An Investigation into the Use of Mesoporous Silica for Improving Physical Stability of Amorphous Solid Dispersion with High Drug Loading

2021 ◽  
Author(s):  
Fahad Alqahtani ◽  
Peter Belton ◽  
Sheng Qi
Author(s):  
Bhianca Lins de Azevedo Costa ◽  
Martial Sauceau ◽  
Romain Sescousse ◽  
Maria Ines Re

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.


Molecules ◽  
2021 ◽  
Vol 26 (15) ◽  
pp. 4492
Author(s):  
Eric Ofosu Kissi ◽  
Robin Nilsson ◽  
Liebert Parreiras Nogueira ◽  
Anette Larsson ◽  
Ingunn Tho

Fused deposition modelling-based 3D printing of pharmaceutical products is facing challenges like brittleness and printability of the drug-loaded hot-melt extruded filament feedstock and stabilization of the solid-state form of the drug in the final product. The aim of this study was to investigate the influence of the drug load on printability and physical stability. The poor glass former naproxen (NAP) was hot-melt extruded with Kollidon® VA 64 at 10–30% w/w drug load. The extrudates (filaments) were characterised using differential scanning calorimetry (DSC), dynamic mechanical analysis (DMA), and thermogravimetric analysis (TGA). It was confirmed that an amorphous solid dispersion was formed. A temperature profile was developed based on the results from TGA, DSC, and DMA and temperatures used for 3D printing were selected from the profile. The 3D-printed tablets were characterised using DSC, X-ray computer microtomography (XµCT), and X-ray powder diffraction (XRPD). From the DSC and XRPD analysis, it was found that the drug in the 3D-printed tablets (20 and 30% NAP) was amorphous and remained amorphous after 23 weeks of storage (room temperature (RT), 37% relative humidity (RH)). This shows that adjusting the drug ratio can modulate the brittleness and improve printability without compromising the physical stability of the amorphous solid dispersion.


RSC Advances ◽  
2019 ◽  
Vol 9 (61) ◽  
pp. 35566-35578 ◽  
Author(s):  
Subhankar Mukhopadhyay ◽  
Hanitrarimalala Veroniaina ◽  
Tadious Chimombe ◽  
Lidong Han ◽  
Wu Zhenghong ◽  
...  

Protean mesoporous silica nanoparticles are propitious candidates over decades for nanoscale drug delivery systems due to their unique characteristics, including changeable pore size, mesoporosity, high drug loading capacity and biodegradability.


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