Cited by 116Advanced Drug Delivery SystemsNanoparticle-Based Drug DeliveryCholinesterase and Neurodegenerative Diseases

Optimization of brain targeted chitosan nanoparticles of Rivastigmine for improved efficacy and safety

Nagpal, Kalpana, Singh, S.K., Mishra, D.N.·2013·International Journal of Biological Macromolecules

Abstract

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 (3(2)) 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.

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Crossref · 10.1016/j.ijbiomac.2013.04.024

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Authors
Nagpal, K., Singh, S. K., & Mishra, D. N.
Affiliations
Guru Jambheshwar University of Science and Technology (IN)
Corresponding author
Nagpal, Kalpana
Venue
International Journal of Biological Macromolecules
Publisher
Elsevier BV
Published
2013-08
Volume
59
Pages
72-83
ISSN
0141-8130 (ISSN-L)
OpenAlex
W2024268060
Cited by
116
References
32
Citations by year
2026: 8 · 2025: 10 · 2024: 11 · 2023: 16 · 2022: 10 · 2021: 10 · 2020: 16 · 2019: 6 · 2018: 5 · 2017: 6 · 2016: 7 · 2015: 7 · 2014: 3 · 2013: 1
FWCI
3.61
Type
journal article
Language
en
Open access
closed
Locations
  • International Journal of Biological Macromolecules (publishedVersion)
  • PubMed (publishedVersion)
Topics
  • Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
  • Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
  • Health Sciences › Medicine › Pharmacology › Cholinesterase and Neurodegenerative Diseases
Keywords
rivastigmine, chitosan nanoparticles, brain drug delivery, central composite design, scopolamine-induced amnesia, maximum tolerated dose, encapsulation efficiency, zeta potential, particle size, in vitro drug release, Alzheimer's disease
MeSH terms
Rivastigmine, Amnesia, Animals, Behavior, Animal, Body Weight, Brain, Dose-Response Relationship, Drug, Drug Carriers, Drug Compounding, Drug Evaluation, Preclinical, Factor Analysis, Statistical, Male, Memory, Polysorbates, Scopolamine, Treatment Outcome, Neuroprotective Agents, Maze Learning, Chitosan, Phenylcarbamates, Mice, Rats, Nanoparticles

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