These data obtained demonstrated that as the result of optimized physico-chemical properties, drug release rate, cytotoxicity profile, ex vivo permeation enhancement and increased in vivo absorption, nanoparticles prepared from N-aryl derivatives of chitosan can be considered as valuable method for the oral delivery of insulin.
The aim of this research was to develop an artificial neural network (ANN) in order to design a nanoparticulate oral drug delivery system for insulin. The pH of polymer solution (X1), concentration ratio of polymer/insulin (X2) and polymer type (X3) in 3 level including methylated N-(4-N,N- dimethyl aminobenzyl) chitosan, methylated N-(4-pyridinyl) chitosan, and methylated N-(benzyl) chitosan are considered as the input values and the particle size, zeta potential, PdI, and entrapment efficiency (EE %) as output data. ANNs are employed to generate the best model to determining the relationships between input and response values. In this research, a multi-layer percepteron with different topologies has been tested in order to define the one with the best accuracy and performance. The optimization was used by minimizing the error between the predicted and observed values. Three training algorithms (Levenberg-Marquardt (LM), Bayesian-Regularization (BR), and Gradient Descent (GD)) were employed to train ANNs with various numbers of nodes, hidden layers and transfer functions by random selection. The accuracy of prediction data were assayed by the mean squared error (MSE).The ability of all algorithms was in the order: BR>LM>GD. Thus, BR was selected as the best algorithm.
The aim of this study was preparation, optimization and in vitro characterization of nanoparticles composed of 6-[O-carboxymethyl]-[N,N,N-trimethyl] (TMCMC) for oral delivery of low-molecular-weight heparin. The chitosan derivative was synthesized. Nanoparticles were prepared using the polyelectrolyte complexation method. Box-Behnken response surface experimental design methodology was used for optimization of nanoparticles. The morphology of nanoparticles was studied using transmission electron microscopy. In vitro release of enoxaparin from nanoparticles was determined under simulated intestinal fluid. The cytotoxicity of nanoparticles on a Caco-2 cell line was determined, and finally the transport of prepared nanoparticles across Caco-2 cell monolayer was defined. Optimized nanoparticles with proper physico-chemical properties were obtained. The size, zeta potential, poly-dispersity index, entrapment efficiency and loading efficiency of nanoparticles were reported as 235 ± 24.3 nm, +18.6 ± 2.57 mV, 0.230 ± 0.03, 76.4 ± 5.43% and 12.6 ± 1.37%, respectively. Morphological studies revealed spherical nanoparticles with no sign of aggregation. In vitro release studies demonstrated that 93.6 ± 1.17% of enoxaparin released from nanoparticles after 600 min of incubation. MTT cell cytotoxicity studies showed no cytotoxicity at 3 h post-incubation, while the study demonstrated concentration-dependent cytotoxicity after 24 h of exposure. The obtained data had shown that the nanoparticles prepared from trimethylcarboxymethyl chitosan may be considered as a good candidate for oral delivery of enoxaparin.
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