الخلاصة
ABSTRACT: The aim of this study was to develop oil in water
nanoemulsion of nimodipine intended for oral use. Nimodipine is a calcium
channel blocker that has poor oral bioavailability (3-30%) due to its low
solubility and first- pass metabolism. So, nanoemulsion of nimodipine
increase its solubility and enhance its oral bioavailability. Pseudo -ternary
phase diagrams were made by using aqueous titration method.
Nanoemulsions of pseudo-ternary phase diagrams composed of S mix
(mixture of surfactant and co- surfactant), oil and deionized water. These
nanoemulsions subjected for thermodynamic stability tests in order to select
optimized formulations. Nimodipine nanoemulsions were subjected for
characterizations studies in order to select the optimized formula. The
characterizations studies explain that the optimized formula NE5 composed
of 0.6% of nimodipine, 25% of S mix (2:1) that mean (16.66% tween 20:
8.33% PEG400), 10% of oleic acid and 64.4% of deionized water. The
optimized formula NE5 characterized by droplet size (50 – 81.2 nm),
polydispersity index (0.01), pH value (6.51), higher zeta potential (- 45.6
mV), drug content (98.9%), low viscosity and in vitro release of nimodipine
was significantly higher (P<0.05) for NE5. Scanning probe microscopy
(SPM) study confirms that the droplet size of NE5 was in nanoscale. It can
be concluded that the optimized formula (nimodipine NE5) was a promising
formula of nanoemulsion to enhance the oral bioavailability of nimodipine. |