Formulation of clarithromycin floating microspheres for eradication of Helicobacter pylori

Nashar, Nourhan F. El; Donia, Ahmed A.; Mady, Omar Y.; Maghraby, Gamal M. El

doi:10.1016/j.jddst.2017.07.016

Cited by 13 publications

(10 citation statements)

References 22 publications

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“…The diffractogram of clarithromycin revealed the characteristic diffraction pattern for a crystalline material with intense reflections at Bragg's angle (2θ) of 11.41°, 13.69°, 15.11°, 17.23°, 20.38°, and 23.08°. This confirms the crystalline nature of clarithromycin as previously described in the literature [19]. The XRD results are also supported by our SEM analysis in which crystalline drug particles are clearly visible.…”

Section: Ray Diffraction (Xrd)supporting

confidence: 92%

“…The surface morphology and shape were assessed using a scanning electron microscope (SEM). The dry samples of blank, CLM3, and CLM6 were placed on aluminum stubs and coated with gold before taking SEM images [19].…”

Section: Drug Loading and Drug Entrapment Efficiencymentioning

confidence: 99%

“…The pure drug shows an absorption band at 3471 cm −1 , 2977 cm −1 , 23 cm −1 , 2341 cm −1 , 1691 cm −1 , and 1731 cm −1 which is due to the stretching of (O-H), (C-H (C≡N), (C≡C), carbonyl groups (C=O), and lactone rings, respectively. Moreover, the a sorbance bands of oxygen (ether linkage) were recorded at 1172 cm −1 , 1057 cm −1 , and 10 cm −1 [19,46]. The characteristic peak at 1596 cm −1 indicates the stretching of a (COO-) gro in sodium alginate, which was observed in the blank as well as both formulations [4 Similarly, HPMC shows the absorption peak at 1050 cm −1 , which is due to stretching the (C-O) group [48] and was observed in all formulations (Figure 6).…”

Section: Fourier Transform Infrared Spectroscopymentioning

confidence: 99%

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Assessing the Synergistic Activity of Clarithromycin and Therapeutic Oils Encapsulated in Sodium Alginate Based Floating Microbeads

et al. 2022

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We developed alginate-based floating microbeads of clarithromycin with therapeutic oils for the possible eradication of Helicobacter pylori (H. pylori) infections by enhancing the residence time of the carrier at the site of infection. In pursuit of this endeavor, the alginate was blended with hydroxy propyl methyl cellulose (HPMC) as an interpenetrating polymer to develop beads by ionotropic gelation using calcium carbonate as a gas generating agent. The developed microbeads remained buoyant under gastric conditions for 24 h. These microbeads initially swelled and afterwards decreased in size, possibly due to the erosion of the polymer. Furthermore, swelling was also affected by the type of encapsulated oil, i.e., swelling decreased with increasing concentrations of eucalyptus oil and increased with increasing concentrations of oleic acid. Antibacterial assays of the formulations showed significant antibacterial activity against Staphylococcus aureus (S. aureus) and Escherichia coli (E. coli); these assays also showed synergistic activity between clarithromycin and therapeutic oils as evident from the higher zone of inhibition of the microbeads as compared to the pure drug and oils. Scanning electron microscopy (SEM) images revealed a smoother surface for oleic acid containing the formulation as compared to eucalyptus oil containing the formulation. Differential scanning calorimetry (DSC) and thermogravimetric analysis (TGA) revealed the development of a stable formulation, while Fourier transform infrared spectrophotometry (FTIR) studies did not reveal any interaction between the polymers and the active ingredients. Optimized formulations (CLM3 and CLM6) were designed to release the drug in a controlled manner in gastric media by Fickian diffusion. Conclusively, the developed microbeads are a promising carrier to overcome the narrow therapeutic index and low bioavailability of clarithromycin, while the presence of therapeutic oils will produce synergistic effects with the drug to eradicate infection effectively.

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Section: Ray Diffraction (Xrd)supporting

confidence: 92%

Section: Drug Loading and Drug Entrapment Efficiencymentioning

confidence: 99%

Section: Fourier Transform Infrared Spectroscopymentioning

confidence: 99%

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Assessing the Synergistic Activity of Clarithromycin and Therapeutic Oils Encapsulated in Sodium Alginate Based Floating Microbeads

et al. 2022

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“…According to the ICH guidelines stability study was carried out for optimized formulations. Formulations of oating microspheres were held in stability chamber for 90 days with temperature of 40ºC ± 2ºC, and relative humidity of 75% ± 5% (19) . After each time interval of 0, 30, 60 and 90 days optimized formulations were evaluated for buoyancy and in-vitro dissolution study [26,34].…”

Section: Stability Studiesmentioning

confidence: 99%

Floating microspheres of Miglitol as gastro retentive drug delivery system: 32 full factorial design and in vitro evaluation

Cheran

Bolmal

Patil

et al. 2021

Preprint

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Background: The goal of this study was to develop a gastro retentive floating drug delivery system that would improve site specific activity, patient compliance and therapeutic efficacy.Methodology: Floating microspheres of Miglitol were formulated by double emulsion method using ethyl cellulose and eudragit E100 different weight ratio and PVA as an emulsifier. It has been prepared with respect quantity of polymer concentration and stirring speed to evaluate for % buoyancy, drug entrapment efficiency, particle size drug release rate. Result: The percent of buoyancy, drug entrapment efficiency, particle size, and percentage yield were increased with increase the polymer mixture concentration. Among all formulation batches, F6 showed acceptable results drug entrapment efficiency (86.57%) and buoyancy (94.25%). F10 formulation was prepared to check the predicted and actual factors and compared with optimized formulation F6. The drug release was increased as the polymer concentration was decrease. The kinetic model zero order had the highest regression coefficient value, it was described as a sustained release dosage form. According to ICH guideline accelerated stability studies of F6 and F10 formulations were conducted for 90 days. After 90 days buoyancy and in vitro drug release was performed and the results were F6 and F10 buoyancy was found to be 88.21%, 87.22% and in vitro drug release was found to be 62.87%, 63.51%. Conclusion: The present study, showed compatibility of drug with polymers by FTIR in formulation. Floating microsphere of Miglitol was prepared by double emulsion technique. The F6 Miglitol floating microsphere was optimized formulation demonstrated with excellent drug entrapment performance (86.57%), good floating behaviour (94.25%), and the largest particle size (670µm). The present study concludes that floating based gastro retentive delivery system of Miglitol microspheres has a safe and effective drug delivery system with increased therapeutic efficacy and a longer duration of action.

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“…The drug entrapment efficiency in floating microspheres can be estimated by dissolving a predetermined amount of microspheres in methanol, filter the samples and analyze spectrophotometrically after appropriate dilution if required [25,26]. This study is carried out by using USP Type I dissolution apparatus stirred at 100 rpm at 37±0.5 °С.…”

Section: Drug Entrapment Efficiencymentioning

confidence: 99%

Effect Processing Variables on the Characteristics of Itraconazole Hollow Microspheres

2019

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Objective: The purpose of the study was to develop the multiple unit non-effervescent gastroretentive floating hollow microspheres to enhance the bioavailability of the drug by varying the concentration of low-density polymer and release modifier to retaining the formulation at its absorption site. Design of experiment approach applied to get the best possible formulation with minimum assets and experimentation. Methods: The hollow microspheres were prepared by emulsion solvent diffusion-evaporation technique using ethylcellulose as low-density polymer and Eudragit E100 as release modifier. The central composite design was used for the optimization of independent variables and was evaluated for particle size, entrapment efficiency, in vitro floating ability and drug release characteristics. Results: The physicochemical analysis was done to confirm any interaction between drug and excipients. The Scanning Electron Microscopy (SEM) showed a smooth, spherical surface with an inner hollow cavity. The stability study proves that the hollow microspheres were more stable under different storage conditions with no significant changes in formulation. The drug release mechanism of the optimized batch can be explained by Korsmeyer Peppas model. Conclusion: Based on the results, the hollow microspheres with a release modifying polymer offers a superior approach to retain the formulation in the stomach.

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Formulation of clarithromycin floating microspheres for eradication of Helicobacter pylori

Cited by 13 publications

References 22 publications

Assessing the Synergistic Activity of Clarithromycin and Therapeutic Oils Encapsulated in Sodium Alginate Based Floating Microbeads

Assessing the Synergistic Activity of Clarithromycin and Therapeutic Oils Encapsulated in Sodium Alginate Based Floating Microbeads

Floating microspheres of Miglitol as gastro retentive drug delivery system: 32 full factorial design and in vitro evaluation

Effect Processing Variables on the Characteristics of Itraconazole Hollow Microspheres

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