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Development and characterization of lipid nanocarriers for spironolactone delivery: A comparative study of solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC)
International Conference and Expo on Biopharmaceutics
Spironolactone (SP), a synthetic steroidal diuretic, is a poorly water-soluble drug with a low and variable oral bioavailability.
Regarding the good solubility of SP in lipid materials, SP loaded solid lipid nanoparticles (SP-SLNs) and nanostructured lipid
carrier (SP-NLCs) were thus prepared in this work for accelerating dissolution of this drug. The SP loaded on NLC was prepared
with stearic acid (SA) as solid lipid and a different oleic acid (OA) as liquid lipid content but SLN were prepared without OA by
probe ultra-sonication method. By increasing the percentage of OA from 0 to 30 wt% in SLN/NLC, the average size and zeta
potential of nanoparticles decreased and the entrapment efficiency (EE%) rose dramatically. The obtained micrograph particles
showed pronounced spherical shape with smooth surface. Differential Scanning Calorimeter (DSC) measurements indicated that
the presence of OA reduced the melting temperature and melting enthalpy of solid lipid in NLC structure. The results reflected good
long-term stability of the nanoparticles and the measurements show that the particle size remains lower in NLC compared to SLN
formulations, 6 months after production. Dissolution of SP-SLN and SP-NLC was about 5.1 and 7.2 times faster than raw drugs in 120
min, respectively. These results indicated that the SP loaded NLC containing 70:30 solid lipid to liquid lipid ratio is a suitable carrier
of SP with improved drug EE and steady drug release properties.