Chimeral agglomerates of microparticles for the administration of caffeine nasal powders

Russo, Paola; Buttini, Francesca; Sonvico, Fabio; Bettini, Ruggero; Massimo, Gina; Sacchetti, C.; Colombo, Paolo; Santi, Patrizia

doi:10.1016/s1773-2247(04)50083-7

Cited by 24 publications

(14 citation statements)

References 27 publications

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“…In order to determine the tensile strength, a single agglomerate (n=8) was placed on a mobile platform under the measuring head of a calibrated load cell (514 QD, DS Europe, Milan, Italy) (14). The very slow movement of the platform caused the compression of the agglomerate against the measuring head.…”

Section: Characterization Of the Agglomeratesmentioning

confidence: 99%

“…The boiling point of the solvent, as well as the spray-drier scale, can affect particle sizes (10,11). Microparticulated dried powders, granules, or agglomerates can be used as oral dosage forms (4,9,12) and nasal powders (13,14).…”

Section: Introductionmentioning

confidence: 99%

“…Unfortunately, the attainment of biopharmaceutical attributes by microparticles is opposed by the small size of the particles that leads to powders with bulk volume and problematic flow for dosage forms manufacturing (14,21). In several pharmaceutical applications, particles might be fine for drug delivery but coarse enough to facilitate the solid dosage form preparation.…”

Section: Introductionmentioning

confidence: 99%

“…In particular, this technological problem could be solved using soft agglomeration, a process in which the powder size is enlarged by constructing weak clusters of primary microparticles (14). Soft agglomerates are easily broken down by air turbulence or water uptake, reconstituting the original size of the microparticles.…”

Section: Introductionmentioning

confidence: 99%

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Agglomerates Containing Pantoprazole Microparticles: Modulating the Drug Release

et al. 2009

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Abstract. Pantoprazole-loaded microparticles were prepared using a blend of Eudragit® S100 and Methocel® F4M. The accelerated stability was carried out during 6 months at 40°C and 75% relative humidity. In order to improve technological characteristics of the pantoprazole-loaded microparticles, soft agglomerates were prepared viewing an oral delayed release and gastro-resistant solid dosage form. The agglomeration was performed by mixing the pantoprazole microparticles with spray-dried mannitol/ lecithin powders. The effects of factors such as the amount of lecithin in the spray-dried mannitol/lecithin powders and the ratio between pantoprazole microparticles and spray-dried mannitol/lecithin powders were evaluated. The pantoprazole-loaded microparticles present no significant degradation in 6 months. The agglomerates presented spherical shape, with smooth surface and very small quantity of nonagglomerated particles. The agglomerates presented different yields (35.5-79.0%), drug loading (58-101%), and mechanical properties (tensile strength varied from 44 to 69 mN mm −2 ), when the spraydried mannitol/lecithin powders with different lecithin amounts were used. The biopharmaceutical characteristics of pantoprazole microparticles, i.e., their delayed-release properties, were not affected by the agglomeration process. The gastro-resistance of the agglomerates was affected by the amount of spray-dried mannitol/lecithin powders. The ratio of lecithin in the spray-dried mannitol/lecithin powders was the key factor in the agglomerate formation and in the drug release profiles. The agglomerates presenting better mechanical and biopharmaceutical characteristics were prepared with 1:2 (w/w) ratio of pantoprazole-loaded microparticles and mannitol/lecithin (80:20) powder.

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Section: Characterization Of the Agglomeratesmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Agglomerates Containing Pantoprazole Microparticles: Modulating the Drug Release

et al. 2009

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“…1 Those primary microparticles were agglomerated in porous, brittle globules giving rise to powders having improved flowability and handling. 2 Owing to their high porosity and relatively weak internal bonding, these agglomerates are fragile clusters of microparticles, strong enough to be handled, but sufficiently weak to be fragmented during insufflation. In the case of caffeine, it was shown that the fragments of agglomerates had useful size for deposition into the nasal cavity.…”

Section: Introductionmentioning

confidence: 99%

Primary Microparticles and Agglomerates of Morphine for Nasal Insufflation

Russo

Sacchetti

Pasquali

et al. 2006

Journal of Pharmaceutical Sciences

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Amorphous nasal powder advanced performance: in vitro/ex vivo studies and correlation with in vivo pharmacokinetics

Henriques,

Bicker,

Carona

et al. 2023

J. Pharm. Investig.

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Purpose Amorphous solid dispersions (ASD) for nasal delivery offer the opportunity to increase drug release performance, while using polymers with mucoadhesive properties. The aim of the present study was to apply this solubility enhancement technique to a poorly soluble drug for nasal delivery, while comparing two particle engineering strategies, namely spray dried microparticles and chimeral agglomerates, with the corresponding physical blends with crystalline drug. Methods Formulations of piroxicam were manufactured using varied polymer and particle engineering strategies and evaluated through in vitro drug release and ex vivo permeation studies, as well as nasal deposition and in vivo pharmacokinetic studies. Results ASD with hydroxypropyl methylcellulose (HPMC) showed enhanced drug release and permeation, compared to polyvinylpyrrolidone/vinyl acetate formulations and blends. Nasal deposition of HPMC chimeral agglomerates suggested off-target deposition. In vivo pharmacokinetic studies revealed that spray-dried HPMC-containing microparticles exhibited the highest maximum plasma concentration (Cmax) and the lowest time to attain it (tmax). In vitro release rate and in vivo absorption rate were correlated as well as tmax and in vitro performance. When excluding the formulation with least nasal targeted deposition, in vitro release and ex vivo permeation performance were also correlated with Cmax and area under the drug concentration-time curve (AUC) from 0 to 1 h, with R2 > 0.89. Conclusion ASD for nasal delivery provide fast drug absorption, which depends on the supersaturation ability of the polymer employed. In vitro-in vivo correlations suggested that in vitro release and ex vivo permeation studies are predictive tools regarding nasal absorption.

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Chimeral agglomerates of microparticles for the administration of caffeine nasal powders

Cited by 24 publications

References 27 publications

Agglomerates Containing Pantoprazole Microparticles: Modulating the Drug Release

Agglomerates Containing Pantoprazole Microparticles: Modulating the Drug Release

Primary Microparticles and Agglomerates of Morphine for Nasal Insufflation

Amorphous nasal powder advanced performance: in vitro/ex vivo studies and correlation with in vivo pharmacokinetics

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