| Rivastigmine hydrogen tartrate (RHT), one of the potential cholinesterase inhibitors, has received great
attention as a new drug candidate for the treatment
of Alzheimer's disease. However, the bioavailability of
RHT from the conventional pharmaceutical forms is low because
of the
presence
of the blood brain barrier.
The main aim of the present study was to prepare positively charged Eudragit RL 100 nanoparticles as a
model scaffold for providing a sustained release profil
e for RHT. The formulations were evaluated in terms
of particle size, zeta potential,
surface morphology, X-ray diffraction (XRD),
Fourier transform infrared
spectroscopy
(FTIR),
and differential scanning calorimetry (D
SC). Drug entrapment efficiency and
in vitro
release properties of lyophilized nanoparticles were also
examined. The resulting formulations were found to
be in the size range of
118 nm to 154 nm and zeta potential was positive (+22.5 to 30 mV). Nanoparticles
showed
the entrapment efficiency from 38.40 ± 8.94 to 62.00
± 2.78%. An increase in the mean particle size
and the entrapment efficiency was observed with an
increase in the amount of polymer. The FTIR, XRD, and
DSC results ruled out any chemical interaction between the drug and Eudragit RL100 polymer. RHT
nanoparticles containing low ratio of polymer to drug (4:1) presented a faster drug release and on the
contrary, nanoparticles containing high ratio of polymer to
drug (10:1) were able to give a more sustained
release of the drug. The study revealed that RHT na
noparticles were capable of releasing the drug in a
prolonged period of time and increasing the drug bioavailability. |