Optimization of Rivastigmine Chitosan Nanoparticles for Neurodegenerative Alzheimer; In Vitro and Ex Vivo Characterizations

El-Assal, Mona I.A.; Samuel, Dalia

doi:10.22159/ijpps.2022v14i1.43145

Cited by 17 publications

(15 citation statements)

References 40 publications

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“…Tinctures with optical activity above the upper value (|α°|≥2.21°) of the interval were unstable dispersed systems with low values of the electrokinetic potential (|ξ|≪25mV), because of the presence of large unstable particles of the dispersed phase with sizes matching the micrometer range [10,16]. These particles interfered with polarimetric measurements, and they were also excluded from consideration.…”

Section: Resultsmentioning

confidence: 99%

“…The study of alcohol and water dilutions showed that the latter had greater stability. Water dilutions had electro kinetic potentials higher than the limiting values of the stability of the colloidal system (25 mV) [10,16] and reached-34 mV. It was reasonable to assume that stable nanoparticles in aqueous dilutions would freely penetrate cells (for example, due to pinocytosis) and transport biologically active substances.…”

Section: Resultsmentioning

confidence: 99%

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Polarimetry and Dynamic Light Scattering in Quality Control of Cardiotonic and Hypotensive Tinctures

et al. 2022

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Objective: To substantiate the possibility of using polarimetry to control the quality of tinctures as an additional pharmacopoeial method. Methods: The polarimetric method (POL-1/2, Atago, Japan, the measurement accuracy of±0.002 °) was used to measure the optical activity (α °) of motherwort, valerian and hawthorn tinctures. The dynamic light scattering method (DLS; Zetasizer Nano ZS, Malvern, UK) was used to assess the stability of alcoholic and aqueous dilutions of tinctures according to the intensity of dynamic light scattering dependent on the size (d, nm) of the dispersed phase particles and the values of the electrokinetic potential (ξ, mV). Results: For the first time in this investigation, the polarimetry approach was proposed to evaluate the cardiotonic and hypotensive tinctures' quality and for their identification. Valerian tincture, dilution 1:40,-0.10°<α°<-0.89°; motherwort, tincture-dilution 1:10,-0.10°<α°<-2.21°; hawthorn, tincture without dilution,-0.76°<α°<-1.55°-these are the acceptable ranges of optical activity (α°) of their alcohol dilutions. Beyond these intervals, the use of the polarimetric approach is impossible. Values of optical activity below 0.1 correspond to too low a content of optically active components. Tinctures with optical activity above the upper value of the interval were unstable dispersed systems with low values of the electrokinetic potential (|ξ|≪25mV) and micron particle sizes. Reference tinctures were made from raw materials (Leonurus cardiaca L.) to verify the results. The quality parameters: optical activity (α°), spectra of dynamic light scattering by intensity, volume, and number ("I-d"; "V-d"; "N-d"), electrokinetic potential (ξ) values, and photon pulse count per second (Count Rate, kcps) corresponded to the results obtained for pharmaceutical dosage forms. Conclusion: The permissible intervals of optical activity (α°) of their ethanol dilutions, as well as their relationships with the particle size of the dispersed phase and the values of the electrokinetic potential, were established for the first time to evaluate the quality of tinctures. The obtained results show that polarimetry can be recommended as an additional pharmacopoeial quality control method for tinctures.

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Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

Polarimetry and Dynamic Light Scattering in Quality Control of Cardiotonic and Hypotensive Tinctures

et al. 2022

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“…Chitosan nanoparticles loaded with rivastigmine were used to target the brain through skin permeation [ 262 ]. Drug loading, ex-vivo skin permeation and kinetic studies were conducted to determine the stability over three months at different temperatures.…”

Section: Therapymentioning

confidence: 99%

“…Ex vivo studies revealed that the RVG-chitosan nanoparticles in gel formulae were not irritating to rat skin and had better skin permeation than chitosan nanoparticles’ aqueous dispersion. The chitosan nanoparticles also were capable of releasing RVG in a sustained manner and increasing the time release of the drug [ 262 ]. Another report compared liposomal formulations and observed that chitosan-coated liposomes have a better and longer release pattern than conventional liposomes.…”

Section: Therapymentioning

confidence: 99%

Amyloid β, Lipid Metabolism, Basal Cholinergic System, and Therapeutics in Alzheimer’s Disease

Campos-Peña

Pichardo-Rojas

Sánchez-Barbosa

et al. 2022

IJMS

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The presence of insoluble aggregates of amyloid β (Aβ) in the form of neuritic plaques (NPs) is one of the main features that define Alzheimer’s disease. Studies have suggested that the accumulation of these peptides in the brain significantly contributes to extensive neuronal loss. Furthermore, the content and distribution of cholesterol in the membrane have been shown to have an important effect on the production and subsequent accumulation of Aβ peptides in the plasma membrane, contributing to dysfunction and neuronal death. The monomeric forms of these membrane-bound peptides undergo several conformational changes, ranging from oligomeric forms to beta-sheet structures, each presenting different levels of toxicity. Aβ peptides can be internalized by particular receptors and trigger changes from Tau phosphorylation to alterations in cognitive function, through dysfunction of the cholinergic system. The goal of this review is to summarize the current knowledge on the role of lipids in Alzheimer’s disease and their relationship with the basal cholinergic system, as well as potential disease-modifying therapies.

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“…One of the main applications of nanotechnology is the nano-encapsulation of bioactive compounds for biological purposes. During the nano-encapsulation process, besides bioactive protection, their bioavailability also is improved due to an increase in the surface-to-volume ratio by reducing particle size into the nano-range [10].…”

Section: Introductionmentioning

confidence: 99%

Development and Optimization of Astragalin-Loaded Polymeric Nanoparticles Using Central Composite Factorial Design

Kalidas

GEETHA

2022

Int J App Pharm

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Objective: The objective of the present study was to develop and optimize Astragalin-loaded polymeric nanoparticles (AST-NPs) using a central composite factorial design (CCD). Methods: AST-NPs were prepared by the dialysis method. CCD was employed to study the influence of formulation factors, polymer concentration, aqueous organic phase ratio, and process parameter stirring time on dependent physicochemical characteristics, particle size, zeta potential, and percentage entrapment efficiency (%EE) of the drugs. The optimized formulation was evaluated for in vitro release studies and subjected to stability studies. Results: Polymer concentration and process parameters were optimized to produce nanoparticles with desired parameters. The prepared NPs were characterized by Fourier transmission infrared (FT-IR), differential scanning calorimetry (DSC), drug loading, entrapment efficiency, particle size, zeta potential, and in vitro studies. FT-IR and DSC studies indicated that there was no interaction between the drug and polymer. The optimized NPs exhibits stability. Optimized NPs exhibited spherical and porous surfaces with a mean PS of 118 nm, the zeta potential of-25 mV, and %EE of 89%. Conclusion: Astragalin-loaded nanoparticles prepared with optimized formulation composition and process parameters.

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Optimization of Rivastigmine Chitosan Nanoparticles for Neurodegenerative Alzheimer; In Vitro and Ex Vivo Characterizations

Cited by 17 publications

References 40 publications

Polarimetry and Dynamic Light Scattering in Quality Control of Cardiotonic and Hypotensive Tinctures

Polarimetry and Dynamic Light Scattering in Quality Control of Cardiotonic and Hypotensive Tinctures

Amyloid β, Lipid Metabolism, Basal Cholinergic System, and Therapeutics in Alzheimer’s Disease

Development and Optimization of Astragalin-Loaded Polymeric Nanoparticles Using Central Composite Factorial Design

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