Pharmaceutical Characteristics Of Aerosolized Antibiotics

There are several relevant pharmaceutical factors that should be considered in formulating drug products for aerosol administration to the lung. The purpose of early investigations was to assess potential benefit of aerosolized antibiotics, and they often used crude formulations in which the stability and integrity of the product were not known. In formulating products, consideration should be given to drug-specific characteristics such as pH, stability, tonicity, particle size, and taste. Additionally, the inhalation system used to deliver the dose is an important consideration.

In addition to these various characteristics, patient-specific factors can affect delivery of aerosolized antimicrobials to the lung. Patient breathing technique and several physiologic variables affect ultimate deposition, including age, breathing pattern, ventilation volumes, and the presence of disease [9].

Chemical properties that may affect drug absorption from the airway surface into the systemic circulation include molecular weight, protein binding, and lipophilicity [8], although the extent of absorption is highly variable [10]. However, the extent of absorption into the systemic circulation is felt to be minimal. More research is warranted to evaluate the impact of other patient variables on systemic exposure resulting from inhaled therapies.

The ideal agent for administration by aerosolization to treat infection in the lung would be safe and effective. It should exhibit no local adverse effects and have little or no systemic absorption. The agent should exhibit good activity against the bacteria causing infection and minimize the risk for resistance. Finally, the product should be stable chemically during storage and administration and have an acceptable taste and odor.

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