http://dx.doi.org/10.4314/tjpr.v12i3.2
Abstract
Purpose: To formulate solid lipid
microparticles (SLM) of loratadine (LRT) for the
treatment of allergic reactions via the nasal route.
Methods: Microparticles were prepared by
emulsion congealing technique. The drug content of
microparticles was analysed. Drug/excipient
compatibility and crystallinity characteristics of
microparticles were investigated by Fourier Transform
Infrared Spectroscopy (FT-IR) and differential scanning
calorimetry (DSC). Particle size distribution was
determined by laser diffraction (LD). Drug release from
microparticles was compared to that from conventional
vehicles (O/W emulsion, gel and oleageneous cream) using
Franz-type diffusion cells.
Results:
Drug content of microparticles was > 87.96 %. FT-IR and
DSC analysis indicated that the drug and excipients were
compatible for at least 6 months at room temperature
after production. Microparticle size was between 86 ±
5.63 µm and 184 ± 13.21 µm while mean droplet size of
O/W emulsion was 76 ± 3.45 µm. Release profiles of LRT
from microparticles were significantly different from
those of O/W emulsion, gel and oleageneous cream (p <
0.05). In the case of conventional vehicles, increase in
the hydrophilicity of the vehicles led to increase in
drug release rate. Drug release fitted generally to zero
order kinetics as well as Korsmeyer-Peppas model for one
of the SLM formulations, indicating non-Fickian drug
release (super case II transport).
Conclusion: SLM provided LRT release for a longer period than
the conventional vehicles. However, in vivo studies are
required to ascertain the effectiveness of the
formulations.
Keywords: Loratadine, Solid lipid
microparticles, Allergy, Controlled drug delivery,
Transnasal delivery