An in vitro comparison of the mucoactive properties of guaifenesin, iodinated glycerol, surfactant, and albuterol.
OBJECTIVE
The mechanism of action of potential mucoactive agents could relate to effects on the mucociliary apparatus or to direct effects on the secretions. The purpose of this study was to determine the in vitro effects of several agents on the properties of mucus simulants and sputum collected from 30 adults with stable chronic bronchitis.


METHODS
Sputum or simulants were analyzed untreated and after the addition of the test agent at 1:5 volume to volume ratio for a contact period of 60 s. The concentrations of the agents were as follows: guaifenesin, 20 mg/mL; iodinated glycerol, 3 mg/mL; surfactant (Exosurf; Glaxo Wellcome; Research Triangle Park, NC) containing 13.5 mg of phospholipid per milliliter; albuterol, 5 mg/mL; and amphibian Ringer's solution (ARS) as a control. Dynamic viscoelasticity and surface mechanical impedance were measured in a magnetic microrheometer. Cohesiveness was measured using a filancemeter. The wettability of a hydrophilic surface was measured using an image processing system. The mucociliary transportability of sputum was timed on the frog palate, and cough transportability (CTR) was measured in a cough machine.


RESULTS
When compared to sputum that had no test agent or ARS added, all agents reduced sputum elasticity G', with surfactant, albuterol, and guaifenesin significant at p < 0.001. As well, guaifenesin (p = 0.006), albuterol (p = 0.003), and surfactant (p = 0.02) decreased surface mechanical impedance (frictional adhesiveness) compared to untreated sputum. However, there were no significant changes in wettability, hydration, cohesiveness, or CTR with any agent, and there were no significant changes in the properties of sputum or simulants treated with test agents when compared to those treated with ARS. Guaifenesin irreversibly disrupted mucociliary transport when applied directly to the frog palate.


CONCLUSIONS
These agents appear to have a minimal direct action on sputum in vitro, suggesting that at the concentrations studied, these agents do not have a significant beneficial effect on either the mucociliary transportability or CTR of chronic bronchitis sputum. However, there could be an effect of some of these agents after oral administration, especially if there is a secondary effect of the agent on an effector cell.
Rubin
B K
BK
Department of Pediatrics, Wake Forest University School of Medicine, Winston-Salem, NC 27157-1081, USA. brubin@wfubmc.edu
D000328:Adult; D000420:Albuterol / Q000494:pharmacology*; D000818:Animals; D004338:Drug Combinations; D005100:Expectorants / Q000494:pharmacology*; D005233:Fatty Alcohols / Q000494:pharmacology; D005990:Glycerol / Q000494:pharmacology*; D006140:Guaifenesin / Q000494:pharmacology*; D006801:Humans; D009079:Mucociliary Clearance / Q000187:drug effects; D009093:Mucus / Q000187:drug effects*; D010767:Phosphorylcholine; D011092:Polyethylene Glycols / Q000494:pharmacology; D011663:Pulmonary Surfactants / Q000494:pharmacology*; D011898:Ranidae; D013183:Sputum / Q000187:drug effects*
D004338:Drug Combinations; D005100:Expectorants; D005233:Fatty Alcohols; D011663:Pulmonary Surfactants; D010767:Phosphorylcholine; D011092:Polyethylene Glycols; D006140:Guaifenesin; C047049:dipalmitoylphosphatidylcholine, hexadecanol, tyloxapol drug combination; D005990:Glycerol; D000420:Albuterol