Improvement in Dissolution of Bosentan Monohydrate by Solid Dispersions Using Spray Drying Technique

Dangre, Pankaj V.; Sormare, Vikesh B.; Godbole, Mangesh D.

doi:10.2174/1874844901704010023

Cited by 13 publications

(2 citation statements)

References 15 publications

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“…It is also not changed after spray drying process and there are no significant shifts in the positions of peaks. There are few variations in the intensity in at 1080 cm −1 (C–O stretching) and 1300 cm −1 (S=O stretching) [ 35 ], which is due to the crystallographic difference between amorphous SD formulations and typical crystalline BST monohydrate [ 36 ].…”

Section: Resultsmentioning

confidence: 99%

The Effect of Particle Size and Surface Roughness of Spray-Dried Bosentan Microparticles on Aerodynamic Performance for Dry Powder Inhalation

et al. 2020

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The purpose of this study was to prepare spray dried bosentan microparticles for dry powder inhaler and to characterize its physicochemical and aerodynamic properties. The microparticles were prepared from ethanol/water solutions containing bosentan using spray dryer. Three types of formulations (SD60, SD80, and SD100) depending on the various ethanol concentrations (60%, 80%, and 100%, respectively) were used. Bosentan microparticle formulations were characterized by scanning electron microscopy, powder X-ray diffraction, laser diffraction particle sizing, differential scanning calorimetry, Fourier-transform infrared spectroscopy, dissolution test, and in vitro aerodynamic performance using Andersen cascade impactor™ (ACI) system. In addition, particle image velocimetry (PIV) system was used for directly confirming the actual movement of the aerosolized particles. Bosentan microparticles resulted in formulations with various shapes, surface morphology, and particle size distributions. SD100 was a smooth surface with spherical morphology, SD80 was a rough surfaced with spherical morphology and SD60 was a rough surfaced with corrugated morphology. SD100, SD80, and SD60 showed significantly high drug release up to 1 h compared with raw bosentan. The aerodynamic size of SD80 and SD60 was 1.27 µm and SD100 was 6.95 µm. The microparticles with smaller particle size and a rough surface aerosolized better (%FPF: 63.07 ± 2.39 and 68.27 ± 8.99 for SD60 and SD80, respectively) than larger particle size and smooth surface microparticle (%FPF: 22.64 ± 11.50 for SD100).

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Section: Resultsmentioning

confidence: 99%

The Effect of Particle Size and Surface Roughness of Spray-Dried Bosentan Microparticles on Aerodynamic Performance for Dry Powder Inhalation

et al. 2020

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“…Spray drying has no solvent limitations and is most suitable for large-scale production [9]. Previously, SD of BM was made using hydroxypropyl β-cyclodextrin (HP β-CD) and polyethylene glycol (PEG) 4000 polymers, but BM in such SD retained its crystallinity, limiting its solubility [10].…”

Section: Introductionmentioning

confidence: 99%

Formulation, Development, and Evaluation of Bosentan Monohydrate Spray Dried- Solid Dispersion Tablets for Improved Dissolution Profile

Raut,

Hajare,

Chougale

et al. 2023

Jordan j. pharm. sci.

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Bosentan monohydrate (BM) is utilized for the treatment of pulmonary arterial hypertension, exhibiting poor aqueous solubility and bioavailability. This study aims to enhance the dissolution rate of the drug using Eudragit®EPO through spray drying. The drug and Eudragit®EPO were combined in ratios of 1:1, 1:2, 1:3, 1:4, and 1:5 (w/w) to generate compositions SD1 to SD5. SD5, at a 1:5 drug-to-carrier ratio, demonstrated a statistically significant increase in saturation solubility and drug content. Six tablet formulations (F1 to F6) containing SD5 and tableting excipients were developed and processed. Formulation F2, consisting of 26.36% HPMC K4M and 23.63% MCC, exhibited the highest dissolution and drug release. The probable mechanism underlying BM dissolution in SD involves its amorphous form and the solubilizing effect facilitated by hydrogen bonding between BM and Eudragit®EPO. The carrier's binding effect likely contributed to high tensile strength, low friability, and extended disintegration time. Direct mixing of SD with HPMC might have improved the uniformity of SD within the tablet matrix and the release profile. This study demonstrates the efficacy of spray drying in preparing SD of BM with Eudragit®EPO, potentially enhancing its solubility and stability.

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Preparation and characterization of bosentan monohydrate/ε‐polycaprolactone nanoparticles obtained by electrospraying

Giménez

Sperandeo

Faudone

et al. 2018

Biotechnology Progress

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The electrospraying technique provides nano and microparticles that can be used as drug delivery systems. The aims of this study were, firstly, to optimize the influent parameters of electrospraying for the manufacture of a Bosentan (BOS) nanoparticulate platform, and secondly, to evaluate its physicochemical properties and in vitro biopharmaceutical behavior. Particles were characterized by scanning electron microscopy (SEM), powder X‐ray diffraction (PXRD), differential scanning calorimetry (DSC), thermogravimetry (TG) and Fourier transformed Infrared spectroscopy (FTIR). Drug loading, encapsulation efficiency and kinetic dissolution were determined. Additionally, Bosentan release assays at 24 and 72 h were performed in vitro to evaluate biopharmaceutical properties of nano‐scaffolds by diffusion technique through dialysis bag. The nanostructures had heterogeneous sizes predominantly smaller than 550 nm and they were semicrystalline according to PXRD, indicating a partial amorphization of BOS during the encapsulation in the polymer matrix. FT‐IR and DSC showed an absence of chemical interactions between BOS and ε‐Polycaprolactone (PCL), suggesting that both components behaved as a physical mixture in these particles. The drug loading was 25.98%, and the encapsulation efficiency was 58.51%. Additionally, the release assays showed an extended and controlled release of BOS, in comparison to non‐encapsulated BOS. These data also showed to fit with the Cubic Root kinetic dissolution. As a conclusion, we demonstrate that the use of electrospraying for the manufacture of BOS (or similar drugs) controlled release nanoplatforms would represent an interesting contribution in the development of new therapeutic alternatives for the treatment of pathologies such as pulmonary hypertension and other related diseases. © 2018 American Institute of Chemical Engineers Biotechnol. Prog., 35: e2748, 2019.

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Improvement in Dissolution of Bosentan Monohydrate by Solid Dispersions Using Spray Drying Technique

Cited by 13 publications

References 15 publications

The Effect of Particle Size and Surface Roughness of Spray-Dried Bosentan Microparticles on Aerodynamic Performance for Dry Powder Inhalation

The Effect of Particle Size and Surface Roughness of Spray-Dried Bosentan Microparticles on Aerodynamic Performance for Dry Powder Inhalation

Formulation, Development, and Evaluation of Bosentan Monohydrate Spray Dried- Solid Dispersion Tablets for Improved Dissolution Profile

Preparation and characterization of bosentan monohydrate/ε‐polycaprolactone nanoparticles obtained by electrospraying

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