Rivastigmine-loaded PLGA and PBCA nanoparticles: Preparation, optimization, characterization, in vitro and pharmacodynamic studies

Effect of RT NPs after intraveneous administration on the escape latency achieved in Morris Water Maze test in saline and scopolamine treated mice. Sustained release nanoparticulate formulations of Rivastigmine tartrate (RT) were prepared, optimized (using factorial design) and characterized using t...

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Bibliographic Details
Published in:	European journal of pharmaceutics and biopharmaceutics Vol. 76; no. 2; pp. 189 - 199
Main Authors:	Joshi, Shrinidh A., Chavhan, Sandip S., Sawant, Krutika K.
Format:	Journal Article
Language:	English
Published:	Amsterdam Elsevier B.V 01-10-2010 Elsevier
Subjects:	Amnesia - drug therapy Animals Biological and medical sciences Biological Transport Brain - metabolism Delayed-Action Preparations Disease Models, Animal Drug Carriers - chemistry Drug Delivery Systems Enbucrilate - chemistry Factorial design General pharmacology In vitro release Lactic Acid - chemistry Maze Learning - drug effects Medical sciences Mice Morris Water Maze Test Nanoparticles Neuroprotective Agents - administration & dosage Neuroprotective Agents - pharmacokinetics Neuroprotective Agents - pharmacology Particle Size PBCA nanoparticles Pharmaceutical technology. Pharmaceutical industry Pharmacology. Drug treatments Phenylcarbamates - administration & dosage Phenylcarbamates - pharmacokinetics Phenylcarbamates - pharmacology PLGA nanoparticles Polyglycolic Acid - chemistry Rivastigmine Rivastigmine tartrate Scopolamine Hydrobromide PBCA nanoparticles In vitro release Rivastigmine tartrate Morris Water Maze Test Factorial design PLGA nanoparticles Water Nanoparticle Psychotropic Esterases Acetylcholinesterase Glycolic acid polymer Lactone polymer Optimization Characterization Rivastigmine Aliphatic polymer Microparticle Anticholinesterase agent Copolymer Release Pharmaceutical technology Enzyme Enzyme inhibitor Antialzheimer agent In vitro Biological activity Carboxylic ester hydrolases Lactic acid polymer Nootropic agent Preparation Hydrolases
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Summary:	Effect of RT NPs after intraveneous administration on the escape latency achieved in Morris Water Maze test in saline and scopolamine treated mice. 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 ± 4.2 nm and PDE of 74.46 ± 0.76 %, whereas PBCA NPS showed PS of 146.8 ± 2.6 nm 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 72 h, 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.
Bibliography:	ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23
ISSN:	0939-6411 1873-3441
DOI:	10.1016/j.ejpb.2010.07.007