Aerosolized Therapeutics

A study on differential deposition of aerosols in the maxillary sinus of human cadavers by particle size showed superior efficiency of deposition with smaller particle sizes compared with the larger particle size. One effective way to disperse medication in smaller particle size is by aerosolizing medication.

Aerosolized therapeutic agents have been used to relieve diseases of the airways since early in medical history. The earliest versions were medicines that were added to boiling water and inhaled.

Today’s more sophisticated aerosolized therapeutic agents are delivered via:

• ultrasonic compressors • jet nebulizers • dry powder inhalers • metered-dose inhalers

The delivery of aerosolized therapeutic agents for systemic activity or locally to the airways via inhalation confers numerous advantages. Advances in the formulation of pharmacologic agents, coupled with newly designed aerosol devices, have expanded treatment options to accommodate various and specific patient factors.

Challenges in Administration of Aerosolized Therapeutics

The most efficient delivery of systemic therapeutic agents historically has been via the parenteral route. However, there are several disadvantages associated with parenteral administration. Among these,

• systemic toxicity • injection site reactions • in-hospital administration to provide accurate dosing by a medically competent individual • patient adherence to therapy • cost

When it is available, aerosolized therapeutic delivery provides solutions to some of the shortcomings inherent in parenteral drug therapy.

Applications for Aerosolized Therapeutics

Diseases of the airways are logical candidates for treatment with aerosolized therapeutics, and aerosolized formulations of corticosteroids have been used in the treatment of asthma, cystic fibrosis, and obstructive lung disorders for several years. Other airway diseases in which aerosolized drug delivery may be effective include bronchiectasis, pulmonary and bronchial infections, ventilator-associated infections such as pneumonia, and sinusitis.

Among those on a lengthy list, some of the more promising agents include the following:

• leuprolide acetate for the treatment of infertility, postmenopausal breast cancer, and prostate cancer • morphine and fentanyl for analgesia • cyclosporine for the prevention of allograft rejection • antitrypsin proteinase inhibitor for the treatment of congenital emphysema • growth hormone-releasing factor for the treatment of pituitary short stature

Some of the challenges encountered in creating new formulations that are both safe and effective for inhalation are

• dosing and drug deposition in relation to particle size • delivery device • delivery target • establishing and maintaining effective antibiotic concentrations • physical and chemical conditions that increase the complexity and difficulty of treatment

Development of new technologies has stimulated further clinical investigation with aerosolized agents in a number of therapeutic areas. Advances throughout the last decade have expanded our knowledge of the pharmacokinetics and pharmacodynamics of aerosolized therapeutics, and our understanding of the diseases has improved stimulating research activity with aerosol devices for effective delivery.

Technologic and scientific progress in aerosolized therapeutics to manage chronic disease conditions, offer hope and new-found freedom to patients. Quality-of-life benefits and the conservation of health-care dollars make continued research and clinical trials of aerosolized therapeutics essential. A number of new therapeutic agents are being explored for aerosol delivery that may have important implications for disease management in the future.

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