Physical characteristics and aerosolization performance of insulin dry powders for inhalation prepared by a spray drying method.

Yu You, Min Zhao, Guangli Liu, Xing Tang

Research output: Contribution to journalArticle

37 Citations (Scopus)

Abstract

The objective of this study was to investigate the influence of formulation excipients on the physical characteristics and aerosolization performance of insulin dry powders for inhalation. Insulin dry powders were prepared by a spray drying technique using excipients such as sugars (trehalose, lactose and dextran), mannitol and amino acids (L-leucine, glycine and threonine). High performance liquid chromatography and the mouse blood glucose method were used for determination of the insulin content. The powder properties were determined and compared by scanning electron microscopy, thermo-gravimetric analysis and size distribution analysis by a time-of-flight technique. The in-vitro aerosolization behaviour of the powders was assessed with an Aerolizer inhaler using a twin-stage impinger. Powder yield and moisture absorption were also determined. Results showed that there was no noticeable change in insulin content in any of the formulations by both assay methods. All powders were highly wrinkled, with median aerodynamic diameters of 2-4 microm, and consequently suitable for pulmonary administration. The tapped density was reduced dramatically when glycine was added. The powders containing mannitol, with or without L-leucine, were less sensitive to moisture. The highest respirable fraction of 67.3 +/- 1.3% was obtained with the formulation containing L-leucine, in contrast to formulations containing glycine and threonine, which had a respirable fraction of 11.2 +/- 3.9% and 23.5 +/- 2.5%, respectively. In addition, powders with good physical properties were achieved by the combination of insulin and trehalose. This study suggests that L-leucine could be used to enhance the aerosolization behaviour of the insulin dry powders for inhalation, and trehalose could potentially be used as an excipient in the formulations.
Original languageEnglish
Pages (from-to)927-34
Number of pages8
JournalThe Journal of pharmacy and pharmacology
DOIs
Publication statusPublished - 2007

Keywords

  • Administration, Inhalation
  • Aerosols
  • Animals
  • Blood Glucose
  • Blood Glucose: metabolism
  • Chemistry, Pharmaceutical
  • Drug Carriers
  • Drug Carriers: chemistry
  • Drug Delivery Systems
  • Excipients
  • Hypoglycemic Agents
  • Hypoglycemic Agents: administration & dosage
  • Hypoglycemic Agents: chemistry
  • Hypoglycemic Agents: pharmacokinetics
  • Insulin
  • Insulin: administration & dosage
  • Insulin: chemistry
  • Insulin: pharmacokinetics
  • Male
  • Mice
  • Particle Size
  • Powders

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