Purpose:
To prepare solid lipid
nanoparticles (SLN) and nanostructured lipid carriers (NLC)
of loratadine (LRT) for the
treatment of allergic skin reactions.
Methods: SLN and NLC were prepared
by high pressure homogenization method. Their entrapment
efficiency (EE) and loading capacity (LC) were
determined. The physical stability of nanoparticles was
investigated during 6 months of storage at room
temperature (RT), 4 and 40 oC. Fourier
transform infrared spectroscopy (FTIR), differential
scanning calorimetry (DSC) and laser diffraction (LD)
were used for the investigation of drug:excipient
compatibility, thermal behaviour and particle size of
the nanoparticles. In vitro release and ex vivo skin
penetration of LRT were studied. Nanoemulsions (NE) were
also prepared and characterized for comparison.
Results: Nanoparticles sizes ranged
from 0.222 ± 0.011 μm to 0.252 ± 0.014 μm (D50 as a
value based on the volume distribution, the maximum
particle diameter below which 50 % of the sample volume
exists) They were obtained with high drug payloads (>
90.67 %). LRT was compatible with the other excipients
after 6 months. Particle size did not significantly
alter particularly at RT. The highest release rate was
obtained with NE (1.339 ± 0.026 mcg/ml/h) followed by
NLC (1.007 ± 0.011 mcg/ml/h) and SLN (0.821 ± 0.012
mcg/ml/h), indicating anomalous transport (p < 0.05).
Penetration profiles of LRT through skin were
statistically similar for SLN and NLC (p > 0.05). NE
showed the highest penetration rate (0.829 ± 0.06 mcg/cm2/h)
(p < 0.05).
Conclusion: SLN and NLC of LRT are
alternative formulations for immediate treatment of
allergic skin reactions with prolonged drug delivery via
reservoir action.
Keywords: Loratadine, Transdermal
delivery, Controlled drug delivery, Solid Lipid
nanoparticles, Nanostructured lipid carriers, Allergy