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Optimization of brain targeted chitosan nanoparticles of Rivastigmine for improved efficacy and safety
- Nagpal, Kalpana, Singh, S.K., Mishra, D.N.
- International journal of biological macromolecules 2013 v.59 pp. 72-83
- brain, chitosan, drugs, nanoparticles, particle size, zeta potential
- The study aims at formulation and optimization brain targeted nanoparticles (NP) of Rivastigmine (RT) to improve its therapeutic potential and to verify its safety profile. The NP were optimized using a two factor three level (3²) central composite design aiming to minimize particle size; maximize zeta potential and drug entrapment efficiency of NP. The optimized formulation (cRTNP) was evaluated using in vitro drug release study; in vivo behavioral, and biochemical and maximum tolerated dose (MTD) study. The optimized formulation evidenced a significant reversal of scopolamine-induced amnesia by Tween 80® coated nanoparticles as compared to both pure RT as well as uncoated nanoparticles. The MTD of RT was increased by 10% by formulating them as cRTNP. Thus, formulation of RT as cRTNP improved the therapeutic and safety profile of RT.