The Impact of Solid Dispersion on Formulation, Using Confocal Micro Raman Spectroscopy as Tool to Probe Distribution of Components

Melian, María Elisa; Munguía, A. Beatriz; Faccio, Ricardo; Palma, Santiago Daniel; Domínguez, Laura

doi:10.1007/s12247-017-9306-9

Cited by 18 publications

(11 citation statements)

References 26 publications

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“…Fen is a crystalline powder represented by two endothermic peaks, one at 244 °C (Δ H m = 252 J g −1 ) characteristic of the sample melting transition, followed by a second peak at 271 °C (Δ H m = 27 J g −1 ) representing its decomposition. Other studies have reported the same thermal profile for Fen, exhibiting the melting event followed by decomposition [ 14 , 15 , 20 ].…”

Section: Resultssupporting

confidence: 60%

Formulation and Evaluation of Fenbendazole Extended-Release Extrudes Processed by Hot-Melt Extrusion

Bezerra¹,

Lima²,

Colbert³

et al. 2022

Polymers

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This study aimed to demonstrate the feasibility of hot-melt extrusion in the development of extended-release formulations of Fenbendazole (Fen) dispersed in PEO/PCL blend-based matrices. Their thermal, physical, chemical and viscosity properties were assessed by differential scanning calorimetry, thermogravimetric analysis/derivative thermogravimetry, Fourier transform infrared spectroscopy, X-ray diffraction spectroscopy, and melt flow index. Drug dispersion was analyzed by scanning electron microscopy with electron dispersive X-ray spectroscopy, and drug release was evaluated by ultraviolet-visible spectroscopy. A thermal analysis indicated the conversion of the drug to its amorphous state. FTIR analysis endorsed the thermal studies pointing to a decrease in the drug’s crystallinity with the establishment of intermolecular interactions. XRD analysis confirmed the amorphous nature of Fen. MFI test revealed that PCL acts as a plasticizer when melt-processed with PEO. SEM images displayed irregular surfaces with voids and pores, while EDX spectra demonstrated a homogeneous drug distribution throughout the polymeric carrier. Dissolution testing revealed that PCL retards the drug release proportionally to the content of such polymer incorporated. These melt-extruded matrices showed that the drug release rate in a PEO/PCL blend can easily be tailored by altering the ratio of PCL to address the issues related to the multiple-dosing regimen of Fen in ruminants.

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Section: Resultssupporting

confidence: 60%

Formulation and Evaluation of Fenbendazole Extended-Release Extrudes Processed by Hot-Melt Extrusion

Bezerra¹,

Lima²,

Colbert³

et al. 2022

Polymers

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“…As indicated by the figure, the DSC of FBZ demonstrated a baseline shift at a glass transition temperature (Tg) of 190 °C. Moreover, an exothermic peak was observed at 222 °C, indicating its melting point, which is in agreement with the current literature [ 31 ]. However, FBZ did not demonstrate a melting peak in the DSC curves obtained from MCM-FBZ and PEG-MCM-FBZ NPs.…”

Section: Resultssupporting

confidence: 92%

PEGylated Mesoporous Silica Nanoparticles (MCM-41): A Promising Carrier for the Targeted Delivery of Fenbendazole into Prostrate Cancer Cells

et al. 2021

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Low water solubility and thus low bioavailability limit the clinical application of fenbendazole (FBZ) as a potential anticancer drug. Solubilizing agents, such as Mobil Composition of Matter Number 41 (MCM) as a drug carrier, can improve the water solubility of drugs. In this study, PEGylated MCM (PEG-MCM) nanoparticles (NPs) were synthesized and loaded with FBZ (PEG-MCM-FBZ) to improve its solubility and, as a result, its cytotoxicity effect against human prostate cancer PC-3 cells. The loading efficiency of FBZ onto PEG-MCM NPs was 17.2%. The size and zeta potential of PEG-MCM-FBZ NPs were 366.3 ± 6.9 nm and 24.7 ± 0.4 mV, respectively. They had a spherical shape and released the drug in a controlled manner at pH 1.2 and pH 6.2. PEG-MCM-FBZ were found to inhibit the migration of PC-3 cells, increase the cytotoxicity effects of FBZ against PC-3 cells by 3.8-fold, and were more potent by 1.4-fold, when compared to the non-PEGylated NPs. In addition, PEG-MCM-FBZ promoted the production of reactive oxygen species by 1.3- and 1.2-fold, respectively, when compared to FBZ and MCM-FBZ. Overall, the results demonstrate that PEG-MCM-FBZ NPs enhanced FBZ delivery to PC-3 cells; therefore, they have the potential to treat prostate cancer after a comprehensive in vivo study.

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“…Although potassium and sodium salts of the drug have been recently patented by Cirilli et al, no evidence of multicomponent crystalline forms with organic coformers or counterions has been reported. Instead, alternative strategies based on solid dispersions, , cyclodextrins, polymeric micelles, and nanocrystals have been adopted to modify the physicochemical profile of fenbendazole.…”

Section: Introductionmentioning

confidence: 99%

Pharmaceutical Salts of Fenbendazole with Organic Counterions: Structural Analysis and Solubility Performance

Surov

Vasilev

Vener

et al. 2021

Crystal Growth & Design

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In this work, three new pharmaceutical salts of fenbendazole (FNB), a benzimidazole-based anthelmintic drug, with sulfonic acids have been obtained and thoroughly investigated by different analytical techniques, including thermal methods, infrared/Raman spectroscopy, and theoretical methods (periodic DFT computations and Bader analyses of the crystalline electronic density). Single-crystal and high-resolution synchrotron powder X-ray diffraction data for the first time made it possible to determine the crystal structures of mesylate and tosylate salts of the drug, which were further validated by dispersion-corrected density functional theory calculations. All the solid forms were stabilized by a robust R2 2(8) supramolecular motif formed by relatively strong N–H···O hydrogen bonds. In the monohydrate of FNB tosylate, a considerable gain in the stabilization energy was due to the intermolecular interactions generated by the water molecules. A careful examination of the solubility–pH profile of the FNB salts revealed that, despite being thermodynamically unstable within the physiologically relevant pH range, the new solid forms demonstrated superior dissolution performance in terms of both the apparent solubility and the release rate in comparison to the parent drug. Since FNB has also been reported to possess anticancer activity, improving the drug’s poor physicochemical properties through salt formation with the selected sulfonic acids is expected to promote further investigations toward repurposing of this potent compound.

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The Impact of Solid Dispersion on Formulation, Using Confocal Micro Raman Spectroscopy as Tool to Probe Distribution of Components

Cited by 18 publications

References 26 publications

Formulation and Evaluation of Fenbendazole Extended-Release Extrudes Processed by Hot-Melt Extrusion

Formulation and Evaluation of Fenbendazole Extended-Release Extrudes Processed by Hot-Melt Extrusion

PEGylated Mesoporous Silica Nanoparticles (MCM-41): A Promising Carrier for the Targeted Delivery of Fenbendazole into Prostrate Cancer Cells

Pharmaceutical Salts of Fenbendazole with Organic Counterions: Structural Analysis and Solubility Performance

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