Downstream drug product processing of itraconazole nanosuspension: Factors influencing tablet material properties and dissolution of compacted nanosuspension-layered sugar beads

Tan, En Hui; Parmentier, Johannes; Low, Ariana; Möschwitzer, Jan P.

doi:10.1016/j.ijpharm.2017.08.107

Cited by 12 publications

(5 citation statements)

References 24 publications

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“…This difference could potentially be attributed to CA's ability to inhibit drug crystallization within supersaturated solutions [34]. Although the excipients present in pellets have also been reported to possess crystallization inhibition effects [35,36], our study demonstrates that cholic acid exhibits superior efficacy. Notably, the dissolution percentage of ITZ at a pH of 6.8 was higher in FaSSIF than in PBS.…”

Section: In Vitro Dissolution Under Supersaturating Conditionsmentioning

confidence: 68%

The Increased Dissolution and Oral Absorption of Itraconazole by Nanocrystals with an Endogenous Small-Molecule Surfactant as a Stabilizer

Chang,

Yang,

Liu

et al. 2024

Molecules

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The aim of this study was to develop cholic-acid-stabilized itraconazole nanosuspensions (ITZ-Nanos) with the objective of enhancing drug dissolution and oral absorption. A laboratory-scale microprecipitation–high-pressure homogenization method was employed for the preparation of the ITZ-Nanos, while dynamic light scattering, transmission electron microscope analysis, X-ray diffraction, differential scanning calorimetry, and high-performance liquid chromatography analysis were utilized to evaluate their physicochemical properties. The absorption and bioavailability of the ITZ-Nanos were assessed using Caco-2 cells and rats, with Sporanox® pellets as a comparison. Prior to lyophilization, the particle size of the ITZ-Nanos measured approximately 225.7 nm. Both X-ray diffraction and differential scanning calorimetry confirmed that the ITZ remained crystalline within the nanocrystals. Compared to the pellets, the ITZ-Nanos exhibited significantly higher levels of supersaturation dissolution and demonstrated enhanced drug uptake by the Caco-2 cells. The AUC(0–t) value for the ITZ-Nanos in rats was 1.33-fold higher than that observed for the pellets. These findings suggest that cholic acid holds promise as a stabilizer for ITZ nanocrystals, as well as potentially other nanocrystals.

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Section: In Vitro Dissolution Under Supersaturating Conditionsmentioning

confidence: 68%

The Increased Dissolution and Oral Absorption of Itraconazole by Nanocrystals with an Endogenous Small-Molecule Surfactant as a Stabilizer

Chang,

Yang,

Liu

et al. 2024

Molecules

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“…84,101−103 These teams have developed itraconazole nanoformulations by compact nanosuspension-layered sugar beads (blending with excipients, i.e., HPMC, MCC, copovidone or isomalt, crospovidone-PEG 4000, dibasic calcium phosphate, and HPC) and evaluated factors influencing particle size, tablet properties, and dissolution profiles. 84,101 Another itraconazole nanosuspension was formulated into a tablet formulation for direct compression to improve micrometric properties such as flowability and compressibility. 85 A doxazosin mesylate fast-disintegrating tablet formulation was developed by applying contour plots of nanosuspension that were made using PVP k-30, poloxamer 407 (POX 407), and SDS.…”

Section: Nanoparticle-based Tablets a Tablet Incorporating Gold Nanop...mentioning

confidence: 99%

“…However, it is apparent that both nanosuspension formulations exhibited similar hardness, disintegration time, and friability properties. Itraconazole nanosuspensions were widely reported for tablet preparation. ,− These teams have developed itraconazole nanoformulations by compact nanosuspension-layered sugar beads (blending with excipients, i.e., HPMC, MCC, copovidone or isomalt, crospovidone-PEG 4000, dibasic calcium phosphate, and HPC) and evaluated factors influencing particle size, tablet properties, and dissolution profiles. , Another itraconazole nanosuspension was formulated into a tablet formulation for direct compression to improve micrometric properties such as flowability and compressibility …”

Section: Role Of Nanocarriers In Tabletized Nanomedicinementioning

confidence: 99%

Tabletized Nanomedicine: From the Current Scenario to Developing Future Medicine

Tiwari,

Kolli,

Chauhan

et al. 2024

ACS Nano

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The limitations of conventional therapeutic treatments prevailed in the development of nanotechnology-based medical formulations, termed nanomedicine. Nanomedicine is an advanced medicine that often consists of therapeutic agent(s) embedded in biodegradable or biocompatible nanomaterial-based formulations. Among nanomedicine approaches, tablet (oral) nanomedicine is still under development. In tabletized nanomedicine, the dynamic interplay between nanoformulations and the intricate milieu of the gastrointestinal tract simulates a pivotal role, particularly accentuating the influence exerted upon the luminal, mucosal, and epithelial cells. In this work, we document the perspectives and opportunities of nanoformulations toward the development of tabletized nanomedicine. This review also unveils the notion of integrating nanomedicine within a tablet formulation, which facilitates the controlled release of drugs, biomolecules, and agent(s) from the formulation to achieve a better therapeutic response. Finally, an attempt was made to explore current trends in nanomedicine technology such as bacteriophage, probiotic, and oligonucleotide tabletized nanomedicine and the combination of nanomedicine with imaging agents, i.e., nanotheranostics.

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“…However, an experimental study comparing vacuum drum drying with spray drying as a commonly used drying technique for crystalline nanosuspensions and exploring benefits and distinctions of each technique is missing. In the literature, several studies investigated the manufacturability and dissolution of nanocrystalline-based tablets [ 26 , 29 ]. However, the specific impact of the compaction pressure on the redispersibility of a solidified nanocrystalline intermediate addressing even a mechanistic understanding by considering tablets with tensile strengths higher than usually targeted was not reported.…”

Section: Introductionmentioning

confidence: 99%

Transformation of ABT-199 Nanocrystal Suspensions into a Redispersible Drug Product—Impact of Vacuum Drum Drying, Spray Drying and Tableting on Re-Nanodispersibility

Schönfeld,

Sundermann,

Keller

et al. 2024

Pharmaceutics

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The present study compared vacuum drum drying (VDD) and conventional spray drying (SD) for solidifying crystalline ABT-199 nanosuspensions into redispersible oral drug products. The aim was to optimize formulation compositions and process conditions to maintain nanoparticle size after tablet redispersion. The impact of drug load (22%, 33%, 44%) and type of drying protectant (mannitol, mannitol/trehalose mix (1:1), trehalose) on redispersibility and material powder properties were investigated. Moreover, compression analysis was performed assessing the influence of compaction pressure on primary nanocrystal redispersibility and tablet disintegration. Higher drug loads and lower drying protectant levels resulted in particle growth, confirming a drug load dependence on redispersibility behavior. Notably, all drying protectants showed similar protection properties at properly chosen drying process parameters (Tg-dependent), except when VDD was used for mannitol formulations. Differences between the applied drying processes were observed in terms of downstream processing and tabletability: mannitol-containing formulations solidified via VDD showed an improved processability compared to formulations with trehalose. In conclusion, VDD is a promising drying technique that offers advantageous downstream processability compared to SD and represents an attractive novel processing technology for the pharmaceutical industry. As demonstrated in the present study, VDD combines higher yields with a leaner manufacturing process flow. The improved bulk properties provide enhanced tabletability and enable direct compression.

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Downstream drug product processing of itraconazole nanosuspension: Factors influencing tablet material properties and dissolution of compacted nanosuspension-layered sugar beads

Cited by 12 publications

References 24 publications

The Increased Dissolution and Oral Absorption of Itraconazole by Nanocrystals with an Endogenous Small-Molecule Surfactant as a Stabilizer

The Increased Dissolution and Oral Absorption of Itraconazole by Nanocrystals with an Endogenous Small-Molecule Surfactant as a Stabilizer

Tabletized Nanomedicine: From the Current Scenario to Developing Future Medicine

Transformation of ABT-199 Nanocrystal Suspensions into a Redispersible Drug Product—Impact of Vacuum Drum Drying, Spray Drying and Tableting on Re-Nanodispersibility

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