Steroid/mucokinetic hybrid nanoporous microparticles for pulmonary drug delivery

Tewes, Frédéric; Paluch, Krzysztof J.; Tajber, Lidia; Gulati, Karan; Kalantri, Devesh; Ehrhardt, Carsten; Healy, Anne Marie

doi:10.1016/j.ejpb.2013.03.020

Cited by 30 publications

(18 citation statements)

References 44 publications

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“…The SSA initially increased with the increasing concentration of ammonium carbonate, then dropped when the concentration of ammonium carbonate reached to 25 wt% of total solid content. The change tendency in the SSA of mannitols was consistent with the porosity and pore size of mannitols, as shown in SEM micrographs (Figure 1), which was well agreed with previous documents2425. The pore size resulting from different ammonium carbonate concentration was discussed in the part of aforementioned formation mechanism of porous particles.…”

Section: Resultssupporting

confidence: 91%

Nanoporous mannitol carrier prepared by non-organic solvent spray drying technique to enhance the aerosolization performance for dry powder inhalation

Peng

Zhang

Huang

et al. 2017

Sci Rep

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An optimum carrier rugosity is essential to achieve a satisfying drug deposition efficiency for the carrier based dry powder inhalation (DPI). Therefore, a non-organic spray drying technique was firstly used to prepare nanoporous mannitol with small asperities to enhance the DPI aerosolization performance. Ammonium carbonate was used as a pore-forming agent since it decomposed with volatile during preparation. It was found that only the porous structure, and hence the specific surface area and carrier density were changed at different ammonium carbonate concentration. Furthermore, the carrier density was used as an indication of porosity to correlate with drug aerosolization. A good correlation between the carrier density and fine particle fraction (FPF) (r2 = 0.9579) was established, suggesting that the deposition efficiency increased with the decreased carrier density. Nanoporous mannitol with a mean pore size of about 6 nm exhibited 0.24-fold carrier density while 2.16-fold FPF value of the non-porous mannitol. The enhanced deposition efficiency was further confirmed from the pharmacokinetic studies since the nanoporous mannitol exhibited a significantly higher AUC0-8h value than the non-porous mannitol and commercial product Pulmicort. Therefore, surface modification by preparing nanoporous carrier through non-organic spray drying showed to be a facile approach to enhance the DPI aerosolization performance.

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Section: Resultssupporting

confidence: 91%

Nanoporous mannitol carrier prepared by non-organic solvent spray drying technique to enhance the aerosolization performance for dry powder inhalation

Peng

Zhang

Huang

et al. 2017

Sci Rep

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“…This was attributed to the high solubility in water of LVX associated to the high drug loading and to the large surface area developed by the micrometric-sized particles, which allowed the rapid diffusion of the drug from the MS matrix. In addition, the amorphous state of LVX, evidenced by XRD and DTA analyses, is usually associated with higher dissolution rate compared to crystalline state [38]. Similar results were obtained by Corrigan et al by the preparation of salbutamol sulphate loaded in formaldehydecrosslinked chitosan MS [63] with no difference between crosslinked and noncrosslinked systems.…”

Section: -Lvx Release From Mssupporting

confidence: 80%

“…the fraction of LVX in particles with aerodynamic diameters below 5.0 µm, was calculated by interpolation, from the inverse of the standard normal cumulative mass percentage distribution, and considering stages 1 to 3. The mass median aerodynamic diameter (MMAD) of the particles was calculated from a similar plot (considering stages 1 to 6) as the particle aerodynamic diameter at which the line crosses the 50% mark [37][38][39]. The fine particle fraction (FPF) was calculated by converting the FPD mass as the percentage of the ED.…”

Section: -In Vitro Deposition Studies Using Next Generation Impactor mentioning

confidence: 99%

Optimization of levofloxacin-loaded crosslinked chitosan microspheres for inhaled aerosol therapy

Gaspar

Sousa

Pais

et al. 2015

European Journal of Pharmaceutics and Biopharmaceutics

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The aim of this work was the development of innovative levofloxacin-loaded swellable microspheres (MS) for the dry aerosol therapy of pulmonary chronic Pseudomonas aeruginosa infections in Cystic Fibrosis patients. In a first step, a factorial design was applied to optimize formulations of chitosan-based MS with glutaraldehyde as crosslinker. After optimization, other crosslinkers (genipin, glutaric acid and glyceraldehyde) were tested. Analyses of MS included aerodynamic and swelling properties, morphology, drug loading, thermal and chemical characteristics, in vitro antibacterial activity and drug release studies. The prepared MS presented a drug content ranging from 39.8 to 50.8 % of levofloxacin in an amorphous or dispersed state, antibacterial activity and fast release profiles. The highest degree of swelling was obtained for MS crosslinked with glutaric acid and genipin. These formulations also presented satisfactory aerodynamic properties, making them a promising alternative, in dry-powder inhalers, to levofloxacin solution for inhalation.3

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“…X-ray powder diffraction measurements were conducted using a low background silicon sample holder and a Rigaku Miniflex II desktop X-ray diffractometer (Rigaku, Tokio, Japan) as previously described (Caron et al, 2011;Tewes et al, 2013). The samples (n ≥ 2) were scanned over a range of 5-40 • in 2Â scale using a step size of 0.05 • /s.…”

Section: Powder X-ray Diffraction (Xrd)mentioning

confidence: 99%

Bulk, surface properties and water uptake mechanisms of salt/acid amorphous composite systems

Bianco

Tewes

Tajber

et al. 2013

International Journal of Pharmaceutics

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Developing amorphous pharmaceuticals can be desirable due to advantageous biopharmaceutical properties. Low glass transition temperature (Tg) amorphous drugs can be protected from crystallisation by mixing with high Tg excipients, such as polymers, or with salt forms. However, both polymers and salts can enhance the water uptake. The aim of this study was to formulate physico-chemically stable amorphous materials, by co-processing different proportions of sulfathiazole and its sodium salt to produce an optimum ratio, characterised by the best physical stability and lowest hygroscopicity. Both sulfathiazole and salt amorphised upon spray drying. At room temperature, sulfathiazole crystallised within 1h at <5% relative humidity while the salt deliquesced when exposed to ambient humidity conditions. In the case of composite systems, FTIR spectroscopy, thermal and surface analysis suggested interactions with an acid:salt stoichiometry of 1:2. Increasing proportions of salt raised the Tg, enhancing the storage stability, however this was opposed by an enhanced hygroscopicity. The water uptake mechanism within the different amorphous systems, analysed by fitting the water sorption isotherms with the Young and Nelson equation, was dependent on the ratio employed, with the salt and the acid facilitating absorption and adsorption, respectively. Tuning the properties of amorphous salt/acid composites by optimising the ratio appears potentially promising to improve the physical stability of amorphous formulations.

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Steroid/mucokinetic hybrid nanoporous microparticles for pulmonary drug delivery

Cited by 30 publications

References 44 publications

Nanoporous mannitol carrier prepared by non-organic solvent spray drying technique to enhance the aerosolization performance for dry powder inhalation

Nanoporous mannitol carrier prepared by non-organic solvent spray drying technique to enhance the aerosolization performance for dry powder inhalation

Optimization of levofloxacin-loaded crosslinked chitosan microspheres for inhaled aerosol therapy

Bulk, surface properties and water uptake mechanisms of salt/acid amorphous composite systems

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