Formation Of Chitosan Nanoparticles Research Articles

Characterization of behavior of the inclusion complex between Sulfobutylether-β-cyclodextrin loaded alginate/chitosan nanoparticles and indomethacin as a potential approach for drug delivery

Indomethacin (IND) is a nonsteroidal anti-inflammatory drug with low aqueous solubility and irritating gastrointestinal side effects. By complexing this drug inside the cavity of cyclodextrin (CD) and loading it into polymer nanoparticles such as Chitosan (CS) and Alginate (Alg), in addition to increasing its solubility, a targeted drug delivery platform can be created to release this drug. In this study, initially, the complex of IND with Sulfobutylether-β-cyclodextrin (SBE-β-CD) was created using the freeze-drying method. Then, by ionic gelation method, the complex was loaded into CS nanoparticles, and finally, these nanoparticles were coated with Alg to enable drug release in the intestinal environment. Complexes and nanoparticles formation were investigated by phase solubility, FTIR, HNMR, XRD, and SEM methods. Moreover, the Zeta potential method was used to measure the stability of nanoparticles coated with Alg. According to phase solubility studies, drug solubility increased linearly with increasing CD concentration, indicating an AL-type system. In addition, according to the phase solubility diagram, the stability constant and complexation efficiency were obtained 177 M−1 and 0.388, respectively. In the following, the formation of chitosan nanoparticles was confirmed through spectral shifts observed in FTIR analysis as well as morphological changes revealed in SEM analysis. Also, the zeta potential of Alg coated nanoparticles was 110.067 mV, which indicates the good stability of these nanoparticles. At the end, in vitro release studies were conducted to investigate the pH-sensitive capability of these nanoparticles at pH = 1.5 and pH = 7. The formed nanosystem successfully released 78.51 % of the drug at pH = 7 and prevented its release in acidic pH.

ISOLATION AND CHARACTERIZATION OF CHITOSAN NANOPARTICLES FROM CRAB SHELL WASTE (PORTUNUS PELAGICUS)

Objective: The purpose of this study was to isolate and characterize of chitosan nanoparticles derived from Portunus pelagicus shell waste. Methods: Chitosan was isolated by deproteination, demineralization, and deacetylation methods. Furthermore, nanoparticles (NPs) were made by the ionic gelation method by dissolving chitosan in a mixture of acetic acid and sodium tripolyphosphate. The particle size analyzer and Fourier Transform Infrared Spectroscopy were used to measure the particle size of NPs and determine the functional group and degree of deacetylation. Results: The yield percentage of chitosan was 90.7%. The size of chitosan nanoparticles based on the highest intensity is 15.05 nm with a polydispersity index (PDI) value of 0.1140 at a concentration of 1%. Based on the degree of deacetylation of chitosan nanoparticles, it was found to be 84.98% at 1% concentration. Conclusion: The conclusion of this study is the formation of chitosan nanoparticles (1-100 nm) isolated from Portunus pelagicus shell waste. Based on the degree of deacetylation, chitosan nanoparticles with high chitosan content (>75%) were obtained.

Development and Evaluation of Chitosan Nanoparticles for Ocular Delivery of Tedizolid Phosphate.

This study investigates the development of topically applied non-invasive chitosan-nanoparticles (CSNPs) for ocular delivery of tedizolid phosphate (TZP) for the treatment of MRSA-related ocular and orbital infections. An ionic-gelation method was used to prepare TZP-encapsulated CSNPs using tripolyphosphate-sodium (TPP) as cross-linker. Particle characterization was performed by the DLS technique (Zeta-Sizer), structural morphology was observed by SEM. The drug encapsulation and loading were determined by the indirect method. In-vitro release was conducted through dialysis bags in simulated tear fluid (pH 7) with 0.25% Tween-80. Physicochemical characterizations were performed for ocular suitability of CSNPS. An antimicrobial assay was conducted on different strains of Gram-positive bacteria. Eye-irritation from CSNPs was checked in rabbits. Transcorneal flux and apparent permeability of TZP from CSNPs was estimated through excised rabbit cornea. Ionic interaction between the anionic and cationic functional groups of TPP and CS, respectively, resulted in the formation of CSNPs at varying weight ratios of CS/TPP with magnetic stirring (700 rpm) for 4 h. The CS/TPP weight ratio of 3.11:1 with 10 mg of TZP resulted in optimal-sized CSNPs (129.13 nm) with high encapsulation (82%) and better drug loading (7%). Release profiles indicated 82% of the drug was released from the TZP aqueous suspension (TZP-AqS) within 1 h, while it took 12 h from F2 to release 78% of the drug. Sustained release of TZP from F2 was confirmed by applying different release kinetics models. Linearity in the profile (suggested by Higuchi’s model) indicated the sustained release property CSNPs. F2 has shown significantly increased (p < 0.05) antibacterial activity against some Gram-positive strains including one MRSA strain (SA-6538). F2 exhibited a 2.4-fold increased transcorneal flux and apparent permeation of TZP as compared to TZP-AqS, indicating the better corneal retention. No sign or symptoms of discomfort in the rabbits’ eyes were noted during the irritation test with F2 and blank CSNPs, indicating the non-irritant property of the TZP-CSNPs. Thus, the TZP-loaded CSNPs have strong potential for topical use in the treatment of ocular MRSA infections and related inflammatory conditions.

Particle Engineering of Chitosan and Kaolin Composite as a Novel Tablet Excipient by Nanoparticles Formation and Co-Processing.

Chitosan is not a common excipient for direct compression due to poor flowability and inadequate compressibility. Co-processing of chitosan and kaolin is a challenging method to overcome the limitations of the individual excipients. The purpose of the present study was to develop co-processed chitosan–kaolin by the spray drying technique (rotary atomizer spray dryer) and to characterize the excipient properties. The formation of chitosan nanoparticles was the major factor for desirable tablet hardness. The ratio of chitosan/tripolyphosphate of 10:1 and 20:1 had a significant effect on hardness. The successful development of co-processed chitosan–kaolin as a novel tablet excipient was obtained from a feed formulation composed of chitosan and kaolin at a ratio of 55:45 and the optimum chitosan/tripolyphosphate ratio of 20:1. Co-processing altered the physical properties of co-processed chitosan–kaolin in such a way that it enhanced the flowability and tableting performance compared to the physical mixture.

Synthesis and Properties of Chitosan Nanoparticles CrossLinked with Tripolyphosphate

Chitosan nanoparticles (ChNPs) have been extensively examined for various biomedical applications due to their advantages include large surface area, biodegradability, and biocompatibility. The purpose of this research was to synthesize ChNPs using a simple ionic gelation technique by the interaction of low molecular weight chitosan (LMWC) and sodium tripolyphosphate (TPP) as a cross-linking agent. ChNPs, TPP, and LMWC were analysed by X-ray diffraction (XRD) and Fourier transforms infrared (FTIR) spectra that indicated the formation of ChNPs, attributing to the rearrangement of the nanoparticles after adding the TPP cross-linker into the LMWC solution. XRD analysis exhibited that ChNPs were amorphous, due to the effect of TPP cross-linker. Dynamic light scattering showed the nano-dimension of ChNPs with a hydrodynamic size of 68.50 nm. Thus, the obtained results indicated that the properties of chitosan were improved through converting it into nanoparticles using TPP initiated ionic gelation procedure.

Oregano (Origanum vulgar subsp. viride) Essential Oil: Extraction, Preparation, Characterization, and Encapsulation by Chitosan-Carbomer Nanoparticles for Biomedical Application

Background: Plant essential oils (EOs) as natural agents have broad activities, including antibacterial, antifungal, antiviral, insecticidal, and repel activities because of their chemical compositions. Objectives: The objective of this study was to increase the stability of Origanum vulgar subsp. viride EOs by encapsulation in chitosan-carbomer nanoparticles by ionic gelation method. Methods: The EOs from dried leaves of O. vulgar subsp. viride were extracted by hydro-distillation method, and EO components were determined by gas chromatography-mass spectrometry (GC-MS). Besides, OEO-loaded chitosan (CS) nano-capsules were prepared using the ionic gelation method. The molecular structure and morphology of nanoparticles were characterized by Fourier Transform-Infrared (FTIR) and scanning electron microscopy (SEM), respectively. The encapsulation efficiency (EE), loading capacity (LC) of the OEO-loaded CS nanoparticles, and their release profiles were determined using UV/Vis spectrophotometry. Results: The major components of OEO were thymol (20.53%), 4-terpinenol (20.28%), and γ-terpinene (12.22%). The percentages of EE and LC of OEO ranged from 99.25 ± 0.74 to 93.84 ± 0.71 and 38.02 ± 0.18 to 66.73 ± 0.51, respectively, with increasing the OEO to chitosan ratio from 1:0.01 to 1:0.04 W/V. The nanoparticles were regular, uniform, and spherical in shape with an average size of 134 to 181 nm, which were dispersed throughout the solution. The zeta potential values for blank chitosan nanoparticles (CSNPs) and OEO-loaded CSNPs were +23.4 and +38.5 mV, respectively. Conclusions: The results confirmed the suitability of the CS-carbomer complex for OEO- CSNPs formation. It is recommended to evaluate the antimicrobial, insecticidal and insect repel activities of developed OEO nanoparticles in laboratory and field studies.

Entrapment Formulation for env-Tm Gene Based on Chitosan Low Molecular Weight as a Jembrana Disease Virus Vaccine Candidate

Jembrana disease (JD) caused by Jembrana Disease Virus (JDV) becomes an obstacle in Bali cattle (Bos javanicus). The development of JD vaccines has a critical meaning to prevent losses in the B. javanicus in Indonesia and is one of the models in the development of the Human Immunodeficiency Virus (HIV) vaccine. The development of vaccines for JDV has carried out DNA vaccines that are expected to provide better immunological effects. This study aimed to determine the low molecular weight chitosan (LC) entrapment towards pEGFP-C1-env-Tm in the formation of Chitosan Nanoparticles Low/pEGFP-C1-env-Tm complex. The env-Tm gene was inserted in pEGFP-C1 into the pEGFPC1/ env-Tm construct transformed on the E. coli DH5α host. The construct was formulated into LC/pEGFP-C1/env-Tm complex with a low molecular weight chitosan concentration of 0.06 % and the ratio of pEGFP-C1/env-Tm: LC (wt/wt) was 1:0.5-1:3. The complexes were then analyzed by gel retardation assay agarose 1 %. The results of this study indicated that the best entrapment results of low molecular weight chitosan to pEGFPC1/ env-Tm was in the mass ratio of pEGFP-C1/env-Tm: LC was 1:2. The best formulation entrapment for env-Tm by low molecular weight chitosan 0.06 % is in the rate 1:2.

Bioinspired Green Synthesis of Chitosan and Zinc Oxide Nanoparticles with Strong Antibacterial Activity against Rice Pathogen Xanthomonas oryzae pv. oryzae.

Bacterial leaf blight caused by Xanthomonas oryzae pv. oryzae (Xoo) is one of the most devastating diseases, resulting in significant yield losses in rice. The extensive use of chemical antibacterial agents has led to an increase the environmental toxicity. Nanotechnology products are being developed as a promising alternative to control plant disease with low environmental impact. In the present study, we investigated the antibacterial activity of biosynthesized chitosan nanoparticles (CSNPs) and zinc oxide nanoparticles (ZnONPs) against rice pathogen Xoo. The formation of CSNPs and ZnONPs in the reaction mixture was confirmed by using UV-vis spectroscopy at 300–550 nm. Moreover, CSNPs and ZnONPs with strong antibacterial activity against Xoo were further characterized by scanning and transmission electron microscopy, Fourier-transform infrared spectroscopy, and X-ray diffraction. Compared with the corresponding chitosan and ZnO alone, CSNPs and ZnONPs showed greater inhibition in the growth of Xoo, which may be mainly attributed to the reduction in biofilm formation and swimming, cell membrane damage, reactive oxygen species production, and apoptosis of bacterial cells. Overall, this study revealed that the two biosynthesized nanoparticles, particularly CSNPs, are a promising alternative to control rice bacterial disease.

Covalently and ionically, dually crosslinked chitosan nanoparticles block quorum sensing and affect bacterial cell growth on a cell-density dependent manner

In our efforts to improve the quality and stability of chitosan nanoparticles (NPs), we describe here a new type of chitosan NPs dually crosslinked with genipin and sodium tripolyphosphate (TPP) that display quorum quenching activity. These NPs were created using a simplified and robust procedure that resulted in improved physicochemical properties and enhanced stability. This procedure involves the covalent crosslinking of chitosan with genipin, followed by the formation of chitosan NPs by ionic gelation with TPP. We have optimized the conditions to obtain genipin pre-crosslinked nanoparticles (PC-NPs) with positive ς-potential (~ +30 mV), small diameter (~130 nm), and low size distributions (PdI = 0.1–0.2). PC-NPs present physicochemical properties that are comparable to those of other dually crosslinked chitosan NPs fabricated with different protocols. In contrast to previously characterized NPs, however, we found that PC-NPs strongly reduce the acyl homoserine lactone (AHL)-mediated quorum sensing response of an Escherichia coli fluorescent biosensor. Thus, PC-NPs combine, in a single design, the stability of dually crosslinked chitosan NPs and the quorum quenching activity of ionically crosslinked NPs. Similar to other chitosan NPs, the mode of action of PC-NPs is consistent with the existence of a “stoichiometric ratio” of NP/bacterium, at which the positive charge of the NPs counteracts the negative ς-potential of the bacterial envelope. Notably, we found that the time of the establishment of the “stoichiometric ratio” is a function of the NP concentration, implying that these NPs could be ideal for applications aiming to target of bacterial populations at specific cell densities. We are confident that our PC-NPs are up-and-coming candidates for the design of efficient anti-quorum sensing and a new generation antimicrobial strategies.

Impact of the molecular weight on the size of chitosan nanoparticles: characterization and its solid-state application

Chitosan nanoparticles (CSNPSs) were prepared from noncommercial chitosan of different molecular weights by the ionic gelation methodology. CSNPSs were applied in solid state (g) to observe the bacterial growth of Bacillus halotolerans MCC1, bacteria that appear in the biofilms of the desalinization membranes. Characterization of CSNPS of high (CSNP2), medium (CSNP3), and low (CSNP4) molecular weight (MW) was studied by TGA, DSC, SEM, EDX, DLS, and XRD. The effect of MW onto the formation of CSNPS was investigated as well as the effect of its application (0.01, 0.03, and 0.03 g at 24, 48, and 72 h) in the growth (%) of B. halotolerans MCC1. The results showed that the average size of CSNPS was in the range of 420–600.3 nm. CSNPS were considered amorphous and less thermally stable than the original chitosan where they were produced. Morphologically when the MW decreases, a reduction in the size of the particle was exhibited. When MW increase a reduction in the zeta potential from 45.7 to 29.9 mV was resulted. The essays to observe the growth (%) of B. halotolerans MCC1 indicated that CSNPS applied in solid state allows the growth of the bacteria; when the MW decreases, the growth of the bacteria increases. The maximum and minimum value of growth was obtained at 72 h, with the use of 0.05 g of CSNP4 (16.86%) and 0.05 g of CSNP2 (2.15%), respectively. The use of CSNPS indicates that the inhibitory effect depends on the MW as well as the doses of application.

Green Synthesis and Evaluation of Dimocarpus longan Leaves Extract Based Chitosan Nanoparticles against Periodontitis Triggering Bacteria

Present study was intended to synthesize and evaluate the Dimocarpus longan leaves aqueous extract (DLLAE) based chitosan nanoparticles (CSNPs) against periodontitis triggering bacteria. In present study the DLLAE was prepared by extracting D. Longan leaves in distilled water using decoction method. The prepared DLLAE was subjected to phytochemical investigations, total phenolic content, total flavonoid content study and CSNPs synthesis. The CSNPs were characterized (using UV-visible, FT-IR, SEM, FESEM, XRD and EDX) and evaluated for their potential against periodontitis triggering bacteria (using agar well diffusion method). The phytochemical investigations over DLLAE exhibited presence of monosaccharides, reducing sugars, proteins, steroids, anthraquinones and coumarins glycosides, flavonoids, alkaloids, organic acid, tannic and phenolic compounds. The CSNPs were formed using DLLAE when the colour changed from white to pale brown. Absorbance of the CSNPs was in the desired range (201-310 nm). The optimization study revealed 1% acetic acid, 1% sodium alginate, 2 mg/mL chitosan, pH 5.8 and 1 mL DLLAE as the standard requirement for CSNPs synthesis using DLLAE. The CSNPs characterization data of FT-IR exhibited shifted bands. The FESEM revealed that the synthesized CSNPs were spherical in shape and their size ranged from 74.66 to 94.07 nm. The XRD data showed peaks at 2θ values of 22.28º, 25.19º, 34.72º, 40.0º, 71.16º and 73.0º. The average size for CSNPs was between 30.11-62.98 nm. The EDX spectrum revealed signal for carbon (76.17%), oxygen (22.14%) and sodium (1.53%) which confirmed formation of CSNPs. The antibacterial activity revealed high inhibitory potential of green CSNPs against S. aureus. Present studies establish that CSNPs biosynthesis using D. longan leaves aqueous extract is an efficient method and the biosynthesized CSNPs possess high antibacterial potential against S. aureus (bacteria that triggers periodontitis).

Role of proton balance in formation of self-assembled chitosan nanoparticles.

Researchers have explored the ability of chitosan to form nanoparticles, to suit varying applications, ranging from wound-healing to gene delivery. Ionic gelation is a widely used method for formulating chitosan nanoparticles, where self-assembly plays a crucial role. This self-assembly is initially promoted by hydrophilic-hydrophobic parity amongst individual chitosan residues, along with electrostatic and Van der Waals interactions with the cross-linker. However, until now the intrinsic ability of chitosan to self-assemble is not widely studied; hence, we investigate the self-assembly of chitosan, based on proton balance between its protonated and deprotonated residues, to promote facile nanoparticle synthesis. This is one of the first reports that highlights subtle but critical influence of proton balance in the chitosan polymer on the formation of chitosan nanoparticles.

Formation of Chitosan Nanoparticles Using Deacetylated Chitin Isolated from Freshwater Algae and Locally Synthesized Zeolite A and their Influence on Cancer Cell Growth

This work reports the isolation and characterization of chitin from green algae using XRD, 13C CP/MAS NMR, FTIR and Microscopy. The XRD diffraction pattern confirmed orthorhombic structure of the crystalline polysaccharide, whereas the FTIR spectra revealed strong absorption bands at 896.9 cm-1 and 852 cm-1 typical of C–H axial and C–H equatorial vibrations within the anomeric center of the glucopyranosicyclic moiety. Another strong absorption band was observed at 1039.9 cm-1 and was assigned to C–O–C, C–O stretching bands. The purity and structure of the deacetylated chitin was confirmed using 13C NMR, showing overlapping peaks around 65 ppm assigned to both the sugar carbon at C2, as well as a methylene carbon at C6. An intense peak at 74 ppm is assigned to C3 and C5 with corresponding resonances at 81 and 104 ppm assigned to C4 and C1 respectively. Zeolite/Chitosan nanocomposites were synthesized by ionic cross-linking of chitosan with sodium tripolyphosphate. Chitosan nanoparticles and LTA of different concentrations were incubated with HeLa cancer cells to investigate their cytotoxicity effects. The exposure of the cells to chitosan nanoparticles resulted in a decreased in cell growth and this was concentration-dependent. Our results revealed the utility of locally available materials to produce new biodegradable nanoparticles to investigate their biological nanotoxicity.

Biological preparation of chitosan nanoparticles and its in vitro antifungal efficacy against some phytopathogenic fungi

The aim of the present study was to prepare Chitosan nanoparticles through biological method with high antifungal activities. Chitosan nanoparticles were prepared by the addition of anionic proteins isolated from Penicillium oxalicum culture to chitosan solutions. The formation of chitosan nanoparticles was preliminary confirmed by UV–vis spectrophotometric analysis. The physico-chemical properties of the chitosan nanoparticles were determined by size and zeta potential analysis, FTIR analysis, HRTEM and XRD pattern. The chitosan nanoparticles were evaluated for its potential to inhibit the growth of phytopathogens viz., Pyricularia grisea, Alternaria solani, Fusarium oxysporum. It is evident from our results that chitosan nanoparticles inhibit the growth of phytopathogens tested. Chitosan nanoparticle treated chickpea seeds showed positive morphological effects such as enhanced germination%, seed vigor index and vegetative biomass of seedlings. All these results indicate that chitosan nanoparticle can be used further under field condition to protect various crops from the devastating fungal pathogens as well as growth promoters.

Size-controlled synthesis of chitosan nanoparticles and their structural characterization

ABSTRACTThe agricultural industry worldwide is facing several challenges including environmental pollution problems (soils and water) caused by the unsuitable control on the use of agrochemicals. Recently, nanotechnology has become an option to improve the existing crop management techniques. Polymer nanoparticles can be used for storage and controlledrelease of agrochemicals, such as pesticides and fertilizers. In this regard, chitosan nanoparticles have been considered for agricultural applications due to the capability of size control at the nanoscale and porosity control capability, in addition to biodegradable and biocompatible characteristics. On this basis, this work focuses on the development of a sizecontrolled synthesis method for chitosan nanoparticles for further use as a platform for the controlled-release system of agrochemicals. The chitosan nanoparticles were synthesized by polymerization using methacrylic acid in water. Several chitosan precursor concentrations (0.2- 0.8 wt.%) were evaluated in order to manipulate the size of produced nanoparticles. The hydrodynamic diameter of those nanoparticles was determined by using a Malvern Zetasizer and the suspension stability trough zeta potential measurements. The morphology and geometrical size were investigated by Transmission Electron Microscopy (TEM). Chitosan nanoparticles size was around 17 nm when a precursor 0.2 wt.% chitosan solution was used. X-ray diffraction and Fourier Transform Infrared Spectroscopy techniques confirmed the chitosan nanoparticles formation and its interaction with functional groups of methacrylic acid.

Novel and simple route for the synthesis of core–shell chitosan–gold nanocomposites

This work presents a novel and simple route for the synthesis of water-soluble core–shell chitosan–gold nanocomposites. The experimental procedure can be summarized by the following steps: (i) chitosan deacetylation, (ii) chitosan depolymerization, (iii) chitosan nanoparticles’ formation and (iv) chitosan–gold nanocomposite formation. FT-IR spectroscopic results indicate that the formation of chitosan nanoparticles (ChtNPs) occurs via NH3+ and PO− groups electrostatic interactions, while UV–vis spectra points to a possible embedding of gold nanoparticles into the ChtNPs. This feature was confirmed by electronic transmission microscopy measurements. Chitosan and gold are biocompatible materials. Added to this, the obtained chitosan–gold nanocomposites presented thermal and absorbance properties which strongly point to their potential use in phototherapeutic processes.

Understanding the mechanism of ionic gelation for synthesis of chitosan nanoparticles using qualitative techniques

We focused on qualitatively exploring the basic mechanisms involved in the Ionic gelation (IG) process, a method quite frequently used for synthesis of chitosan (CS) microparticles (MPs) and nanoparticles (NPs).We synthesized CS MPs and NPs using the Ionic gelation and microemulsion methods, and characterized the CS NPs and MPs at different stages of formulation using scanning electron microscopy (SEM) and fluorescence microscopy. Fourier Transform Infrared (FTIR) analysis was carried out to confirm effective cross-linking. Moreover, for the first time, we reported the mechanisms of IG technique for CS NP and MP synthesis with qualitative proof: (1) Complex formation of long chain oligomers with polyanions (long beaded structures) (2) cleavages at weak sites on addition of acid (HCl) (3) formation of CS NPs on chain scission.The versatility of IG for the synthesis of CS MPs and NPs was proved and compared with the microemulsion technique, thereby enhancing the wide spectrum of its use in therapeutics and biomedical applications.