Combination chemotherapeutic dry powder aerosols via controlled nanoparticle agglomeration

Pharm Res. 2009 Jul;26(7):1752-63. doi: 10.1007/s11095-009-9886-2. Epub 2009 May 5.

Abstract

Purpose: To develop an aerosol system for efficient local lung delivery of chemotherapeutics where nanotechnology holds tremendous potential for developing more valuable cancer therapies. Concurrently, aerosolized chemotherapy is generating interest as a means to treat certain types of lung cancer more effectively with less systemic exposure to the compound.

Methods: Nanoparticles of the potent anticancer drug, paclitaxel, were controllably assembled to form low density microparticles directly after preparation of the nanoparticle suspension. The amino acid, L-leucine, was used as a colloid destabilizer to drive the assembly of paclitaxel nanoparticles. A combination chemotherapy aerosol was formed by assembling the paclitaxel nanoparticles in the presence of cisplatin in solution.

Results: Freeze-dried powders of the combination chemotherapy possessed desirable aerodynamic properties for inhalation. In addition, the dissolution rates of dried nanoparticle agglomerate formulations (approximately 60% to 66% after 8 h) were significantly faster than that of micronized paclitaxel powder as received (approximately 18% after 8 h). Interestingly, the presence of the water soluble cisplatin accelerated the dissolution of paclitaxel.

Conclusions: Nanoparticle agglomerates of paclitaxel alone or in combination with cisplatin may serve as effective chemotherapeutic dry powder aerosols to enable regional treatment of certain lung cancers.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Administration, Inhalation
  • Aerosols / chemistry*
  • Antineoplastic Agents / administration & dosage*
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / toxicity
  • Cell Line, Tumor
  • Cell Survival / drug effects
  • Cisplatin / administration & dosage*
  • Cisplatin / chemistry
  • Drug Delivery Systems / methods*
  • Drug Therapy, Combination
  • Freeze Drying
  • Humans
  • Leucine / chemistry
  • Lung / cytology
  • Nanoparticles / chemistry*
  • Nanoparticles / toxicity
  • Nanoparticles / ultrastructure
  • Paclitaxel / administration & dosage*
  • Paclitaxel / chemistry
  • Paclitaxel / toxicity
  • Particle Size
  • Powders / chemistry
  • Solubility
  • Transition Temperature

Substances

  • Aerosols
  • Antineoplastic Agents
  • Powders
  • Leucine
  • Paclitaxel
  • Cisplatin