Home

Personnel

Publications

Newsletters

Glossary

Bibliography

Calendar

Services

Products

Instructions,
Descriptions,
Manuals

Links

 

 

 

CRITICAL REVIEW AND COMMENTARY

Reference: Efficacy of aerosolized amphotericin B desoxycholate and liposomal amphotericin B in the treatment of invasive pulmonary aspergillosis in severely immunocompromised rats. by Elisabeth J Ruijgrok, Arnold G Vulto and Els W.M. Van Etten.Journal of Antimicrobial Chemotherapy. 2001. 48. 89-95.

 Invasive pulmonary aspergillosis is a life threatening disease. Current clinical treatment, intravenously administered antifungals, is poor especially in immunocompromised patients. This paper explores the inhalation delivery route as a relevant and effective treatment of this disease.

 Female rats, immunocompromised with cyclophosphamide were infected with Aspergillus fumigatus by intratracheal instillation into the left lung. They were then treated with different inhalation exposure regimens of two antifungal formulations, amphotericin B desoxycholate (Fungizone) or Liposomal amphotericin B.

 The study was designed with group sizes of 15 animals.  Controls were exposed to 5% aerosolised glucose or placebo liposomes.  A separate group was exposed to an aerosol of pure amphotericin B in 5% glucose.  Nominal nebuliser concentrations were quoted.  The dose of Aspergillus fumigatus to the animals could not be quoted  because aerosol concentrations and particle size analyses were not undertaken. This may have influenced interpretation of the results.

 A nebuliser concentration of 2mg/mL amphotericin B desoxycholate 30 hours after infection did significantly prolong the survival of rats by up to 5 days. Neither 1mg/mL nor 4mg/mL showed any significant effect on survival. The authors give reasons for these differences. Without estimates of the actual dose or support of the statement concerning pulmonary toxicity of the 4mg/mL solution, these statements are speculative.

 A single exposure to a 4mg/mL liposomal formulation of amphotericin B was as effective in prolonging survival for up to 4 days as were 2 exposures in 24 hours or 2 or 4 exposures in 24hours. This indicates the limited advantage of additional exposures.

 The rats exposed to 4mg/mL suspension of amphotericin B in 5% glucose alone showed no improvement in survival. These data are only mentioned in the discussion. They should have been emphasised in the results as they could suggest that the modified formulations were critical in enhancing survival. It is difficult to draw any clear conclusions because it could not be determined whether any drug was delivered to the lungs of the rats without aerosol concentration and particle size measurements or information on whether the suspension was micronised.

 All rats infected showed positive organ cultures in both lungs and the liver, the only organs examined. No systemic drug estimations were undertaken in this study but the authors report previous work indicating low systemic exposure following inhalation delivery. This suggests that aerosol delivery alone would be insufficient to treat the disseminated disease as indicated by the authors. Their suggestions of observing low systemic doses of amphotericin and other antifungals delivered by inhalation is a well-founded extension of this work.

 The authors undertook additional surface tension work to demonstrate that inhalation of amphotericin B desoxycholate but not the liposomal amphotericin B leads to surfactant dysfunction.  This could have clinical implications.

 This interesting paper emphasises the value of using the inhalation route of delivery as an effective means of delivering drugs to the respiratory tract to treat pulmonary disease while limiting systemic toxicity. This should encourage further development of inhaled drug delivery for the treatment of invasive Aspergillus fumigatus infections.

By: David Alexander , PhD

Guest WriterIndependent pharmaceutical Consultant ,  DA Nonclinical Safety

Email: david_a@ntlworld .com ; Website: http://www.da-nonclinsafety.com