Lungs deposition and pharmacokinetic study of submicron budesonide particles in Wistar rats intended for immediate effect in asthma
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Date
2017-03-10
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Abstract
The purpose of the present investigation was to study the aerosolization, lungs deposition and
pharmacokinetic study of inhalable submicron particles of budesonide in male Wistar rats. Submicron
particles were prepared by antisolvent nanoprecipitation method and freeze-dried to obtain free
flowing powder. The freeze-drying process yielded dry powder with desirable aerodynamic properties
for inhalation therapy. An in-house model inhaler was designed to deliver medicine to lungs,
optimized at dose level of 10 mg for 30 sec of fluidization. The in vitro aerosolization study
demonstrates that submicron particles dissolve faster with improved aerosolization effect as
compared to micronized budesonide. Both submicron and micron particles were compared for in vivo
lungs dep- osition. The results showed that relatively high quantity of submicron particles reaches
deep into the lungs as compared to micron particles. Most pronounced effect observed with submicron
particles from pharmacokinetic parameters was the enhancement in peak plasma concentration (Cmax)
by 28.85 %, and increase in area under concentration curve (AUC0–8h) by 30.33 % compared to micron
sized particles. The results suggested that devel- oped submicronized formulation of budesonide can
be used for pulmonary drug delivery for high deposition to deep lungs tissues.
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Keywords
budesonide, asthma, submicron particles, aerosolization, lungs deposition, pharmacokinetic