Manufacturing of Pharmaceuticals by Impregnation of an Active Pharmaceutical Ingredient onto a Mesoporous Carrier: Impact of Solvent and Loading

Omar, Thamer A.; Oka, Sarang; Muzzio, Fernando J.; Glasser, Benjamin J.

doi:10.1007/s12247-018-9349-6

Cited by 3 publications

(2 citation statements)

References 33 publications

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“…Recently reported approaches for encapsulating drug molecules in MOFs have usually involved incubation with a solvent, one-step solution-based reaction processes, or mechanochemistry techniques, such as grinding or ball-milling strategies . However, these methods are hampered by the necessity of removing the solvent and the tendency of simple mechanical processes to destroy the macromorphology of the MOFs.…”

Section: Introductionmentioning

confidence: 99%

Diffusion Kinetics-Based Loading of Lipoic Acid into Cyclodextrin Metal–Organic Frameworks via a Solvent-Free Method and Mechanism of Stability Enhancement

Yang

Zhou

et al. 2023

J. Phys. Chem. C

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It is difficult to accurately distinguish the amount of a drug inside versus outside of a carrier during drug loading, which limits the ability to determine the kinetic data (the drug diffusion coefficient, energy barrier, etc.). Here, we demonstrated the feasibility of determining the drug diffusion coefficient and content without distinguishing whether it is inside or outside of a carrier. Specifically, the sample of gamma-cyclodextrin metal−organic frameworks (CD-MOF) loaded with unstable and viscous alphalipoic acid (LA) was examined. Furthermore, the LA stability was enhanced by the CD-MOF via a straightforward and unambiguous solvent-free method, and the mechanism behind it was thoroughly explored based on the diffusion coefficient. For the first time, a combination of mathematical modeling and new experimental measurements was used to determine the diffusion coefficient of LA in CD-MOF crystals. Accordingly, the strong adhesion free energy (−8.64 ± 0.56 kcal•mol −1 ) between LA and the dicyclodextrin cavity in the CD-MOF was determined. Furthermore, the nature of the adhesion force was identified to be the chemisorption dominated by hydrogen binding employing a combination of molecular modeling (docking and density functional theory, DFT) and experimental methods (solid-state nuclear magnetic resonance, ssNMR). Finally, this study revealed that the stability enhancement of LA in the CD-MOF is due to the combined actions of the high binding free energy of LA with the dicyclodextrin cavity and its steric hindrance, together with the accelerating roles of the CD-MOF cage environment.

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Section: Introductionmentioning

confidence: 99%

Diffusion Kinetics-Based Loading of Lipoic Acid into Cyclodextrin Metal–Organic Frameworks via a Solvent-Free Method and Mechanism of Stability Enhancement

Yang

Zhou

et al. 2023

J. Phys. Chem. C

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“…The high porosity and large specific surface area give Neusilin ® significant adsorption capacity [ 33 ]. With respect to this, Neusilin ® is an excellent carrier for solid drug delivery systems and hot-melt extrusion [ 34 , 35 , 36 , 37 , 38 , 39 ]. Moreover, it is known for its ability to improve powder flow properties [ 33 , 40 , 41 , 42 ].…”

Section: Introductionmentioning

confidence: 99%

Stress-Dependent Particle Interactions of Magnesium Aluminometasilicates as Their Performance Factor in Powder Flow and Compaction Applications

2021

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In the pharmaceutical industry, silicates are commonly used excipients with different application possibilities. They are especially utilized as glidants in low concentrations, but they can be used in high concentrations as porous carriers and coating materials in oral solid drug delivery systems. The desirable formulations of such systems must exhibit good powder flow but also good compactibility, which brings opposing requirements on inter-particle interactions. Since magnesium aluminometasilicates (MAS) are known for their interesting flow behavior reported as “negative cohesivity” yet they can be used as binders for tablet compression, the objective of this experimental study was to investigate their particle interactions within a broad range of mechanical stress from several kPa to hundreds of MPa. Magnesium aluminometasilicate (Neusilin® US2 and Neusilin® S2)-microcrystalline cellulose (Avicel® PH102) physical powder mixtures with varying silicate concentrations were prepared and examined during their exposure to different pressures using powder rheology and compaction analysis. The results revealed that MAS particles retain their repulsive character and small contact surface area under normal conditions. If threshold pressure is applied, the destruction of MAS particles and formation of new surfaces leading to particle interactions are observed. The ability of MAS particles to form interactions intensifies with increasing pressure and their amount in a mixture. This “function switching” makes MAS suitable for use as multifunctional excipients since they can act as a glidant or a binder depending on the applied pressure.

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Solvent-Free Loading of Vitamin A Palmitate into β-Cyclodextrin Metal-Organic Frameworks for Stability Enhancement

Zhang,

Chen,

Zhang

et al. 2023

AAPS PharmSciTech

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Manufacturing of Pharmaceuticals by Impregnation of an Active Pharmaceutical Ingredient onto a Mesoporous Carrier: Impact of Solvent and Loading

Cited by 3 publications

References 33 publications

Diffusion Kinetics-Based Loading of Lipoic Acid into Cyclodextrin Metal–Organic Frameworks via a Solvent-Free Method and Mechanism of Stability Enhancement

Diffusion Kinetics-Based Loading of Lipoic Acid into Cyclodextrin Metal–Organic Frameworks via a Solvent-Free Method and Mechanism of Stability Enhancement

Stress-Dependent Particle Interactions of Magnesium Aluminometasilicates as Their Performance Factor in Powder Flow and Compaction Applications

Solvent-Free Loading of Vitamin A Palmitate into β-Cyclodextrin Metal-Organic Frameworks for Stability Enhancement

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