Rivastigmine-loaded PLGA and PBCA nanoparticles: Preparation, optimization, characterization, in vitro and pharmacodynamic studies
Abstract
Sustained release nanoparticulate formulations of Rivastigmine tartrate (RT) were prepared, optimized (using factorial design) and characterized using the biodegradable polymers, PLGA and PBCA as carriers. The pharmacodynamic performances of the nanoparticles (NPs) were evaluated for brain targeting and memory improvement in scopolamine-induced amnesic mice using Morris Water Maze Test. PLGA NPs were prepared by nanoprecipitation technique, while PBCA NPs were prepared by emulsion polymerization technique. Effect of key formulation variables on particle size (PS) and percentage drug entrapment (PDE) of NPs was studied by using factorial design. PLGA NPs showed PS of 135.6±4.2nm and PDE of 74.46±0.76 %, whereas PBCA NPS showed PS of 146.8±2.6nm and PDE of 57.32±0.91%. FTIR and GPC characterization confirmed complete polymerization of n-butyl cyanoacrylate (nBCA) monomer into PBCA. DSC thermograms indicated that RT was dispersed as amorphous state in both PLGA and PBCA NPs. TEM studies indicated that the NPs were spherical. In vitro studies showed 30.86±2.07% and 43.59±3.80% release from PLGA and PBCA NPs in 72h, respectively. Pharmacodynamic study demonstrated faster regain of memory loss in amnesic mice with both PLGA and PBCA NPs when compared to RT solution. This indicates rapid and higher extent of transport of RT into the mice brain and thus shows the suitability of both NPs as potential carriers for providing sustained brain delivery of RT.
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In preclinical studies, RT-loaded PLGA and PBCA-80-coated poly(n-butylcyanoacrylate) nanoparticles have shown potential in brain targeting.
“In preclinical studies, RT-loaded poly(lactide-co-gycolide) (PLGA) and polysorbate 80 (PBCA-80)-coated poly(n-butylcyanoacrylate) nanoparticles have shown potential in brain targeting.100”
From Targeted therapy in chronic diseases using nanomaterial-based drug delivery vehicles (2019) · cites this paper as [100]
RT-loaded PLGA and PBCA-80-coated PBCA nanoparticles improved memory faster than RT in solution in the Morris Water Maze test.
“These nanoformulations improved the memory faster than RT in solution, as confirmed by the Morris Water Maze test.100”
From Targeted therapy in chronic diseases using nanomaterial-based drug delivery vehicles (2019) · cites this paper as [100]
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- Authors
- Joshi, S. A., Chavhan, S. S., & Sawant, K. K.
- Affiliations
- Maharaja Sayajirao University of Baroda (IN)
- Corresponding author
- Sawant, Krutika K.
- Venue
- European Journal of Pharmaceutics and Biopharmaceutics
- Publisher
- Elsevier BV
- Published
- 2010-10
- Volume
- 76
- Issue
- 2
- Pages
- 189-199
- ISSN
- 0939-6411 (ISSN-L)
- OpenAlex
- W2054546290
- Cited by
- 235
- References
- 53
- Citations by year
- 2026: 3 · 2025: 3 · 2024: 11 · 2023: 18 · 2022: 14 · 2021: 15 · 2020: 22 · 2019: 22 · 2018: 10 · 2017: 15 · 2016: 18 · 2015: 19 · 2014: 18 · 2013: 26 · 2012: 13
- FWCI
- 10.43
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- European Journal of Pharmaceutics and Biopharmaceutics (publishedVersion)
- PubMed (publishedVersion)
- Funders
- Sun Pharma
- Topics
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
- Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advancements in Transdermal Drug Delivery
- Keywords
- PLGA nanoparticles, sustained drug release, brain targeting, memory enhancement, scopolamine-induced amnesia, nanoprecipitation, emulsion polymerization, encapsulation efficiency, particle size, n-butyl cyanoacrylate, amorphous drug dispersion, factorial design optimization, in vitro drug release
- MeSH terms
- Rivastigmine, Polylactic Acid-Polyglycolic Acid Copolymer, Amnesia, Animals, Biological Transport, Brain, Delayed-Action Preparations, Disease Models, Animal, Drug Carriers, Enbucrilate, Particle Size, Polyglycolic Acid, Scopolamine, Drug Delivery Systems, Neuroprotective Agents, Maze Learning, Lactic Acid, Phenylcarbamates, Mice, Nanoparticles
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