GABA and 5-HT chitosan nanoparticles enhanced liver cell proliferation and neuronal survival in partially hepatectomised rats: GABAB and 5-HT2A receptors functional

Nanoparticulate drug delivery systems provide wide opportunities for solving problems associated with drug stability or disease states and create great expectations in the area of drug delivery (Bosselmann & Williams, 2012). Nanotechnology, in a simple way, explains the technology that deals with one billionth of a meter scale (Ochekpe, et al., 2009). Fewer side effects, poor bioavailability, absorption at intestine, solubility, specific delivery to site of action with good pharmacological efficiency, slow release, degradation of drug and effective therapeutic outcome, are the major challenges faced by most of the drug delivery systems. To a great extent, biopolymer coated drug delivery systems coupled with nanotechnology alleviate the major drawbacks of the common delivery methods. Chitosan, deacetylated chitin, is a copolymer of β-(1, 4) linked glucosamine (deacetylated unit) and N- acetyl glucosamine (acetylated unit) (Radhakumary et al., 2005). Chitosan is biodegradable, non-toxic and bio compatible. Owing to the removal of acetyl moieties that are present in the amine functional groups of chitin, chitosan is readily soluble in aqueous acidic solution. The solubilisation occurs through the protonation of amino groups on the C-2 position of D-glucosamine residues whereby polysaccharide is converted into polycation in acidic media. Chitosan interacts with many active compounds due to the presence of amine group in it. The presence of this active amine group in chitosan was exploited for the interaction with the active molecules in the present study. Nanoparticles of chitosan coupled drugs are utilized for drug delivery in eye, brain, liver, cancer tissues, treatment of spinal cord injury and infections (Sharma et al., 2007; Li, et a., 2009; Paolicelli et al., 2009; Cho et al., 2010). To deliver drugs directly to the intended site of action and to improve pharmacological efficiency by minimizing undesired side effects elsewhere in the body and decrease the long-term use of many drugs, polymeric drug delivery systems can be used (Thatte et al., 2005).

Highly Stable, Edible Cellulose Films Incorporating Chitosan Nanoparticles

The need for biodegradable polymers for packaging has fostered the development of novel, biodegradable polymeric materials from natural sources, as an alternative to reduce amount of waste and environmental impacts. The present investigation involves the synthesis of chitosan nanoparticles-carboxymethylcellulose films, in view of their increasing areas of application in packaging industry. The entire process consists of 2-steps including chitosan nanoparticles preparation and their incorporation in carboxymethylcellulose films. Uniform and stable particles were obtained with 3 different chitosan concentrations. The morphology of chitosan nanoparticles was tested by transmission electron microscopy, revealing the nanoparticles size in the range of 80 to 110 nm. The developed film chitosan nanoparticles-carboxymethylcellulose films were characterized by Fourier transform infrared spectroscopy (FT-IR), thermogravimetric analysis, solubility tests, and mechanical analysis. Improvement of thermal and mechanical properties were observed in films containing nanoparticles, with the best results occurring upon addition of nanoparticles with 110 nm size in carboxymethylcellulose films. Practical Application Carboxymethylcellulose films containing chitosan nanoparticles synthesized and characterized in this article could be a potential material for food and beverage packaging applications products due to the increase mechanical properties and high stability. The potential application of the nanocomposites prepared would be in packaging industry to extend the shelf life of products.

Development of ligand incorporated chitosan nanoparticles for the selective delivery of 5-fluorouracil to colon

Drug delivery systems with active targeting ligand provide improved therapeutic efficiency due to the selectivity towards tumor cells. In this paper we prepared drug loaded nanoparticles (NPs) using folate (FA) incorporated chitosan (FA-CS) based on ionic gelation technology. FA-CS NPs were spherical in shape with an average particle size of 100 nm, while 5-fluorouracil (5-FU) loaded NPs became less circular with average particle size of 100-500 nm. NPs made from FA-CS conjugates exhibited improved capability to encapsulate hydrophilic 5-FU. It was found 5-FU distributed in FA-CS NPs in solid solution state. In vitro release results demonstrated the release of 5-FU from FA-CS NPs was more controllable as compared to that of CS NPs.

Formulation of vanillin cross-linked chitosan nanoparticles and its characterization.

Chitosan nanoparticles were successfully prepared by chemical cross-linking with vanillin. The nanoparticles were spherical in shape with smooth surface, and the average particle size of chitosan nanoparticles was 141 nm. The formulation of chitosan nanoparticles is based on Shiff reaction between aldehyde group of vanillin and amino group of chitosan. Chitosan nanoparticles prepared by crosslinking with vanillin are promising vehicle for the drug delivery of various anticancer drugs in the chemotherapy of cancers.

Microencapsulation of coupled folate and chitosan nanoparticles for targeted delivery of combination drugs to colon

Folate-chitosan nanoparticles, co-loaded with 5-fluourouacil (5-FU) and leucovorin (LV) and prepared by ionic gelation technology were physically microencapsulated by enteric polymer using a solvent evaporation method. Average particle size of the microencapsulated particles was in the range of 15 to 35 µm. High drug encapsulation efficiency was obtained for both 5-FU and LV in the microencapsulated particles. Both drugs were in amorphous state in the microencapsulated particles. By enteric coating, excellent pH-dependent release profile was achieved and no drug release was observed in simulated gastric and intestinal fluids. However, when the pH value reached the soluble threshold of Eudragit S-100, a constant and slow drug release was observed. The results indicated that these microencapsulated particles are a promising vehicle for selectively targeting drugs to colon in the chemotherapy of colon cancer.

Evaluation of the Genotoxicity of Chitosan Nanoparticles for Use in Food Packaging Films

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Paraquat-loaded alginate/chitosan nanoparticles: Preparation, characterization and soil sorption studies

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Development of Novel Guava Puree Films Containing Chitosan Nanoparticles

One of the overall goals of industries is to use packages that do not cause environmental problems at disposal time, but that have the same properties as the conventional ones. The goal of this study is to synthesize edible films based on hydroxypropyl methylcellulose (HPMC) with guava puree and chitosan (CS) nanoparticles. This was divided into two stages, the first is the synthesis of chitosan nanoparticles and the second is the production of the films. For the nanoparticles, average size and zeta potential measurements were performed. The characterizations of mechanical and thermal properties, solubility and water vapor permeability tests were conducted in the films. It was observed that when the nanoparticles were added to HPMC and guava puree films, they improved their mechanical and thermal properties, as well as decreased the films solubility and permeability. The potential application of the films prepared would be in edible films with flavor and odor to extend the shelf life of products.

Chitosan nanoparticles for non-viral gene therapy

The cationic polysaccharide chitosan has been widely used for non-viral transfection in vitro and in vivo and has many advantages over other polycations. Chitosan is biocompatible and biodegradable and protects DNA against DNase degradation. However following administration the ChitosanDNA polyplexes must overcome a series of barriers before DNA is delivered to the cell nucleus. This paper describes the most important parameters involved in the chitosan-DNA interaction and their effects of on the condensation, shape, size and protection of DNA. Strategies developed for chitosanDNA polyplexes to avoid non-specific interaction with blood components and to overcome intracellular obstacles as the crossing of die cell membrane, endosomal escape and nuclear import are presented. © 2006 American Chemical Society.

N,N,N-trimethyl chitosan nanoparticles as a vitamin carrier system

There is considerable interest in incorporating stabilized vitamins into biopolymeric nanoparticles, especially in the development of carriers and active systems for pharmaceutical and food applications. Amongst biopolymer, chitosan is highly desirable owing to its good biocompatibility, biodegradability and ability to be chemically modified. In this paper, nanoparticles from three kinds of water-soluble derivative chitosan (N,N,N-trimethyl chitosan, TMC) have successfully been synthesized by ionic gelation with tripolyphosphate (TPP) anions. Combinations of concentrations of TMC and TPP have resulted in nanoparticles with varying sizes for which the capability for loading with vitamins was investigated. Zeta potential measurement and particle size analysis demonstrated that the size of the nanoparticles wasoptimized (196±8nm) when the lowest TMC and TPP amounts were used, i.e., 0.86mgmL -1 and 0.114mgmL -1 respectively. As the TMC and/or the TPP concentrations increase, the resulting size of the nanoparticles increases considerably. Three different vitamins (B9, B12 and C) were tested as additives and the final system characterized in relation to size, morphology, spectroscopic and zeta potential properties. In general, the incorporation of vitamins increased all the TMC-TPP original nanoparticle sizes, reaching a maximum diameter of 534±20nm when loaded with vitamin C. The presence of vitamins also decreases the zeta potential, with one exception observed when using vitamin C. The preliminary results of this study suggested that all TMC/TPP nanoparticles can be successfully used as a stable medium to incorporate and transport vitamins, with potential applications in foodstuffs. © 2011 Elsevier Ltd.

Preparation and Characterization of Chitosan Nanoparticles for Zidovudine Nasal Delivery

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Factorial design and characterization studies for articaine hydrochloride loaded alginate/chitosan nanoparticles

Nowadays, articaine hydrochloride (ATC) is a local anesthetic widely used in dental procedures, but its side effects include paresthesia and nerve injury. Alginate/chitosan nanoparticles (AG/CSnano) can be used as carrier for drugs, overcoming the problems. The aim of this work was to evaluate the factors (Calcium/alginate [Ca2+:AG] and Chitosan/alginate [CS:AG] mass ratios) influence on the average size, polydispersity index, zeta potential and encapsulation efficiency of ATC. AG/CSnano containing ATC were prepared by ionic pregelation method. A three-level factorial design was carried out and the factors varied were Ca2+/AG mass ratio and CS/AG mass ratio. There were obtained nanoparticles with size range of 340–550 nm and polydispersity index between 0.2 and 0.5, zeta potential range –19 and –22 mV and encapsulation efficiency of ATC in AG/Csnano between 22 and 45%. According to the results, the average size, polydispersity index and encapsulation efficiency were significantly affected to the variation of Ca2+/AG and CS/AG mass ratio, but the zeta potential didn't change significantly with factor variations. The factorial design showed it was possible to identify formulations that presented better results for the parameters measured. The factor chosen for the suitable formulations was the encapsulation efficiency. Through this parameter, one formulation was chosen with highest encapsulation efficiency of ATC and presented good colloidal stability parameters aiming future clinical applications.

Chitosan nanoparticles loaded the herbicide paraquat: The influence of the aquatic humic substances on the colloidal stability and toxicity

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Entrapment characteristics of hydrosoluble vitamins loaded into chitosan and N,N,N-trimethyl chitosan nanoparticles

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)