Enhancing solubility and therapeutic potential of rosuvastatin via β-cyclodextrin inclusion complex-loaded chitosan nanoparticles

Preparation of chitosan–TPP nanoparticles using microengineered membranes – Effect of parameters and encapsulation of tacrine

Chitosan nanoparticles, O-(2-hydroxyl) propyl-3-trimethyl ammonium chitosan chloride (O-HTCC) nanoparticles and bovine serum albumin (BSA) loaded chitosan and O-HTCC nanoparticles of a size (about 200-600 nm) were obtained through the process of ionic gelation between chitosan or O-HTCC and sodium tripolyphosphate (TPP). The physicochemical properties of nanoparticles made from chitosan, O-HTCC, BSA loaded chitosan, and BSA loaded O-HTCC were determined by transmission electron microscopy (TEM), polarized optical microscopy (POM), photon correlation spectroscopy (PCS), and X-ray diffraction (XRD) pattern. Zeta potential was also performed to understand the surface properties of nanoparticles and their ability to bind negatively charged BSA. TEM, POM, and XRD suggested that ionic-gelation process significantly influenced the crystallinity of BSA, and greater chain realignment in the BSA-loaded chitosan and O-HTCC nanoparticles. PCS revealed that BSA-loaded chitosan nanoparticles were bigger than chitosan nanoparticles in size and BSA-loaded O-HTCC nanoparticles were smaller than O-HTCC nanoparticles in size.

Primaquine (PQ) loaded chitosan (CS) nanoparticles were prepared by ionic gelation technique using different concentrations of chitosan and sodium tripolyphosphate (TPP) and the potential of using these nanoparticles for liver targeting was investigated. Various factors such as concentration of chitosan and the amount of the cross-linking agent (TPP) were investigated to reveal their influences on the zeta potential, particle size, entrapment efficiency and in vitro release of the resulted nanoparticles. The formulation conditions were optimized to obtain a positive charged spherical nanoparticles with zeta potential of 29.0mV, polydispersity index of 0.213 and particle size in the range of 100-200nm. The entrapment efficiency of best batch of cross-linked chitosan nanoparticles encapsulated with primaquine (PQ-CS-NP) (i.e. 0.6mg/ml TPP into 0.1% chitosan solution) was found to be 93.21±0.17. It was observed that the in vitro release of primaquine from CS NPs was 96.52±0.54 within 24 h demonstrating sustained drug release effect. TEM showed that the prepared nanoparticles were smooth and spherical in shape. DSC and FTIR revealed no significant interactions between primaquine and CS after encapsulation and cross-linking. XRD data indicated that primaquine creates a non crystalline dispersion into the chitosan nanoparticles. The optimized batch of nanoparticles was tested in vivo to study the liver targeting effect. Primaquine loaded chitosan nanoparticles showed a much higher distribution of drug into liver as compared to that in blood. In comparison, primaquine solution showed lesser concentration in both liver and blood after IV administration into mice. The results concluded that chitosan nanoparticles were efficient carriers for the targeting of drug into liver. Keywords: Chitosan, ionic gelation, liver targeting, malaria, nanoparticles, primaquine.

Primaquine (PQ) loaded chitosan (CS) nanoparticles were prepared by ionic gelation technique using different concentrations of chitosan and sodium tripolyphosphate (TPP) and the potential of using these nanoparticles for liver targeting was investigated. Various factors such as concentration of chitosan and the amount of the cross-linking agent (TPP) were investigated to reveal their influences on the zeta potential, particle size, entrapment efficiency and in vitro release of the resulted nanoparticles. The formulation conditions were optimized to obtain a positive charged spherical nanoparticles with zeta potential of 29.0mV, polydispersity index of 0.213 and particle size in the range of 100-200nm. The entrapment efficiency of best batch of cross-linked chitosan nanoparticles encapsulated with primaquine (PQ-CS-NP) (i.e. 0.6mg/ml TPP into 0.1% chitosan solution) was found to be 93.21±0.17. It was observed that the in vitro release of primaquine from CS NPs was 96.52±0.54 within 24 h demonstrating sustained drug release effect. TEM showed that the prepared nanoparticles were smooth and spherical in shape. DSC and FTIR revealed no significant interactions between primaquine and CS after encapsulation and cross-linking. XRD data indicated that primaquine creates a non crystalline dispersion into the chitosan nanoparticles. The optimized batch of nanoparticles was tested in vivo to study the liver targeting effect. Primaquine loaded chitosan nanoparticles showed a much higher distribution of drug into liver as compared to that in blood. In comparison, primaquine solution showed lesser concentration in both liver and blood after IV administration into mice. The results concluded that chitosan nanoparticles were efficient carriers for the targeting of drug into liver. Keywords: Chitosan, ionic gelation, liver targeting, malaria, nanoparticles, primaquine.

Preparation of mucoadhesive methacrylated chitosan nanoparticles for delivery of ciprofloxacin

In this work, chitosan nanoparticles were prepared by ionotropic gelation of chitosan with tripolyphosphate (TPP). The effects of the ionic strength of the solvent employed in the particle preparation on the average size and compactness of the particles were investigated. In addition, the effects of the chitosan concentration and the crosslinker to polymer ratio on the particle characteristics were studied. The chitosan–TPP nanoparticles were characterized by dynamic light scattering, zeta potential, and turbidity measurements. The compactness of the nanoparticles was estimated with a method based on the size of the nanoparticles and the turbidity of the nanoparticle suspension. All the investigated preparation parameters, i.e., the ionic strength of the solvent, the chitosan concentration, and the TPP to chitosan ratio, affected the particle characteristics. For instance, smaller and more compact particles were formed in saline solvents, compared to particles formed in pure water. Further, the addition of monovalent salt rendered it possible to prepare particles in the nanometer size range at a higher polymer concentration. Solvent salinity is thus an important parameter to address in the preparation of chitosan nanoparticles crosslinked with TPP.

Background: Recombinant human keratinocyte growth factor (rHuKGF) is a protein used to treat oral mucositis caused by radio and chemotherapy in patients with hematologic malignancy. The rHuKGF is available in the form of intravenous bolus injection. In this study, new formulation of rHuKGF-loaded chitosan nanoparticles was developed to improve patient compliance. Methods: Chitosan nanoparticles (CNPs) loaded with rHuKGF were prepared by ionic gelation method. The tripolyphosphate (TPP) cross-linked with chitosan molecules at pH >5.0 and form the nanoparticles. An infrared spectroscopic technique was conducted to confirm the formation of nanoparticles as a result of ionotropic interaction between TPP and chitosan. Zeta Sizer was used to determine the size, polydispersity index (PdI) and zeta potential of the prepared nanoparticles. The morphological characteristics of CNPs were measured by field emission scanning electron microscope. During the formation of CNPs, the rHuKGF was entrapped in the nanoparticles. The loading capacity of rHuKGF in CNPs was observed to be dependent on how much amount of rHuKGF/TPP solution was added to convert all the chitosan molecules to form nanoparticles. A double beam UV/Vis spectroscopic method was used to detect the formation of these rHuKGF loaded CNPs based on their optical properties. Results: The produced rHuKGF-loaded CNPs were colorless, cloudy, and positively charged monodisperse with a spherical shape. The prepared CNPs have particles size of 119 ± 74.62 nm, surface charge of +20.3 ± 6.46 mV and 0.217 polydispersity index. The shape of prepared CNPs was found to be spherical using field emission scanning electron microscope (FESEM). The interfacial polyelectrolyte complexation between TPP and chitosan was confirmed by comparing the FTIR spectra of TPP, chitosan, physical mixture of chitosan and TPP and CNPs. The loading capacity of the rHuKGF in CNPs was found to be 93.3 ± 2.02%. The formation of rHuKGF loaded CNPs was detected by double beam UV/Vis Spectroscopy at 232.2 nm. Conclusion: The results of the current work were utilized for designing a continuous monitoring and detection system for the formation of CNPs. The outcomes of this technique are useful to avoid the loss of rHuKGF during nanoparticle formation and improving the loading capacity of CNPs.

Chitosan (CS) nanoparticles (NPs) are attracting interest because of their applications in drug delivery and medical imaging. This study synthesized low-molecular-weight CS NPs by ionic crosslinking with tripolyphosphate (TPP) as crosslinker using static mixers. Effects of process parameters on the size of CS NPs were investigated. CS NPs 168–1000 nm in size were obtained. Increasing the number of mixing elements, decreasing the CS concentration, or increasing the temperature of CS solution produced small NPs. Increasing the CS/TPP ratio initially decreased and then increased the size of CS NPs, with the smallest NPs obtained at 10:3 CS/TPP ratio. Flow rate exerted a similar effect as volume ratio on the size of CS NPs. Flow rates of 250 and 75 mL/min for CS and TPP solutions, respectively, produced the smallest particles. A fully continuous process was developed by combining static mixing and ionic crosslinking to mass produce CS NPs.

Chitosan nanoparticles (CSNPs) can be widely used in the food, pharmaceutical, and cosmetic sectors due to their high performance, unique properties, and high surface area. In this research, CSNPs were produced by the ionic gelation method and using sodium tripolyphosphate (STPP) as an appropriate technique compared to the conventional methods. To evaluate the effects of various factors on the size, zeta potential (ZP), and optimal synthesis conditions, different concentrations of CS (1, 3, and 5 mg/mL), STPP (0.5, 0.75, and 1 mg/mL), and CS to STPP ratio (1:1, 3:1, and 5:1) were applied and optimized using the response surface methodology. The size of CSNPs was increased by using higher concentrations of CS, STPP, and CS/STPP ratios. The value of ZP was determined positive and it increased with increasing CS concentrations and CS/STPP ratios. ATR-FTIR spectra revealed interactions between CS and STPP. The DSC thermogram of CSNPs showed a double sharp endothermic peak at about 74.5 °C (ΔH = 122.00 J/g); further, the TGA thermograms indicated the total weight loss of STPP, CS, and CSNPs as nearly 3.30%, 63.60%, and 52.00%, respectively. The XRD data also revealed a greater chain alignment in the CSNPs. Optimized, the CSNPs can be used as promising carriers for bioactive compounds where they also act as efficient stabilizers in Pickering emulsions.

Development and characterisation of chitosan nanoparticles for siRNA delivery

Elaboration of chitosan nanoparticles: Favorable impact of a mild thermal treatment to obtain finely divided, spherical, and colloidally stable objects

Evaluation of chitosan nanoparticles as a glazing material for cryogenically frozen shrimp

Purpose: Chitosan is a natural mucoadhesive polymer with antibacterial activity. In the present study, chitosan (CS) nanoparticles were investigated as a vehicle for delivery of antibiotic, ciprofloxacin hydrochloride.Methods: Ionotropic gelation method was used for preparation chitosan nanoparticles. The effects of various factors including concentration of CS, concentration of tripolyphosphate (TPP), and homogenization rate on the size of nanoparticles were studied. The effects of various mass ratios of CS to ciprofloxacin hydrochloride on the encapsulation efficiency of nanoparticles were assessed.Results: The particles prepared under optimal condition of 0.45% CS concentration, 0.45% TPP concentration and homogenizer rate at 6000 rpm, had 72 nm diameter. In these particles with 1:0.5 mass ratio of CS to ciprofloxacin hydrochloride, the encapsulation efficiency was 23%. The antibacterial activity of chitosan nanoparticles and ciprofloxacin-loaded nanoparticles against E.coli and S.aureus was evaluated by calculation of minimum inhibitory concentration (MIC). Results showed that MIC of ciprofloxacin loaded chitosan nanoparticles was 50% lower than that of ciprofloxacin hydrochloride alone in both of microorganism species. Nanoparticles without drug exhibited antibacterial activity at higher concentrations and MIC of them against E.coli and S.aureus was 177 and 277 µg/ml, respectively.Conclusion: Therefore chitosan nanoparticles could be applied as carrier for decreasing the dose of antibacterial agents in the infections.

Shrimp oil is encapsulated in chitosan‐tripolyphosphate nanoparticles (CSNPs) prepared by a dual‐step process involving emulsification of oil followed by entrapment in the chitosan‐tripolyphosphate matrix. CSNPs loaded with shrimp oil at varied levels show different encapsulation efficiencies (32.34–67.54%), mean particle diameters (110.29–278.11 nm), and zeta potential (18.93–33.77 mV). Scanning electron micrographs reveal that CSNPs are spherical or ellipsoidal in shape without flocculation. Differential scanning calorimetry and Fourier transform infrared spectroscopy results further substantiate the entrapment of shrimp oil within the CSNPs. Shrimp oil loaded in CSNPs have better oxidative stability and quality, compared to the free oil plausibly due to the synergistic effect between enclosure of oil by CSNPs and antioxidative property of chitosan. Polyunsaturated fatty acids and astaxanthin are more retained in CSNP encapsulated oil than the free oil over the storage of 8 weeks, indicating high potency of CSNPs in preventing the losses in the nutritional value and active component of shrimp oil.Practical Applications: Shrimp oil is an exemplary source of astaxanthin and n‐3 fatty acids with potential health benefits. Shrimp oil encapsulation in chitosan nanoparticles is a simple and promising technique to protect the oil from oxidation and rancidity with no significant loss of polyunsaturated fatty acids or astaxanthin. Shrimp oil loaded‐chitosan nanoparticles are thermodynamically stable and disperse readily in water, making it highly favorable for fortification in variety of foods, particularly beverages. This technique is cost effective, since chitosan is abundantly available at low cost.

Chitosan and silver nanoparticles as pudding with raisins with antimicrobial properties