| Abstrakt: |
The oral bioavailability of Artemether (ART) is very poor and erratic due to its limited aqueous solubility and first-pass metabolism by the CYP3A4 isoenzyme. Hence, this investigation aims to develop and characterize ART loaded solid lipid nanoparticles (ART-SLNs) for their particle size distribution, zeta potential, % entrapment efficiency, solid-state properties, and morphology. ART-SLNs were evaluated for stability study in simulated gastric fluids and in vitrorelease. The particle size distribution, zeta potential, % entrapment efficiency of optimized batch (ART-SLN3) were found to be 362.4 ± 1.3 nm, −17.6 ± 0.4 mV and 78.32 ± 0.6%, respectively. DSC thermographs showed molecular dispersion of ART in ART-SLNs. The in vitrorelease profile from ART-SLN3revealed that the release of ART was biphasic pattern first bust released followed by slow-release up to 24 h. Further, In situsingle-pass intestinal permeability study (SPIP) studies were performed on the ileum of Wistar rats. The permeability studies suggested a significant improvement in permeability and absorption constant of ART from ART-SLN3as compared to that of control. Thus, the current study demonstrated that SLNs are a promising approach to overcome both the BCS barriers i.e.dissolution rate and permeability. |
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