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Case 1: Salbutamol particles

Salbutamol (or albuterol) is a short-acting β2-adrenergic receptor agonist used for the relief of bronchospasm in conditions such as asthma and chronic obstructive pulmonary disease. Teicos Pharma coated inhalable salbutamol using different amounts of L-leucine and different coating layer structures. The aerosolization properties of the carrier-free powders were studied under different inspiration flow rates. The coated powders were significantly less depended on the inspiration volume and showed excellent powder aerosoliazation, dispersion and alveoli deposition behavior.


Case 2: Aerosolization, Drug Permeation and Cellular Interaction of Leucine Coated Combination DPI powders

We investigated the effect of L-leucine coating on particle integrity, aerosolization properties, cellular interaction, viability and drug permeation properties of combination drug powder particles (beclomethasone dipropionate and salbutamol sulphate) for dry powder inhalation. The powder was prepared using an aerosol-based gas-phase method to combine a water-soluble β-agonist drug, salbutamol sulphate, and corticosteroid, beclomethasone dipropionate, into fine particles which are subsequently encapsulated and coated with L-leucine. Particle morphology studies showed that crystalline leucine coating resulted in intact separated particles. Dissolution profiles showed a faster dissolution of beclomethasone dipropionate, while leaving the salbutamol dissolution unhampered when compared with their physical mixture. Permeation of beclomethasone dipropionate across a differentiated Calu-3 cell monolayer was increased with the L-leucine coating, and time-dependent recrystallization of the drug on top of the Calu-3 cell monolayer was also observed. The L-leucine coated particles were further investigated for cytocompatibility in three different pulmonary (Calu-3, A549 and BEAS-2B) and one human macrophage (THP-1) cell lines showing excellent tolerability. The L-leucine coated particles also elicited low reactive oxygen species generation in pulmonary BEAS-2B and macrophage THP-1 cell lines. The inhalable drug powders coated with leucine offer thus an interesting alternative for the delivery of poorly soluble drugs to the lung.

Teicos Pharma Ltd
Heinasuontie 29
00430 Helsinki

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