Development of porous particles using dextran as an excipient for enhanced deep lung delivery of rifampicin

[Display omitted] This study aimed to develop a dry powder inhaler (DPI) formulation for enhanced deep lung delivery of rifampicin using dextrans of different molecular weights. Porous particles were formed by a spray-drying method, which was designed based on the Peclet number. The morphology of pa...

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Veröffentlicht in:International journal of pharmaceutics 2019-01, Vol.555, p.280-290
Hauptverfasser: Kadota, Kazunori, Yanagawa, Yuko, Tachikawa, Tomoko, Deki, Yuto, Uchiyama, Hiromasa, Shirakawa, Yoshiyuki, Tozuka, Yuichi
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Sprache:eng
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Zusammenfassung:[Display omitted] This study aimed to develop a dry powder inhaler (DPI) formulation for enhanced deep lung delivery of rifampicin using dextrans of different molecular weights. Porous particles were formed by a spray-drying method, which was designed based on the Peclet number. The morphology of particles containing both rifampicin and dextran was dependent on the dextran concentration. The D50 values of SDPs containing rifampicin and dextran 40 or 70 at ratios of less than 1:10 were below 5 μm. The specific surface area values of spray-dried particles containing rifampicin and dextran 40 or 70 of more than 1:10 were over 20 m2/g, assuming that an increase in specific surface area was indicative of an increase in the formation ratio of a porous structure. DPI formulations that contained higher amounts of dextran had higher rifampicin contents. Thus, the formulations containing a dextran: rifampicin ratio of 1:20 had approximately 100% drug encapsulation. The formation of the porous particles can be explained by the related Peclet number, which correlates with the viscosity and surface tension of the ethanol-water solution used in preparing the particles. It was noted that the existence ratio of the porous particles increased as the viscosity of the mixed solution was increased. Furthermore, an increase in the proportion of dextran resulted in higher rifampicin loading into the particles and the formation of finer particle fractions (FPF) (
ISSN:0378-5173
1873-3476
DOI:10.1016/j.ijpharm.2018.11.055