| Bortezomib (BTZ), a proteasome inhibitor, is clinically used for the treatment of multiple
myeloma and mantle cell lymphoma via intravenous or subcutaneous administration. Since BTZ
has limited intestinal permeability, in this study, solid lipid nanoparticles (SLNs) were selected as
lipid carrier to improve the intestinal permeability of BTZ. The nanoparticles were prepared by hot
oil-in-water emulsification method and characterized for physicochemical properties. Moreover, in
situ single-pass intestinal perfusion technique was used for intestinal permeability studies. Mean
particle size of the BTZ-loaded solid lipid nanoparticles (BTZ-SLNs) was 94.6 ± o.66 nm with a
negative surface charge of -18 ± 11 mV. The entrapment efficiency of the BTZ-SLNs was 68.3 ±
3.7% with a drug loading value of 0.8 ± 0.05%. Cumulative drug release (%) over 48 h, indicated a
slow release pattern for nanoparticles. Moreover, the SEM image showed a spherical shape and
uniform size distribution for nanoparticles. Also, FTIR analysis indicated that BTZ was
successfully loaded in the SLNs. The results of the intestinal perfusion studies revealed an
improved effective permeability for BTZ-SLNs with a Peff value of about 3-fold higher than plain
BTZ solution |