Elsevier

Materials Science and Engineering: C

Volume 41, 1 August 2014, Pages 255-266
Materials Science and Engineering: C

New alginic acid–atenolol microparticles for inhalatory drug targeting

https://doi.org/10.1016/j.msec.2014.04.040Get rights and content

Highlights

  • Novel particulate material to target atenolol to the respiratory membrane was developed.

  • Crumbled microparticles were obtained by spray drying of alginic–atenolol dispersions.

  • Ionic interaction between alginic acid and atenolol was demonstrated in the product.

  • Amorphous solids with low moisture content and high load efficiency were produced.

  • Relationships between the feed formulation and the product characteristics were found.

Abstract

The inhalatory route allows drug delivery for local or systemic treatments in a noninvasively way. The current tendency of inhalable systems is oriented to dry powder inhalers due to their advantages in terms of stability and efficiency. In this work, microparticles of atenolol (AT, basic antihypertensive drug) and alginic acid (AA, acid biocompatible polyelectrolyte) were obtained by spray drying. Several formulations, varying the relative composition AT/AA and the total solid content of the atomized dispersions, were tested. The powders were characterized by: Fourier Transform Infrared Spectroscopy, Differential Scanning Calorimetry and Powder X-ray Diffraction, while also the following properties were measured: drug load efficiency, flow properties, particles size and density, moisture content, hygroscopicity and morphology. The ionic interaction between AA and AT was demonstrated, then the new chemical entity could improve the drug targeting to the respiratory membrane and increase its time residence due to the mucoadhesive properties of the AA polymeric chains. Powders exhibited high load efficiencies, low moisture contents, adequate mean aerodynamic diameters and high cumulative fraction of respirable particles (lower than 10 μm).

Keywords

Powder engineering
Spray drying
Polyelectrolyte–drug complex
Solid-state characterization
Inhalatory route

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