Preparation of a ternary amorphous solid dispersion using hot-melt extrusion for obtaining a stable colloidal dispersion of amorphous probucol nanoparticles

Hanada, Naho; Higashi, Kenjirou; Zhao, Zhijie; Ueda, Keisuke; Moribe, Kunikazu

doi:10.1016/j.ijpharm.2023.122959

Cited by 6 publications

(7 citation statements)

References 46 publications

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“…Hanada et al (2023) reported that PXRD data confirming the amorphous form of probucol (PBC) in the ternary hot-melt extrusion (HME) were validated by solid-state NMR spectroscopy, as shown in Figure 4 [ 101 ]. The peaks of the aromatic ring carbon of PBC and PVP were found in the solid-state 13 C NMR spectra of PBC in 115–160 and 170–182 ppm areas [ 102 , 103 ].…”

Section: Characterization Of Ternary Solid Dispersion In the Solid Statementioning

confidence: 99%

“…The absolute value of the amorphous PBC nanoparticles (−11.6 mV) was lower than the result reported for PBC particles (−41.0 mV), indicating the adsorption of P407. The steric repulsion of the P407 coating on the particle interface resulted in the strong dispersion stability of the amorphous PBC nanoparticles [ 101 ]. Pardhi, et al (2021) also reported that the monodispersed particles of the TSD system with an average zeta potential distribution of 23.1 mV were observed, indicating good stability in the dispersed state.…”

Section: Characterization Of Ternary Solid Dispersion After Being Dis...mentioning

confidence: 99%

“…The U-shaped structure created by the molecules covering the particle interface increased the colloidal nanoparticles’ storage durability by preventing drug crystallization and particle agglomeration. The inclusion of additional molecules within the nanoparticles played a crucial role in stabilizing the amorphous form of the drug during storage through the reduction in the thermodynamic activity of the supercooled liquid drug [ 101 ]. Therefore, the preparation of a ternary solid dispersion by applying hot-melt extrusion can form a stable amorphous drug after being dispersed in the water.…”

Section: Mechanism Drug Release Of Ternary Solid Dispersion Systemsmentioning

confidence: 99%

Section: Figurementioning

confidence: 99%

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Ternary Solid Dispersions: A Review of the Preparation, Characterization, Mechanism of Drug Release, and Physical Stability

Budiman,

Lailasari,

Nurani

et al. 2023

Pharmaceutics

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The prevalence of active pharmaceutical ingredients (APIs) with low water solubility has experienced a significant increase in recent years. These APIs present challenges in formulation, particularly for oral dosage forms, despite their considerable therapeutic potential. Therefore, the improvement of solubility has become a major concern for pharmaceutical enterprises to increase the bioavailability of APIs. A promising formulation approach that can effectively improve the dissolution profile and the bioavailability of poorly water-soluble drugs is the utilization of amorphous systems. Numerous formulation methods have been developed to enhance poorly water-soluble drugs through amorphization systems, including co-amorphous formulations, amorphous solid dispersions (ASDs), and the use of mesoporous silica as a carrier. Furthermore, the successful enhancement of certain drugs with poor aqueous solubility through amorphization has led to their incorporation into various commercially available preparations, such as ASDs, where the crystalline structure of APIs is transformed into an amorphous state within a hydrophilic matrix. A novel approach, known as ternary solid dispersions (TSDs), has emerged to address the solubility and bioavailability challenges associated with amorphous drugs. Meanwhile, the introduction of a third component in the ASD and co-amorphous systems has demonstrated the potential to improve performance in terms of solubility, physical stability, and processability. This comprehensive review discusses the preparation and characterization of poorly water-soluble drugs in ternary solid dispersions and their mechanisms of drug release and physical stability.

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Section: Characterization Of Ternary Solid Dispersion In the Solid Statementioning

confidence: 99%

Section: Characterization Of Ternary Solid Dispersion After Being Dis...mentioning

confidence: 99%

Section: Mechanism Drug Release Of Ternary Solid Dispersion Systemsmentioning

confidence: 99%

Section: Figurementioning

confidence: 99%

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Ternary Solid Dispersions: A Review of the Preparation, Characterization, Mechanism of Drug Release, and Physical Stability

Budiman,

Lailasari,

Nurani

et al. 2023

Pharmaceutics

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“…An essential line of research in the future would be precisely the assessment of the role of PU for secondary prevention of cerebral infarction with a high risk of a cerebral hemorrhage in lacunar versus nonlacunar ischemic stroke,[ 37 38 39 40 41 ] because the pathophysiology, prognosis, and clinical features of lacunar strokes are different from other acute cerebrovascular diseases.…”

Section: Problems and Perspectivesmentioning

confidence: 99%

Probucol will become a new model for treating cerebral infarction with a high risk of hemorrhage: A narrative review

Lang,

Zhang,

Zheng

et al. 2023

Brain Circulation

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Lipid-lowering agents are relevant in stroke prevention. Probucol (PU) is an antioxidative and lipid-lowering drug that has been used to treat atherosclerotic cardiovascular diseases and xanthomas. The drug penetrates the core of low-density lipoprotein cholesterol (LDL-C) particles, enhancing the activity of plasma cholesterol l ester transfer protein (CETP) and strengthening the liver scavenger receptor type I, resulting in reducing LDL-C; by increasing the activity of paraoxonase 1, upregulating the antioxidant function of high-density lipoprotein (HDL), and it decreases the serum HDL-cholesterol (HDL-C) level. This drug has been retired from the Western markets for lowering HDL-C levels and Q-interval prolongation. The latter side effect has been rarely reported and may be transient. Recent clinical evidence supports the effectiveness of PU in preventing cardiovascular events and in reducing mortality, irrespective of the reduction of HDL-C. Based on basic research and clinical studies, it appears that PU might be a valuable alternative when statins are ineffective or contraindicated, in patients at high risk of recurrence of cerebral ischemia and hemorrhage.

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Supersaturable diacyl phospholipid dispersion for improving oral bioavailability of brick dust molecule: A case study of Aprepitant

Lale,

Sirvi,

Debaje

et al. 2024

European Journal of Pharmaceutics and Biopharmaceutics

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Preparation of a ternary amorphous solid dispersion using hot-melt extrusion for obtaining a stable colloidal dispersion of amorphous probucol nanoparticles

Cited by 6 publications

References 46 publications

Ternary Solid Dispersions: A Review of the Preparation, Characterization, Mechanism of Drug Release, and Physical Stability

Ternary Solid Dispersions: A Review of the Preparation, Characterization, Mechanism of Drug Release, and Physical Stability

Probucol will become a new model for treating cerebral infarction with a high risk of hemorrhage: A narrative review

Supersaturable diacyl phospholipid dispersion for improving oral bioavailability of brick dust molecule: A case study of Aprepitant

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