Development of Floating-Mucoadhesive Microsphere for Site Specific Release of Metronidazole

Amin, Md. Lutful; Ahmed, Tasnia; Mannan, Md. Abdul

doi:10.15171/apb.2016.027

Cited by 21 publications

(19 citation statements)

References 20 publications

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“…The modified microspheres exhibited a % buoyancy of 87.66 ± 1.28% and a floating lag time of 15 ± 3.2 s. Furthermore, the microspheres remained buoyant for up to 12 h. The improvement in floating behavior of the microspheres was attributed to the generation of CO 2 on contact with the dissolution fluid, resulting in the microspheres floating and these observations are similar to what has been reported [76]. The dissolution of sodium bicarbonate and production of CO 2 may have created spaces within the microspheres into which dissolution medium diffused leading to erosion and reduced density of core [75]. The manufacturing process produced discrete spherical microspheres with a % yield of 97.56%.…”

Section: Responsesupporting

confidence: 80%

“…Consequently, many of the microspheres would be emptied into the small intestine fairly rapidly in vivo, which has bioavailability implications as the solubility and absorption of RIF are low from this part of the GIT. Therefore, the inclusion of sodium bicarbonate (Aspen ® Pharmacare, Port Elizabeth, Eastern Cape, South Africa) to the formulation was considered as CO 2 is generated when the compound is exposed to acid, which would, therefore, improve the floating and buoyancy of the microspheres [75].…”

Section: Responsementioning

confidence: 99%

“…Pharmaceutics 2020, 12, x 20 of 28 has been reported [76]. The dissolution of sodium bicarbonate and production of CO2 may have created spaces within the microspheres into which dissolution medium diffused leading to erosion and reduced density of core [75]. The manufacturing process produced discrete spherical microspheres with a % yield of 97.56%.…”

Section: Responsementioning

confidence: 99%

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Improved Stability of Rifampicin in the Presence of Gastric-Resistant Isoniazid Microspheres in Acidic Media

Mwila

Walker

2020

Pharmaceutics

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The degradation of rifampicin (RIF) in an acidic medium to form 3-formyl rifamycin SV, a poorly absorbed compound, is accelerated in the presence of isoniazid, contributing to the poor bioavailability of rifampicin. This manuscript presents a novel approach in which isoniazid is formulated into gastric-resistant sustained-release microspheres and RIF into microporous floating sustained-release microspheres to reduce the potential for interaction between RIF and isoniazid (INH) in an acidic environment. Hydroxypropyl methylcellulose acetate succinate and Eudragit® L100 polymers were used for the manufacture of isoniazid-loaded gastric-resistant sustained-release microspheres using an o/o solvent emulsification evaporation approach. Microporous floating sustained-release microspheres for the delivery of rifampicin in the stomach were manufactured using emulsification and a diffusion/evaporation process. The design of experiments was used to evaluate the impact of input variables on predefined responses or quality attributes of the microspheres. The percent degradation of rifampicin following 12 h dissolution testing in 0.1 M HCl pH 1.2 in the presence of isoniazid gastric-resistant sustained-release microspheres was only 4.44%. These results indicate that the degradation of rifampicin in the presence of isoniazid in acidic media can be reduced by encapsulation of both active pharmaceutical ingredients to ensure release in different segments of the gastrointestinal tract, potentially improving the bioavailability of rifampicin.

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Section: Responsesupporting

confidence: 80%

Section: Responsementioning

confidence: 99%

Section: Responsementioning

confidence: 99%

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Improved Stability of Rifampicin in the Presence of Gastric-Resistant Isoniazid Microspheres in Acidic Media

Mwila

Walker

2020

Pharmaceutics

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“…A strategy to increase the residence time of the drugs to overcome the above-mentioned drawbacks is necessary for optimal therapeutic outcomes. Numerous strategies have been used to increase the residence time of the dosage forms in the stomach, including mucoadhesive systems [8,9], high-density systems that sink to the bottom of the stomach [10], swelling systems [11] and floating systems [12][13][14]. Among these strategies, floating systems are considered superior as they do not interfere with the physiological activity of the gastrointestinal tract [15].…”

Section: Of 13mentioning

confidence: 99%

Novel Gastroretentive Floating Pulsatile Drug Delivery System Produced via Hot-Melt Extrusion and Fused Deposition Modeling 3D Printing

2020

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This study was performed to develop novel core-shell gastroretentive floating pulsatile drug delivery systems using a hot-melt extrusion-paired fused deposition modeling (FDM) 3D printing and direct compression method. Hydroxypropyl cellulose (HPC) and ethyl cellulose (EC)-based filaments were fabricated using hot-melt extrusion technology and were utilized as feedstock material for printing shells in FDM 3D printing. The directly compressed theophylline tablet was used as the core. The tablet shell to form pulsatile floating dosage forms with different geometries (shell thickness: 0.8, 1.2, 1.6, and 2.0 mm; wall thickness: 0, 0.8, and 1.6 mm; and % infill density: 50, 75, and 100) were designed, printed, and evaluated. All core-shell tablets floated without any lag time and exhibited good floating behavior throughout the dissolution study. The lag time for the pulsatile release of the drug was 30 min to 6 h. The proportion of ethyl cellulose in the filament composition had a significant (p < 0.05) effect on the lag time. The formulation (2 mm shell thickness, 1.6 mm wall thickness, 100% infill density, 0.5% EC) with the desired lag time of 6 h was selected as an optimized formulation. Thus, FDM 3D printing is a potential technique for the development of complex customized drug delivery systems for personalized pharmacotherapy.

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“…The dried microspheres were mounted on slab using carbon plate and subjected to acceleration voltage of 20 kv with secondary electron image to observe surface picture. 4…”

Section: Shape and Surface Morphologymentioning

confidence: 99%

Formulation Design and Pharmacodynamic evaluation of Alginate microspheres of Olanzepine.

Deshmukh¹,

Deshmukh²,

Deshmukh³

et al. 2018

JCPR

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In the present study, alginate based microspheres of Olanzepine was prepared by ionotropic external gelation technique utilizing calcium chloride as a cross linking agent to enhance bioavailability and residence time. The prepared microspheres are discrete, spherical and free flowing which was characterized by entrapment efficiency, particle size, in-vitro release behavior, scanning electron microscopy, in-vivo study etc; Optimized formulation was followed zero-order release kinetic. In-vivo evaluation of antidepressant activity of Olanzapine formulation showed that duration of immobility time was significantly decreased as compare to control and standard marked SR formulation. The optimized formulation was mucoadhesive in nature. Stability studies was carried out for F9 at a temperature of 40±2°C/ RH 75±5% formulation revealed that the drug behavior was within permissible limits.

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Development of Floating-Mucoadhesive Microsphere for Site Specific Release of Metronidazole

Cited by 21 publications

References 20 publications

Improved Stability of Rifampicin in the Presence of Gastric-Resistant Isoniazid Microspheres in Acidic Media

Improved Stability of Rifampicin in the Presence of Gastric-Resistant Isoniazid Microspheres in Acidic Media

Novel Gastroretentive Floating Pulsatile Drug Delivery System Produced via Hot-Melt Extrusion and Fused Deposition Modeling 3D Printing

Formulation Design and Pharmacodynamic evaluation of Alginate microspheres of Olanzepine.

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