The purpose of this study was to address the effect of feedstock properties and process variables on the characteristics of antitubercular drug–palladium (Pd) containing poly(lactic) acid (PLA) microparticles (MP) obtained by spray-drying of noncolloidal particle dispersions in fast drying regime. Two different systems were compared: capreomycin–Pd (C–Pd) and ofloxacin–Pd (Ofx–Pd) dispersions in acetonitrile PLA solution. Particle size, dynamic light scattering, differential scanning calorimetry, SEM–energy dispersive X-ray, and spectrophotometric methods were used for MP characterization. C–Pd-loaded MP were optimized preliminarily by experimental design and compared with Ofx–Pd-loaded MP investigated in our previous work. Morphology of feedstock particles had a dominant role in determining MP morphology. The Charlesworth and Marshall theory was used to explain such behavior. The smaller and homogeneous C–Pd microparticulates favored MP inflation and buckling by forming a thick and nonporous shell. A percolation effect was proposed for the larger and irregular Ofx–Pd particles that produced smaller MP with a more porous shell. Increasing feedstock concentration led to higher particle loss. A tentative descriptive scheme of MP formation according to feedstock particle arrangement was proposed. This work suggested that spray-drying of drug dispersions should carefully consider the morphology of feedstock particles as a major parameter influencing final MP properties.

The influence of feedstock and process variables on the encapsulation of drug suspensions by spray-drying in fast drying regime: the case of novel antitubercular drug–palladium complex containing polymeric microparticles

BLASI, Paolo;
2014-01-01

Abstract

The purpose of this study was to address the effect of feedstock properties and process variables on the characteristics of antitubercular drug–palladium (Pd) containing poly(lactic) acid (PLA) microparticles (MP) obtained by spray-drying of noncolloidal particle dispersions in fast drying regime. Two different systems were compared: capreomycin–Pd (C–Pd) and ofloxacin–Pd (Ofx–Pd) dispersions in acetonitrile PLA solution. Particle size, dynamic light scattering, differential scanning calorimetry, SEM–energy dispersive X-ray, and spectrophotometric methods were used for MP characterization. C–Pd-loaded MP were optimized preliminarily by experimental design and compared with Ofx–Pd-loaded MP investigated in our previous work. Morphology of feedstock particles had a dominant role in determining MP morphology. The Charlesworth and Marshall theory was used to explain such behavior. The smaller and homogeneous C–Pd microparticulates favored MP inflation and buckling by forming a thick and nonporous shell. A percolation effect was proposed for the larger and irregular Ofx–Pd particles that produced smaller MP with a more porous shell. Increasing feedstock concentration led to higher particle loss. A tentative descriptive scheme of MP formation according to feedstock particle arrangement was proposed. This work suggested that spray-drying of drug dispersions should carefully consider the morphology of feedstock particles as a major parameter influencing final MP properties.
2014
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11581/389429
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