High-Drug-Loading Amorphous Solid Dispersions via In Situ Thermal Cross-Linking: Unraveling the Mechanisms of Stabilization

2021 ◽  
Author(s):  
Afroditi Kapourani ◽  
Eleftherios G. Andriotis ◽  
Konstantina Chachlioutaki ◽  
Konstantinos N. Kontogiannopoulos ◽  
Panagiotis A. Klonos ◽  
...  
Keyword(s):  
Drug Loading ◽  
Solid Dispersions ◽  
Amorphous Solid ◽  
Cross Linking ◽  
Amorphous Solid Dispersions ◽  
High Drug ◽  
High Drug Loading

scholarly journals Generation of high drug loading amorphous solid dispersions by Spray Drying

2018 ◽  
Author(s):  
Bhianca Lins de Azevedo Costa ◽  
Martial Sauceau ◽  
Romain Sescousse ◽  
Maria Ines Re
Keyword(s):  
Spray Drying ◽  
Drug Carrier ◽  
Drug Loading ◽  
Solid Dispersions ◽  
Amorphous Solid ◽  
Amorphous Solid Dispersion ◽  
Drug Solubility ◽  
Amorphous Solid Dispersions ◽  
High Drug ◽  
High Drug Loading

Amorphous solid dispersions (ASDs) refers to drug - carrier systems, where the drug is dispersed in the carrier at a molecular level. In this work, ASDs were formulated by spray drying. The aim was to achieve high drug loads of an amorphous hydrophobic drug (Efavirenz - EFV) in  the  carrier Soluplus®. Solid state characterizations (mDSC, XRPD, DVS, Raman, SEM, stability and solubility studies) were done. EFV amorphisation in ASDs (20 to 85% EFV loads) resulted in improved drug solubility compared to unprocessed EFV crystals and tendency of properties evolution over time for ASDs with EFV loads  higher than 70 wt%. Keywords: amorphous solid dispersion, spray drying, high drug loading, soluplus, efavirenz.

scholarly journals Development of a Surface Coating Technique with Predictive Value for Bead Coating in the Manufacturing of Amorphous Solid Dispersions

Pharmaceutics ◽  
2020 ◽  
Vol 12 (9) ◽  
pp. 878
Author(s):  
Eline Boel ◽  
Piyush Panini ◽  
Guy Van den Mooter
Keyword(s):  
Phase Behavior ◽  
Spray Drying ◽  
Surface Coating ◽  
Drug Loading ◽  
Solid Dispersions ◽  
Amorphous Solid ◽  
Film Casting ◽  
Amorphous Solid Dispersions ◽  
Coating Technique ◽  
Amorphous System

The aim of this paper was to investigate whether a surface coating technique could be developed that can predict the phase behavior of amorphous solid dispersions (ASDs) coated on beads. ASDs of miconazole (MIC) and poly(vinylpyrrolidone-co-vinyl acetate) (PVP-VA) in methanol (MeOH) were studied as a model system. First, the low crystallization tendency of the model drug in MeOH was evaluated and confirmed. In a next step, a drug loading screening was performed on casted films and coated beads in order to define the highest possible MIC loading that still results in a one-phase amorphous system. These results indicate that film casting is not suitable for phase behavior predictions of ASDs coated on beads. Therefore, a setup for coating a solid surface was established inside the drying chamber of a spray dryer and it was found that this surface coating technique could predict the phase behavior of MIC-PVP-VA systems coated on beads, in case an intermittent spraying procedure is applied. Finally, spray drying was also evaluated for its ability to manufacture high drug-loaded ASDs. The highest possible drug loadings that still result in a one-phase amorphous system were obtained for bead coating and its predictive intermittent surface coating technique, followed by spray drying and finally by film casting and the continuous surface coating technique, thereby underlining the importance for further research into the underexplored bead coating process.

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