Design and Evaluation of Chitosan Nanoparticles As Novel Drug Carrier for the Delivery of Rivastigmine to Treat Alzheimer‘s Disease

Abstract

Aim: The objective of the study was to develop chitosan nanoparticles of the drug rivastigmine and to study the effect of polysorbate 80 coating on its biodistribution. Results: Chitosan nanoparticles containing rivastigmine were prepared by spontaneous emulsification. The mean size of the particles was 47 ± 4 nm. ζ potential analysis demonstrated a positive charge for the particles and coating with polysorbate 80 slightly reduced the surface charge of the particles. A biphasic release pattern was observed for the release of drug from the nanoparticles. Release of the drug from nanoparticles was diffusion controlled and the mechanism of drug release was Fickian. Conclusion: The biodistribution studies demonstrated that coating of nanoparticles with 1% polysorbate 80 altered the uptake of nanoparticles by different organs.

Biological Safety and Biodistribution of Chitosan Nanoparticles

“…Most studies that have addressed the issue of nanotoxicity of CNPs and chitosan-based nanoparticles have usually performed the biocompatibility studies 2-4 days after intravenous administration in animal models [25,[27][28][29]. However, the toxicities determined by these types of studies, which use short periods of observation for long-circulating dispersed solutions [26,28], may not be fully representative since neither the biodistribution nor the biodegradation processes are completed during these short periods. Nevertheless, studies with longer periods of observation after intravenous administration in subacute or chronic experiments are rare [30], even though long-term observations of the biological effects of dispersed systems are no less important than the analysis of acute toxicity.…”

Formulation, Optimization, <i>in Vivo</i> Pharmacokinetic, Behavioral and Biochemical Estimations of Minocycline Loaded Chitosan Nanoparticles for Enhanced Brain Uptake

“…35) The initial burst release may be due to easy drug diffusion and desorption of surface bound/ free drug. 35,36) The percent drug release was observed to be the greater in case of MHNP (77.46± 1.17%) than cMHNP (73.79± 0.79%) after 24 h (Fig. 8).…”

“…The release rate in the second phase was assumed to be controlled by the diffusion of drug across the polymer matrix of the nanoparticles. 35,36) The in vitro drug release kinetics were characterized by fitting the data of in vitro-release studies of nanoparticles from various batches to standard release kinetics equations (zero order, first-order, Higuchi (M t /M ∞ <0.6), KorsmeyerPeppas model (M t /M ∞ <0.6) and Baker-Lonsdale model, 36) as represented in Table 3. The best fit model for the drug release data was selected on the basis of correlation coefficient.…”

Nanoparticle mediated brain targeted delivery of gallic acid:in vivobehavioral and biochemical studies for improved antioxidant and antidepressant-like activity

“…The cumulative percent release of GA from the nanoparticles in vitro is shown in Table 2. During the in vitro release study of the formulated nanoparticles batches, the initial burst release occurs which may be due to easy drug diffusion and desorption of surface bound/ free drug (Costa & Sousa Lobo, 2001;Nixon, 1983;Wilson et al, 2010Wilson et al, , 2011. Greater percent drug release was observed in case of GANP (85.32 ± 3.76%) than cGANP (76.77 ± 3.89%) after 24 h. Thus coating of nanoparticles with tween 80 slightly decreased the release of drug from the corresponding nanoparticle batch without tween 80 coating which may be attributed to additional barrier layer formed by tween 80 coating although it was not much significant compared to uncoated batches.…”

“…Greater percent drug release was observed in case of GANP (85.32 ± 3.76%) than cGANP (76.77 ± 3.89%) after 24 h. Thus coating of nanoparticles with tween 80 slightly decreased the release of drug from the corresponding nanoparticle batch without tween 80 coating which may be attributed to additional barrier layer formed by tween 80 coating although it was not much significant compared to uncoated batches. The release rate in the second phase is supposed to be controlled mainly by the diffusion of drug across the polymer matrix of the nanoparticles so formulated (Costa & Sousa Lobo, 2001;Nixon, 1983;Wilson et al, 2010Wilson et al, , 2011. The in vitro drug release kinetics were characterized by fitting the data obtained from in vitro-release studies of nanoparticles from various batches to standard drug release kinetics equations (zero order, first-order, Higuchi (M t /M ∞ < 0.6), Korsmeyer-Peppas model (M t /M ∞ < 0.6) and BakerLonsdale model (Costa & Sousa Lobo, 2001) and are represented in Table 2.…”