Summary: | The aims of the present study were to formulate and evaluate nanomicelles
containing poorly water soluble corticosteroids, budesonide (BUD) or
beclomethasone dipropionate (BDP) for pulmonary delivery using PEGylated
polymers (PEG5000-DSPE and PEG2000-DSPE).
All the sterically stabilized phospholipid nanomicelles (SSMs) were successfully
prepared using a co-precipitation and reconstitution method. The SSMs were
characterised by different physicochemical methods. There were significant
differences between the maximum solubilisation tendencies of PEG5000-DSPE and
PEG2000-DSPE for BUD, which were approximately 605.71±6.38 and 646.27±4.93
μg/ml, respectively. The maximum solubilisation tendencies of PEG5000-DSPE and
PEG2000-DSPE for BDP were approximately 209.65±7.74 and 210.01±5.28,
respectively. These results showed that PEGylated polymers had greater tendencies
to solubilise BUD than BDP. The mean particle sizes at maximum solubilisation of
BUD:PEG2000-DSPE (15.97±1.91 nm) and BDP:PEG2000-DSPE (15.44±1.66 nm)
were smaller than BUD:PEG5000-DSPE (20.45±1.65 nm) and BDP:PEG5000-DSPE
(19.99±0.98 nm). Blank SSMs of PEG5000-DSPE were successfully lyophilised at a
concentration of about 5 mM, while 10 mM of PEG2000-DSPE was needed for
lyophilisation.
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