MCM-41 Nanoparticles for Brain Delivery: Better Choline-Esterase and Amyloid Formation Inhibition with Improved Kinetics

Present study was aimed to deliver a low bioavailability drug, rivastigmine hydrogen tartrate (RTG) to the brain through its encapsulation in Mesoporous silica nanoparticles (MSNs) and targeted to amyloid inhibition in brain. MSNs were characterized for size, zeta potential, and drug entrapment using SEM, TEM, HR-TEM, FT-IR and PXRD. Drug-loaded MSNs were assessed for in vitro release kinetics, ex vivo followed by animal studies. The average size of the prepared blank (MCM-41B) and drug-loaded MSNs (MCM-41L) was 114 ± 2.0 and 145 ± 0.4 nm with the zeta potential of approximately −43.5 ± 1.1 and −37.6 ± 1.4 mV, respectively. MCM-41L exhibited an average entrapment efficiency of 88%. In vitro release studies exhibited early surge followed by a sluggish persistent or constant release (biphasic pattern). Hemolytic studies proved that the developed MCM-41L NPs are less hemolytic compared to RTG. A reduced ThT fluorescence was observed with MCM-41L compared to MCM-41B and RTG in the amyloid inhibition studies. ...