Ternary solid dispersions: classification and formulation considerations

Borde, Shambhavi; Paul, Sagar Kumar; Chauhan, Harsh

doi:10.1080/03639045.2021.1908342

Cited by 20 publications

(12 citation statements)

References 145 publications

(6 reference statements)

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“…However, due to a lack of solubility of itraconazole in PVA in solid state, the dissolution of the corresponding ASD did not lead to supersaturation of itraconazole ( Wlodarski et al, 2018 ). Previous investigations on ternary systems with a combination of two polymers showed superior dissolution profiles by enhancing the initial dissolution rate and the supersaturation stabilization ( Baghel et al, 2018b ; Borde et al, 2021 ; Kapote and Wagner, 2021 ; Van Ngo et al, 2016 ; Zecevic et al, 2014 ). Such ternary systems can be obtained by using the supersaturation generating polymer as ASD-carrier for the drug and adding a further, supersaturating stabilizing polymer to the binary ASD formulation as an external phase.…”

Section: Introductionmentioning

confidence: 96%

Boost of solubility and supersaturation of celecoxib via synergistic interactions of methacrylic acid-ethyl acrylate copolymer (1:1) and hydroxypropyl cellulose in ternary amorphous solid dispersions

Pöstges

Kayser

Stoyanov³

et al. 2022

International Journal of Pharmaceutics: X

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Section: Introductionmentioning

confidence: 96%

Boost of solubility and supersaturation of celecoxib via synergistic interactions of methacrylic acid-ethyl acrylate copolymer (1:1) and hydroxypropyl cellulose in ternary amorphous solid dispersions

Pöstges

Kayser

Stoyanov³

et al. 2022

International Journal of Pharmaceutics: X

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“…In addition, when the concentration of surfactant is higher than the critical micelle concentration (CMC), the solubility of the drug is increased due to solubilization [ 14 ]. Most studies have demonstrated that these ternary systems could enhance the solubility and oral absorption of poorly water-soluble drugs [ 15 ]. Meng et al reported that TPGS increased the dissolution rate and supersaturation of celecoxib ASDs consisting of celecoxib (20%), PVPVA, and TPGS at 20% level [ 16 ].…”

Section: Introductionmentioning

confidence: 99%

Effect of Span 20 Feeding Zone in the Twin Screw Extruder on the Properties of Amorphous Solid Dispersion of Ritonavir

Wang

Zhao

et al. 2023

Pharmaceutics

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A ternary amorphous solid dispersion (ASD) system consisting of drug/polymer/surfactant is receiving increased attention to improve the oral bioavailability of poorly water-soluble drugs. The effect of polymers has been extensively studied, while the impact of surfactants has not yet to be studied to the same extent. Challenging questions to be answered are whether the surfactants should be added with the drug or separately and the resulting differences between the two operating processes. By adjusting the liquid feeding zone for Span 20 in the hot-melt twin screw extruder equipment, we investigated the effect of Span 20 on the properties of the polyvinylpyrrolidone/vinyl acetate (PVPVA)-based ASD formulations of ritonavir. We found that with the delayed feeding positions of Span 20 in the twin screw extruder, the ability of the ternary ASDs to maintain the supersaturation of the milled extrudates was observed to be significantly enhanced. Furthermore, adding surfactant after a thorough mixing of polymer and drug could decrease the molecular mobility of ternary ASD formulations. In addition, the effects of Span 20 on the complex viscosity and structure of PVPVA were also investigated. The delayed addition of Span 20 could improve the complex viscosity of PVPVA, thus leading to the drug precipitation inhibition. In conclusion, the delayed addition of Span 20 in the twin screw extruder and prolonging the mixing time of the drug and polymer may be critical to the maintenance of supersaturation.

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“…Such polymers often have a hygroscopic character, possibly causing significant changes in physicochemical properties such as particle size, solubility, dissolution properties, and crystallinity during the storage period [ 3 , 8 , 9 ]. For further improvement of their performance in terms of storage stability and processability, a recent advancement of the SD approach is to design ternary solid dispersions (tSD) [ 10 ]. Along with the drug and single carrier material for the conventional binary system, there are other components of the tSD system like a second polymer, surfactant, and excipients, and the addition of a third component can functionalize the SD system depending on the physicochemical characteristics of that component, including the prevention of precipitation, improvement of storage stability, and controlled release of included drugs in addition to solubility enhancement [ 11 , 12 , 13 , 14 ].…”

Section: Introductionmentioning

confidence: 99%

Cyclosporine A-Loaded Ternary Solid Dispersion Prepared with Fine Droplet Drying Process for Improvement of Storage Stability and Oral Bioavailability

et al. 2023

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This study aimed to develop a cyclosporine A (CsA)-loaded ternary solid dispersion (tSD/CsA) to improve the storage stability of a solid dispersion (SD) system and the oral absorbability of CsA. Hydroxypropyl cellulose (HPC) and hydroxypropyl methylcellulose acetate succinate (HPMCAS) were selected as carrier materials of tSD, and tSD/CsA was prepared with a fine droplet drying process, a powderization technology that employs an inkjet head. The physicochemical properties of tSD/CsA were evaluated in terms of morphology, storage stability, dissolution behavior, and mucoadhesive property. After the oral administration of CsA samples (10 mg-CsA/kg) to rats, the plasma concentration of CsA was monitored to estimate oral absorbability. tSD/CsA comprised uniform shriveled particles with a diameter of 3.4 mm and span factor of 0.4, which is a parameter to estimate the particle size distribution. Although HPC-based binary SD showed marked aggregation of the particles after storage under 40 °C/75% relative humidity, there were no significant aggregations of tSD/CsA, due to the relatively low hygroscopic property of HPMCAS. The pH-dependent release of CsA with improved dissolution was observed in tSD/CsA. In the in vitro mucoadhesive evaluation using a mucin disk, tSD/CsA exhibited a better mucoadhesive property than HPC-based SD, possibly leading to prolonged retention of tSD particles in the gastrointestinal tract after oral administration. Orally-dosed tSD/CsA in rats resulted in significantly improved oral absorption of CsA, as evidenced by a 27-fold higher bioavailability than amorphous CsA. tSD/CsA may be a promising dosage option to improve the storage stability of a SD system and the biopharmaceutical properties of CsA.

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Ternary solid dispersions: classification and formulation considerations

Cited by 20 publications

References 145 publications

Boost of solubility and supersaturation of celecoxib via synergistic interactions of methacrylic acid-ethyl acrylate copolymer (1:1) and hydroxypropyl cellulose in ternary amorphous solid dispersions

Boost of solubility and supersaturation of celecoxib via synergistic interactions of methacrylic acid-ethyl acrylate copolymer (1:1) and hydroxypropyl cellulose in ternary amorphous solid dispersions

Effect of Span 20 Feeding Zone in the Twin Screw Extruder on the Properties of Amorphous Solid Dispersion of Ritonavir

Cyclosporine A-Loaded Ternary Solid Dispersion Prepared with Fine Droplet Drying Process for Improvement of Storage Stability and Oral Bioavailability

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