Development and validation of a RP-HPLC method for Roflumilast and its degradation products

Pinheiro, Mariana Santos; Marins, Rita de Cássia Elias Estrela; Cabral, Lúcio Mendes; Sousa, Valéria Pereira de

doi:10.1080/10826076.2018.1436067

Cited by 7 publications

(1 citation statement)

References 10 publications

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“…Roflumilast is a medication that inhibits phosphodiesterase type 4 (PDE4). It is prescribed for the long-term management of chronic obstructive pulmonary disease and asthma [ 7 ]. Roflumilast is an anti-inflammatory medication known to participate in multiple inflammatory processes.…”

Section: Introductionmentioning

confidence: 99%

Development and Optimization of Dipyridamole- and Roflumilast-Loaded Nanoemulsion and Nanoemulgel for Enhanced Skin Permeation: Formulation, Characterization, and In Vitro Assessment

Maded,

Sfar,

Taqa

et al. 2024

Pharmaceuticals

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This study explores developing and optimizing a nanoemulsion (NE) system loaded with dipyridamole and roflumilast, aiming to improve skin penetration and retention. The NE formulation was further transformed into a nanoemulgel to enhance its application as a topical treatment for psoriasis. Solubility studies were conducted to select the oil, surfactant, and co-surfactant. Phase diagrams were constructed using the aqueous phase titration method. All the formulations were in nanoscale, and Formula (F2) (which contains oleic acid oil as the oil phase, a mixture of Surfactant Tween 80 and co-surfactant (ethanol) at a ratio of 1:2 in addition to distilled water as an aqueous phase in a ratio of 1:5:4, respectively) was the selected formula depending on the particle size, PDI, and zeta potential. Formula (F2) has the best ratio because it gives the smallest nanoemulsion globule size (particle size average of 167.1 nm), the best homogenicity (lowest PDI of 0.195), and the highest stability (higher zeta potential of −32.22). The selected formula was converted into a nanoemulgel by the addition of 0.5% (w/w) xanthan gum (average particle size of 172.7 nm) and the best homogenicity (lowest PDI of 0.121%) and highest stability (higher zeta potential of −28.31). In conclusion, the selected formula has accepted physical and chemical properties, which enhanced skin penetration.

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Section: Introductionmentioning

confidence: 99%

Development and Optimization of Dipyridamole- and Roflumilast-Loaded Nanoemulsion and Nanoemulgel for Enhanced Skin Permeation: Formulation, Characterization, and In Vitro Assessment

Maded,

Sfar,

Taqa

et al. 2024

Pharmaceuticals

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Integrative Validation Method of Roflumilast by Quantification and Detection in Lipid-Nanoparticles via Reverse Phase HPLC

et al. 2023

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Development of a new formulation of roflumilast for pulmonary drug delivery to treat inflammatory lung conditions

Suzuki

Amaro

Almeida

et al. 2018

International Journal of Pharmaceutics

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The aim of this study was to develop roflumilast dry powder inhaler (DPI) formulations by spray drying using hydroxypropyl-β-cyclodextrin (HPβCD) and to determine their suitability for pulmonary delivery. Different feed solution concentrations, solvent systems and spray drying parameters were used to obtain the formulations which were characterized using X-ray powder diffraction, thermal analysis, scanning electron microscopy, particle size distribution, bulk and tapped density, specific surface area, dynamic vapour sorption, in vitro deposition properties using a Next Generation Impactor (NGI) and transepithelial permeability. Microparticles spray dried from ethanol were wrinkled and amorphous, exhibiting high glass transition temperatures while those from methanol:n-butyl acetate consisted of irregularly shaped porous particles partially crystalline. All formulations presented low density, particle size and residual solvent content exhibiting high depositon in the lower stages of the NGI. Mass median aerodynamic diameters (MMADs) were in the range of 3.32-4.49 μm, with high fine particle fractions (FPF < 5 μm). Stability studies demonstrated no significant modifications in the solid-state nature and in the aerolisation performance of the selected formulation which presented a P of 8.73 × 10 ± 4.70 × 10 cm/s. The developed roflumilast DPI formulations have potential therapeutic applications in the treatment of lung diseases.

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Development and validation of a RP-HPLC method for Roflumilast and its degradation products

Cited by 7 publications

References 10 publications

Development and Optimization of Dipyridamole- and Roflumilast-Loaded Nanoemulsion and Nanoemulgel for Enhanced Skin Permeation: Formulation, Characterization, and In Vitro Assessment

Development and Optimization of Dipyridamole- and Roflumilast-Loaded Nanoemulsion and Nanoemulgel for Enhanced Skin Permeation: Formulation, Characterization, and In Vitro Assessment

Integrative Validation Method of Roflumilast by Quantification and Detection in Lipid-Nanoparticles via Reverse Phase HPLC

Development of a new formulation of roflumilast for pulmonary drug delivery to treat inflammatory lung conditions

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