Investigations on particle surface characteristics vs. dispersion behaviour of l-leucine coated carrier-free inhalable powders

Janne Raula, Frank Thielmann, Majid Naderi, Vesa-Pekka Lehto, Esko I. Kauppinen

Research output: Contribution to journalArticleScientificpeer-review

34 Citations (Scopus)

Abstract

Aerosol microparticles of salbutamol sulphate are gas-phase coated with an amino acid l-leucine. Depending of the saturated state of l-leucine, the coating is formed by the surface diffusion of l-leucine molecules within a droplet or by the physical vapour deposition (PVD) of l-leucine or by the combination thereof. The PVD coated particles showed excellent aerosolization characteristics in a carrier-free powder delivery from an inhaler. The aerosolization of the fine powders is compared with surface energy parameters analysed by inverse gas chromatography (IGC). The dispersion testing is conducted by a Inhalation Simulator using a fast inhalation profile with inhalation flow rate of 67 l min−1. It is found that the powder emission is affected by the morphology, surface roughness (asperity size and density) of the particles and acidity of particle surface. The latter affects the dispersion and dose repeatability of fine powder in a case if l-leucine content is high enough. However, there is no direct correlation between dispersive surface energies and aerosolization performances of the powders. Crucial factors for the improved aerosolization rely weakly on surface acid–base properties but strongly on particle morphology and fine-scale surface roughness.
Original languageEnglish
Pages (from-to)79-85
JournalInternational Journal of Pharmaceutics
Volume385
Issue number1-2
DOIs
Publication statusPublished - 2010
MoE publication typeA1 Journal article-refereed

Fingerprint

Leucine
Powders
Inhalation
Surface Properties
Albuterol
Nebulizers and Vaporizers
Aerosols
Particle Size
Gas Chromatography
Sulfates
Gases
Amino Acids

Keywords

  • Aerosolization
  • coating
  • I-leucine
  • pulmonary drug delivery
  • surface energy
  • surface modification

Cite this

Raula, Janne ; Thielmann, Frank ; Naderi, Majid ; Lehto, Vesa-Pekka ; Kauppinen, Esko I. / Investigations on particle surface characteristics vs. dispersion behaviour of l-leucine coated carrier-free inhalable powders. In: International Journal of Pharmaceutics. 2010 ; Vol. 385, No. 1-2. pp. 79-85.
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abstract = "Aerosol microparticles of salbutamol sulphate are gas-phase coated with an amino acid l-leucine. Depending of the saturated state of l-leucine, the coating is formed by the surface diffusion of l-leucine molecules within a droplet or by the physical vapour deposition (PVD) of l-leucine or by the combination thereof. The PVD coated particles showed excellent aerosolization characteristics in a carrier-free powder delivery from an inhaler. The aerosolization of the fine powders is compared with surface energy parameters analysed by inverse gas chromatography (IGC). The dispersion testing is conducted by a Inhalation Simulator using a fast inhalation profile with inhalation flow rate of 67 l min−1. It is found that the powder emission is affected by the morphology, surface roughness (asperity size and density) of the particles and acidity of particle surface. The latter affects the dispersion and dose repeatability of fine powder in a case if l-leucine content is high enough. However, there is no direct correlation between dispersive surface energies and aerosolization performances of the powders. Crucial factors for the improved aerosolization rely weakly on surface acid–base properties but strongly on particle morphology and fine-scale surface roughness.",
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Investigations on particle surface characteristics vs. dispersion behaviour of l-leucine coated carrier-free inhalable powders. / Raula, Janne; Thielmann, Frank; Naderi, Majid; Lehto, Vesa-Pekka; Kauppinen, Esko I.

In: International Journal of Pharmaceutics, Vol. 385, No. 1-2, 2010, p. 79-85.

Research output: Contribution to journalArticleScientificpeer-review

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T1 - Investigations on particle surface characteristics vs. dispersion behaviour of l-leucine coated carrier-free inhalable powders

AU - Raula, Janne

AU - Thielmann, Frank

AU - Naderi, Majid

AU - Lehto, Vesa-Pekka

AU - Kauppinen, Esko I.

PY - 2010

Y1 - 2010

N2 - Aerosol microparticles of salbutamol sulphate are gas-phase coated with an amino acid l-leucine. Depending of the saturated state of l-leucine, the coating is formed by the surface diffusion of l-leucine molecules within a droplet or by the physical vapour deposition (PVD) of l-leucine or by the combination thereof. The PVD coated particles showed excellent aerosolization characteristics in a carrier-free powder delivery from an inhaler. The aerosolization of the fine powders is compared with surface energy parameters analysed by inverse gas chromatography (IGC). The dispersion testing is conducted by a Inhalation Simulator using a fast inhalation profile with inhalation flow rate of 67 l min−1. It is found that the powder emission is affected by the morphology, surface roughness (asperity size and density) of the particles and acidity of particle surface. The latter affects the dispersion and dose repeatability of fine powder in a case if l-leucine content is high enough. However, there is no direct correlation between dispersive surface energies and aerosolization performances of the powders. Crucial factors for the improved aerosolization rely weakly on surface acid–base properties but strongly on particle morphology and fine-scale surface roughness.

AB - Aerosol microparticles of salbutamol sulphate are gas-phase coated with an amino acid l-leucine. Depending of the saturated state of l-leucine, the coating is formed by the surface diffusion of l-leucine molecules within a droplet or by the physical vapour deposition (PVD) of l-leucine or by the combination thereof. The PVD coated particles showed excellent aerosolization characteristics in a carrier-free powder delivery from an inhaler. The aerosolization of the fine powders is compared with surface energy parameters analysed by inverse gas chromatography (IGC). The dispersion testing is conducted by a Inhalation Simulator using a fast inhalation profile with inhalation flow rate of 67 l min−1. It is found that the powder emission is affected by the morphology, surface roughness (asperity size and density) of the particles and acidity of particle surface. The latter affects the dispersion and dose repeatability of fine powder in a case if l-leucine content is high enough. However, there is no direct correlation between dispersive surface energies and aerosolization performances of the powders. Crucial factors for the improved aerosolization rely weakly on surface acid–base properties but strongly on particle morphology and fine-scale surface roughness.

KW - Aerosolization

KW - coating

KW - I-leucine

KW - pulmonary drug delivery

KW - surface energy

KW - surface modification

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SN - 0378-5173

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