmlexes formation was confirmed, in the solid state, by differential scanning calorimetry, infrared spectroscopy and DRX. Complexation spontaneity of drug with cyclodextrin polymers was highlighted using G° values.

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Nimesulide/cyclodextrin/PEG 6000 ternary complexes: physico-chemical characterization, dissolution studies and bioavailability in rats

Cited by 17 publications

References 4 publications

Sodium Alginate–locust Bean Gum Ipn Hydrogel Beads for the Controlled Delivery of Nimesulide-Anti-Inflammatory Drug

Sodium Alginate–locust Bean Gum Ipn Hydrogel Beads for the Controlled Delivery of Nimesulide-Anti-Inflammatory Drug

Preparation and characterization of nimesulide loaded poly (methyl methacrylate)/poly (ethylene oxide) blend microspheres: In vitro release studies

Nimesulide Apparent Solubility Enhancement with Natural Cyclodextrins and their Polymers

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