Optimization of Spray-Drying Parameters for Formulation Development at Preclinical Scale

Nespi, Marika; Kuhn, Robert J.; Yen, Chun-Wan; Lubach, Joseph W.; Leung, Dennis

doi:10.1208/s12249-021-02160-1

Cited by 7 publications

(1 citation statement)

References 40 publications

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“…This might be because the porous mannitol structure prepared with PVP K30 as the template is not smooth, causing the formation of mechanical chimeric particles, resulting in poor flowability of the powder. Secondly, the particle size obtained by the Buchi B-290 laboratory-grade spray-dryer is generally within the range of 1~10 µm [48], and the powder has strong electrostatic and van der Waals forces in the particle size stage, resulting in poor overall flowability of the powder.…”

Section: Porous Mannitol Before Drug Loadingmentioning

confidence: 99%

The Fabrication, Drug Loading, and Release Behavior of Porous Mannitol

Li,

Luo,

et al. 2024

Molecules

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Porous materials are widely used as an effective strategy for the solubilization of insoluble drugs. In order to improve the solubility and bioavailability of low water-solubility drugs, it is necessary to prepare porous materials. Mannitol is one of the most popular excipients in food and drug formulations. In this study, porous mannitol was investigated as a drug carrier for low water solubility drugs. Its fabrication, drug loading, and drug release mechanisms were investigated. Porous mannitol was fabricated using the co-spray–antisolvent process and utilizing polyvinylpyrrolidone K30 (PVP K30) as the template agent. Porous mannitol particles were prepared by changing the proportion of the template agent, spraying the particles with mannitol, and eluting with ethanol in order to regulate their pore structure. In subsequent studies, porous mannitol morphology and characteristics were determined systematically. Furthermore, curcumin and ibuprofen, two poorly water-soluble drugs, were loaded into porous mannitol, and their release profiles were analyzed. The results of the study indicated that porous mannitol can be prepared using PVP K30 as a template and that the amount of template agent can be adjusted in order to control the structure of the porous mannitol. When the template agent was added in amounts of 1%, 3%, and 5%, the mannitol pore size increased by 167.80%, 95.16%, and 163.98%, respectively, compared to raw mannitol. Molecular docking revealed that mannitol and drugs are adsorbents and adhere to each other by force interaction. The cumulative dissolution of curcumin and ibuprofen-loaded porous mannitol reached 69% and 70%, respectively. The release mechanism of curcumin and ibuprofen from drug-loaded mannitol was suitable for the Korsmeyer–Peppas kinetic model. In summary, the co-spray–antisolvent method proved effective in fabricating porous materials rapidly, and porous mannitol had a remarkable effect on drug solubilization. The results obtained are conducive to the development of porous materials.

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Section: Porous Mannitol Before Drug Loadingmentioning

confidence: 99%