Chitosan-sodium Tripolyphosphate Research Articles

Nanomaterial-encapsulated dsRNA of ecdysone-induced early gene E75, a potential RNAi-based SIT strategy for pest control against Bactrocera dorsalis

Bactrocera dorsalis is a notorious pest widely distributed across most Asian countries. With the rapid development of pesticide resistance, new pest control methods are urgently needed. RNAi-based sterile insect technique (SIT) is a species-specific pest management strategy for B. dorsalis control. It is of great significance to identify more target genes from B. dorsalis, and improve the RNAi efficiency. In this study, microinjection-based RNAi results showed that six 20E response genes were necessary for male fertility of B. dorsalis, of which E75 was identified as the key target according to the lowest egg-laying number and hatching rate after E75 knockdown. Three nanoparticles chitosan (CS), chitosan‑sodium tripolyphosphate (CS-TPP), and star polycation (SPc) were used to encapsulate dsE75 expressed by HT115 strain. Properties analysis of nanoparticle-dsRNA complexes showed that both CS-TPP-dsRNA and SPc-dsRNA exhibited better properties (smaller size and polydispersity index) than CS-dsRNA. Moreover, oral administration of CS-TPP-dsE75 and SPc-dsE75 by males resulted in more abnormal testis and significantly lower fertility than feeding naked dsE75. Semi-field trials further confirmed that the number of hatched larvae was dramatically reduced in these two groups. Our study not only provides more valuable targets for RNAi-based SIT, but also promotes the application of environment-friendly management against B. dorsalis in the field.

Chitosan-TPP microcapsules for controlled drug release

Production of chitosan/sodium tripolyphosphate (CS/TPP) microcapsules via spray drying involves atomizing an emulsion containing CS, TPP, acetic acid (AcOH), and folic acid (FA) into fine droplets exposed to high-temperature, low-pressure gas flow. Solvent evaporation within the drying chamber leads to solid particle formation. Spray drying is valuable for creating solid CS/TPP microcapsules. Precise equipment parameter adjustments, like inlet temperature and gas flow rate, enable the study of microcapsule morphology, size, and properties. This adaptability allows for customization to specific pH dissolution ranges. The production method's impact on CS/TPP microcapsules was studied by modifying spray drier parameters, including inlet temperature and aspirator pressure, to enhance understanding of their behavior in solution under varied production conditions.
 In chitosan delivery systems, various approaches can encapsulate drug agents like folic acid, an analog to the cancer treatment drug methotrexate. Agents can be added to the chitosan solution pre-crosslinking, incorporated into gelation-inducing agents pre-mixing with chitosan, or included in the crosslinking mixture. Experiments were conducted to assess CS/TPP microcapsules' behavior when encapsulating agents like folic acid. Release profiles were analyzed to understand their drug delivery capabilities and potential as controlled release carriers.

Optimize the parameters for the synthesis by the ionic gelation technique, purification, and freeze-drying of chitosan-sodium tripolyphosphate nanoparticles for biomedical purposes

BackgroundPolymeric nanoparticles can be used for wound closure and therapeutic compound delivery, among other biomedical applications. Although there are several nanoparticle obtention methods, it is crucial to know the adequate parameters to achieve better results. Therefore, the objective of this study was to optimize the parameters for the synthesis, purification, and freeze-drying of chitosan nanoparticles. We evaluated the conditions of agitation speed, anion addition time, solution pH, and chitosan and sodium tripolyphosphate concentration.ResultsChitosan nanoparticles presented an average particle size of 172.8 ± 3.937 nm, PDI of 0.166 ± 0.008, and zeta potential of 25.00 ± 0.79 mV, at the concentration of 0.1% sodium tripolyphosphate and chitosan (pH 5.5), with a dripping time of 2 min at 500 rpm. The most representative factor during nanoparticle fabrication was the pH of the chitosan solution, generating significant changes in particle size and polydispersity index. The observed behavior is attributed to the possible excess of sodium tripolyphosphate during synthesis. We added the surfactants poloxamer 188 and polysorbate 80 to evaluate the stability improvement during purification (centrifugation or dialysis). These surfactants decreased coalescence between nanoparticles, especially during purification. The centrifugation increased the zeta potential to 40.8–56.2 mV values, while the dialyzed samples led to smaller particle sizes (152–184 nm). Finally, freeze-drying of the chitosan nanoparticles proceeded using two cryoprotectants, trehalose and sucrose. Both adequately protected the system during the process, and the sugar concentration depended on the purification process.ConclusionsIn Conclusion, we must consider each surfactant's benefits in formulations for selecting the most suitable. Also, it is necessary to do more studies with the molecule to load. At the same time, the use of sucrose and trehalose generates adequate protection against the freeze-drying process, even at a 5% w/v concentration. However, adjusting the percentage concentration by weight must be made to work with the CS-TPP NPs purified by dialysis.

Improvement of the Antioxidant and Antitumor Activities of Benzimidazole-Chitosan Quaternary Ammonium Salt on Drug Delivery Nanogels.

The present study focused on the design and preparation of acid-responsive benzimidazole-chitosan quaternary ammonium salt (BIMIXHAC) nanogels for a controlled, slow-release of Doxorubicin HCl (DOX.HCl). The BIMIXHAC was crosslinked with sodium tripolyphosphate (TPP) using the ion crosslinking method. The method resulted in nanogels with low polydispersity index, small particle size, and positive zeta potential values, indicating the good stability of the nanogels. Compared to hydroxypropyl trimethyl ammonium chloride chitosan-Doxorubicin HCl-sodium tripolyphosphate (HACC-D-TPP) nanogel, the benzimidazole-chitosan quaternary ammonium salt-Doxorubicin HCl-sodium tripolyphosphate (BIMIXHAC-D-TPP) nanogel show higher drug encapsulation efficiency and loading capacity (BIMIXHAC-D-TPP 93.17 ± 0.27% and 31.17 ± 0.09%), with acid-responsive release profiles and accelerated release in vitro. The hydroxypropyl trimethyl ammonium chloride chitosan-sodium tripolyphosphate (HACC-TPP), and benzimidazole-chitosan quaternary ammonium salt-sodium tripolyphosphate (BIMIXHAC-TPP) nanogels demonstrated favorable antioxidant capability. The assay of cell viability, measured by the MTT assay, revealed that nanogels led to a significant reduction in the cell viability of two cancer cells: the human lung adenocarcinoma epithelial cell line (A549) and the human breast cancer cell line (MCF-7). Furthermore, the BIMIXHAC-D-TPP nanogel was 2.96 times less toxic than DOX.HCl to the mouse fibroblast cell line (L929). It was indicated that the BIMIXHAC-based nanogel with enhanced antioxidant and antitumor activities and acidic-responsive release could serve as a potential nanocarrier.

Synthesis of β-acids loaded chitosan-sodium tripolyphosphate nanoparticle towards controlled release, antibacterial and anticancer activity

The development of nanoparticles loaded with natural active ingredients is one of the hot trends in the pharmaceutical industry. Herein, chitosan was selected as the base material, and sodium tripolyphosphate was chosen as the cross-linking agent. Chitosan nanoparticles loaded with β-acids from hops were prepared by the ionic cross-linking method. The results of Fourier transform infrared spectroscopy (FTIR) and X-ray diffraction (XRD) indicated that chitosan nanoparticles successfully encapsulated β-acids. The loading capacity of chitosan nanoparticles with β-acids was 2.00 %–18.26 %, and the encapsulation efficiency was 0.58 %–55.94 %. Scanning electron microscopy (SEM), transmission electron microscope (TEM), particle size, and zeta potential results displayed that the nanoparticles revealed a sphere-like distribution with a particle size range of 241–261 nm, and the potential exhibited positive potential (+14.47–+16.27 mV). The chitosan nanoparticles could slowly release β-acids from different simulated release media. Notably, the β-acids-loaded nanoparticles significantly inhibited Staphylococcus aureus ATCC25923 (S. aureus) and Escherichia coli ATCC25922 (E. coli). Besides, β-acids-loaded chitosan nanoparticles were cytotoxic to colorectal cancer cells (HT-29 and HCT-116). Therefore, applying chitosan nanoparticles can further expand the application of β-acids in biomedical fields.

Chitosan, Chitosan/IgG-Loaded, and N-Trimethyl Chitosan Chloride Nanoparticles as Potential Adjuvant and Carrier-Delivery Systems.

This work proposes a feasible, reproducible, and low-cost modified method to manufacture chitosan, chitosan/IgG-protein-loaded, and trimethylated chitosan nanoparticles, using microfluidics combined with the microemulsion technique, which differs from the traditional batch process of chitosan-based nanoparticles. The synthesis process consists of generating microreactors of chitosan-based polymer in a poly-dimethylsiloxane ψ-shaped microfluidic device and then crosslinking with sodium tripolyphosphate outside the cell. Transmission electron microscopy demonstrates an improvement in size control and distribution of the solid-shape chitosan nanoparticles (~80 nm) compared to the batch synthesis. Regarding chitosan/IgG-protein-loaded nanoparticles, these presented a core-shell morphology having a diameter of close to 15 nm. Raman and X-ray photoelectron spectroscopies confirmed the ionic crosslinking between the amino groups of chitosan and the phosphate groups of sodium tripolyphosphate in the fabricated samples and the total encapsulation of IgG protein during the fabrication of chitosan/IgG-loaded nanoparticles. Then, an ionic crosslinking and nucleation-diffusion process of chitosan-sodium tripolyphosphate was carried out during the nanoparticle formation, with and without IgG protein loading. The use of N-trimethyl chloride chitosan nanoparticles in vitro on human-keratinocyte-derived cell line HaCaT did not show side effects independently of its concentration from 1 to 10 μg/mL. Therefore, the proposed materials could be used as potential carrier-delivery systems.

Efektivitas Adsorben Kitosan - Natrium Tripolifosfat dalam Menurunkan Konsentrasi Fe dan Mn pada Air Sumur

In general, well water or ground water often contains iron (Fe) and manganese (Mn) ions in it. One of the effective water treatment processes to remove heavy metals is adsorption. Natural adsorbents such as chitosan can be effective adsorbents used to reduce heavy metal concentrations in the environment. One of the weaknesses of chitosan is the strength of the mechanical structure and low stability. Therefore, crosslinking modifications were carried out to improve the mechanical structure and reduce solubility. This study aims to determine the effect of sodium tripolyphosphate on the process of making chitosan shrimp shell-sodium tripolyphosphate adsorbent and to determine the optimum conditions of the variation of the adsorbent and the mass used. The research variables used were the sodium-tripolyphosphate concentration of 0.25%; 0.50%; and 1.00%, the mass of the adsorbent in the column was 5 grams and 7.5 grams, and the sampling times were 20 minutes, 40 minutes, 60 minutes, 80 minutes, 100 minutes, 120 minutes, 140 minutes and 160 minutes. The results showed that the 1% chitosan-sodium tripolyphosphate adsorbent with a mass of 7.5 grams was the most optimal in reducing the content of Fe by 92% and Mn by 93%.

Preparation of fluorescently and biologically active chain-like chitosan nanocomposite and its use in separating MBP-tagged proteins and as fluorescent tracer of tobacco

Chain-like chitosan-sodium tripolyphosphate (CS-TPP) nanocomposite was prepared by an aqueous solution route. Then fluorescently active 6-carboxyl luciferin (6-FAM) was modified onto CS-TPP surface to afford CS-TPP-6-FAM nanocomposite (CS-TPP-6-FAM) with fluorescent activity. Onto the surface of CS-TPP-6-FAM was grafted bioactive carboxymethyl β-cyclodextrin (CβCD) to obtain CS/TPP/FAM/CβCD that can separate maltose binding protein tagged (MBP-tagged) fusion proteins from E. coli lysate. Findings demonstrate that CS-TPP-6-FAM-CβCD has an average diameter of 22 nm and a chain length of 70 nm. Its adsorption kinetic data can be described by Langmuir isotherm equation and the pseudo 2nd kinetic model, corresponding to high protein binding capacity for MBP-tagged PYL3. Furthermore, CS-TPP-6-FAM-CβCD dispersed in Hoagland nutrient solution can be adsorbed by tobacco through vascular bundle channels. Therefore, CS-TPP-6-FAM-CβCD could have promising applications in separating MBP-tagged fusion proteins from E. coli lysate and in monitoring the growth of plants as the fluorescent tracer.

Double-Coated Nanoparticle of Ribosome Inactivating Protein (RIP) from Mirabilis jalapa L. prepared from Chitosan-Sodium Tripolyphosphate and Alginate-Calcium Chloride: The New Strategy for Protein Drug in Oral Delivery

Oral delivery of protein drugs is challenging due to the instability of the compound and structural barrier exists in the gastrointestinal (GI) tract. Nanoparticle technology is known as a promising drug delivery strategy to ensure drug bioavailability. This study aims to formulate an oral delivery system of a potential anticancer agent named Ribosome Inactivating Protein from Mirabilis jalapa L.-C (RIP MJ-C) through double-coated nanoparticles prepared from Chitosan-Sodium Tripolyphosphate (TPP) and Alginate-Calcium Chloride (CaCl2). Nanoparticles were prepared through the ionic gelation method, with the core nanoparticle (RMJCN-1) formulated in the pH of 3.5-5.5 using 0.3-0.5 % w/v of chitosan and 0.03 % w/v TPP. The RMJCN-1 optimum formula was selected to be subsequently coated with the second layer of alginate and CaCl2, called RMJCN-2, with a concentration of 0.3% w/v and 0.1-0.3 %, respectively. The sample was characterized by the entrapment efficiency (EE), physical appearance, particle size, polydispersity index (PI), and potential zetta. The result showed the optimum RMJCN-1 formula with of EE value of 57.10 ± 0.04 % was obtained by formulating 0.5 % w/v chitosan and 0.3 % w/v STPP in pH 5.5. The optimum RMJCN-2 was obtained by the combination of alginate 0.3 % w/v and CaCl2 0.1% w/v in the outer layer. This final formula produces nanoparticles with a zeta potential of -14.4 mV, 739.8 nm in size, with good stability during 7 days at room temperature. This study has successfully developed a formulation of double-coated nanoparticles from Chitosan-TPP and Alginat-CaCl2 for RIP MJ-C, leads to a safe nanocarrier system for oral delivery of RIP MJ-C that ensures its bioavailability.

Synthesize of the chitosan-TPP coated betanin-quaternary ammonium-functionalized mesoporous silica nanoparticles and mechanism for inhibition of advanced glycation end products formation

Advanced glycation end products (AGEs) are harmful by-products of thermal-processing of food. Betanin is an antioxidant with the potential to inhibit AGEs formation. In this work, we encapsulated betanin in chitosan-sodium tripolyphosphate coated quaternary ammonium-functionalized mesoporous silica nanoparticles (CS@QAMSNPs) to enhance the ability of betanin to inhibit AGEs formation. The inhibition rate of betanin-CS@QAMSNPs was 70.29%, which was higher than that of betanin (39.48%). Compared with betanin (2.16%), betanin-CS@QAMSNPs can trap more methylglyoxal (18.7%), absorb formed AGEs, and retain the antioxidant capacity of betanin under high-temperatures. Betanin-CS@QAMSNPs can reduce the average degree of substitution per peptide molecule value (DSP) of some glycation sites in bovine serum albumin. The cell viability was over 80% in the presence of betanin-CS@QAMSNPs, indicating their good biocompatibility. In the biscuit model, the highest inhibition rate of AGEs formation by betanin-CS@QAMSNPs was 12.5%, and CS@QAMSNPs can further adsorb the AGEs generated during digestion.

Improvement of the stability and anti-AGEs ability of betanin through its encapsulation by chitosan-TPP coated quaternary ammonium-functionalized mesoporous silica nanoparticles

Mesoporous silica nanoparticles (MSNPs) are widely used as encapsulation materials, however, low encapsulation ability and the leakage and inactivation of the encapsulated components are two major disadvantages that limit their applications. Quaternary ammonium-functionalization and chitosan-sodium tripolyphosphate (CS-TPP) coating are used in this study to overcome these disadvantages. Betanin is a bioactive ingredient, but it is easily degraded. In this work, a new type of CS-TPP coated quaternary ammonium-functionalized MSNPs (CS@QAMSNPs) were synthesized by a reversed-phase microemulsion method, and betanin was encapsulated therein. The results of SEM, TEM, and FTIR of CS@QAMSNPs showed that MNSPs were functionalized with quaternary ammonium and coated with CS-TPP. The loading capacity of betanin-CS@QAMSNPs was 21.66 %, while that of betanin-MSNPs was 2.95 %. After encapsulation by CS@QAMSNPs, over 65 % of the antioxidant activity of betanin was retained after high-temperature and alkaline treatment, and 84.24 % of betanin was retained after ultraviolet-radiation treatment, implying an improvement in the stability of betanin. Cell viability was over 80 % in the presence of betanin and encapsulating materials, indicating their good food safety. The highest inhibition rate of betanin-CS@QAMSNPs in advanced glycation end-products in the BSA-fructose and BSA-MGO model was 47.39 % and 15 %, which was higher than those of betanin (BSA-fructose:11.38 %, BSA-MGO:0.83 %).

Co-microencapsulation of Ruellia tuberosa L. and Cosmos caudatus K. Extracts for Pharmaceutical Applications

This study aims to co-microencapsulate the Ruellia tuberosa L. and Cosmos caudatus K. extracts, with chitosan–sodium tripolyphosphate (Na-TPP) as coating material. α-Amylase inhibition and antioxidant assays were conducted to determine the potential of microcapsules used as antidiabetic agents. The microcapsules were manufactured under the influences of pH, Na-TPP concentration, and stirring time. The optimum microencapsulation conditions were selected based on the highest encapsulation efficiency. The optimum microencapsulation conditions were a pH of 4, Na-TPP concentration of 0.15% (w/v), and stirring time of 60 min. The microcapsules exhibited an IC50 (inhibitory concentration) value of 223.64 ± 0.81 µg/mL and an α-amylase inhibition and antioxidant activity of 104.05 ± 0.88 µg/mL. The test for the release of bioactive compounds from microcapsules was conducted in HCl pH 1.2 and phosphate buffer pH 7.4 for 30–120 min. Results showed that 5.99% and 58.96% of bioactive compounds were released at pH 1.2 and 7.4, respectively, in 120 min. The Fourier transform infrared spectra showed the P=O functional group vibrations from Na-TPP at 1,213.71 cm−1 and C–N stretching vibrations from chitosan at 1,155.23 cm−1. Characterization with scanning electron microscopy and particle size analysis indicated that the microcapsules were spherical and had a mean diameter of 132.08 µm. The current study demonstrated that co-microencapsulation is a promising multifaceted approach for the enhancement of the pharmaceutical applications of plant extract combinations

Metronidazole Delivery Nanosystem Able To Reduce the Pathogenicity of Bacteria in Colorectal Infection.

Metronidazole (MTZ) is a drug potentially used for the treatment of intestinal infections, namely, the ones caused by colorectal surgery. The traditional routes of administration decrease its local effectiveness and present off-site effects. To circumvent such limitations, herein a drug delivery system (DDS) based on MTZ-loaded nanoparticles (NPs) immobilized at the surface of electrospun fibrous meshes is proposed. MTZ at different concentrations (1, 2, 5, and 10 mg mL-1) was loaded into chitosan-sodium tripolyphosphate NPs. The MTZ loaded into NPs at the highest concentration showed a quick release in the first 12 h, followed by a gradual release. This DDS was not toxic to human colonic cells. When tested against different bacterial strains, a significant reduction of Escherichia coli and Staphylococcus aureus was observed, but no effect was found against Enterococcus faecalis. Therefore, this DDS offers high potential to locally prevent the occurrence of infections after colorectal anastomosis.

Development of Nanocapsules Containing Cytotoxic Agents- A Review

Background: The incidence and mortality of cancer are rapidly growing worldwide. Modification on drug delivery systems based on nanotechnology was applied to improve the effectiveness and safety of treatment. Nanoencapsulation, a part of nanotechnology, was known can be involved in cytotoxic agents. Objective: This research was conducted to determine the type of polymers for nanoencapsulation of cytotoxic agents and analyze the effect of nanoencapsulation on the cytotoxic activity. Methods: The study was performed by systematic literature review using selected articles from reputable databases that meet the inclusion and exclusion criteria. Results: The results show that many cytotoxic agents have been developed in nanocapsules systems due to their low water solubility, chemical instability, and low bioavailability. The nanoencapsulation process was carried out using synthetic or natural polymers such as polylactic-co-glycolic acid (PLGA), PEGylated PLGA, polycaprolactone (PCL), chitosan-sodium tripolyphosphate, chitosan-sodium alginate, heparin-poly(l-lysine), and polymethyl methacrylate (PMMA). Those polymers are widely used for nanoencapsulation related to their biocompatible, biodegradable, non-toxic, and providing the desired coating properties. The nanoencapsulation on cytotoxic agents significantly increases the in vitro cytotoxicity, marked by the decrease of IC50 value in the range 1.4-15.4 folds compared to pure drugs. The increase in cytotoxicity could be caused by particle size reduction, modification of particle surface properties, and enhancement of drug stability. Conclusion: It can be concluded that nanoencapsulation can be applied for cytotoxic agents to increase their activity using the appropriate coating polymer.

Preparation and Characterization of Electrospun Double-layered Nanocomposites Membranes as a Carrier for Centella asiatica (L.).

A wide range of naturally derived and synthetic biodegradable and biocompatible polymers are today regarded as promising materials for improving skin regeneration. Alongside this, these materials have been explored in conjunction with different types of antimicrobial and bioactive agents, especially natural-derived compounds, to enhance their biological properties. Herein, a double-layered nanocomposite dressing membrane was fabricated with two distinct layers. A bottom layer from Chitosan-Sodium tripolyphosphate (CS-TPP) and Poly(vinyl alcohol) (PVA) containing Centella asiatica (L.) (CA) was electrospun directly over a Polycaprolactone (PCL) layer to improve the biologic performance of the electrospun nanofibers. In turn, the PCL layer was designed to provide mechanical support to the damaged tissue. The results revealed that the produced double-layered nanocomposite membrane closely resembles the mechanical, porosity, and wettability features required for skin tissue engineering. On the other hand, the in vitro drug release profile of the PCL/PVA_CS-TPP containing CA exhibited a controlled release for 10 days. Moreover, the PVA_CS-TPP_CA’s bottom layer displayed the highest antibacterial activity against Staphylococcus aureus (S. aureus) (99.96 ± 6.04%) and Pseudomonas aeruginosa (P. aeruginosa) (99.94 ± 0.67%), which is responsible for avoiding bacterial penetration while endowing bioactive properties. Finally, the 3-(4,5-Dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay showed that this nanocomposite membrane was not cytotoxic for normal human dermal fibroblasts (NHDF) cells. Therefore, these findings suggest the potential use of the double-layered PCL/PVA_CS-TPP_CA as an efficient bionanocomposite dressing material.

Development, Characterization and Pharmacokinetic Profile of Chitosan-Sodium Tripolyphosphate Nanoparticles Based Drug Delivery Systems for Curcumin.

Purpose: This study aimed to provide the method of preparation, characterization of curcumin-loaded chitosan-sodium tripolyphosphate (NaTPP) nanoparticle, and evaluate its pharmacokinetic profiles. Methods: Curcumin-loaded chitosan-NaTPP nanoparticles were synthesized using ionic gelation methods. Curcumin was dissolved using surfactants and cosurfactants. Chitosan polymer was then mixed in the curcumin solution and dripped with NaTPP solution until nanoparticle formation. The mucoadhesive study was evaluated by measuring the fluorescence of curcumin within the prepared nanoparticles. The pharmacokinetic profiles of curcumin particles and nanoparticles were then assessed in rats by administering a single oral dose of 100 mg/kg BW. Blood samples were taken from nine predetermined time points, and curcumin plasma concentrations were then analyzed using UPLC-MS/MS. Results: The particle size of the curcumin nanoparticles obtained were 11.5 nm. Entrapment efficiency (EE) of curcumin nanoparticles were exceeding 99.97%, and drug loading capacity (DLC) was 11.34%. The mucoadhesive properties of the nanoparticles were superior to that of curcumin particles. Pharmacokinetic evaluation in rats revealed that curcumin nanoparticles resulted in an increase of area under the curve (AUC), maximum concentration (Cmax), earlier time to reach maximum concentration (Tmax), and lower clearance (CL). Conclusion: Curcumin-loaded chitosan-NaTPP nanoparticles is an effective formulation to improve curcumin plasma concentrations. Thus, enable its applications for the treatment of various diseases.

The effect of particle size on dissolution rate of fast dissolving oral film containing diclofenac sodium

Diclofenac sodium is a Non-Steroidal Anti Inflammatory Drugs that if being taken orally have the side effects of peptic ulcers and undergone the first pass metabolism, and also included in the Biopharmaceutics Classification System class 2 which resulted in the low rate of dissolution. This study aims to determine the influence of particle size reduction on the dissolution rate of diclofenac sodium in the form of an FDOF dosage. The formation of diclofenac sodium nanoparticles is carried out by ionic gelation method using chitosan and sodium tripolyphosphate as a crosslinker in various ratios characterized by Particle Size Analyzer and Scanning Electron Microscopy, then it is incorporated into the form of an FDOF that were prepared by solvent casting method at a dose of 12.5 mg using variations concentration of SSG as superdisintegrant and PEG 400 as plasticizer. From the research results, diclofenac sodium nanoparticles are formed in the ratio of chitosan-sodium tripolyphosphate 6:1, have a size of 804 nm and spherical-shaped. The best FDOF dosage formula is F8 containing HPMC E5 LV 35% as the film forming agent, SSG 8% as superdisintegrant and PEG 400 10% as plasticizer. FDOF formula containing diclofenac sodium nanoparticles has a slightly bitter taste, disintegration time less than one minute, surface pH around 7 (neutral), drug content that meets the requirements of the range of determination which is 93.24 ± 0.96, the cumulative amount of drug dissolved in the 28th minute is higher by 88.45% compared to FDOF containing diclofenac sodium raw material, which is only 70.0%.

Digestibility and Bioaccessibility of Pickering Emulsions of Roasted Coffee Oil Stabilized by Chitosan and Chitosan-Sodium Tripolyphosphate Nanoparticles

Due to the valuable lipid fraction composition present in roasted coffee oil, it has become important to develop methods that modify its structure, such as emulsion-based encapsulation systems, favoring its use in food industry. Pickering emulsions have appeared as a potential alternative to protect oil droplets stabilized by solid particles rather than the use of surfactants. This work investigated the ability of chitosan (CS) nanoparticles produced by deprotonation and by ionic gelation to stabilize emulsions with different lipid phase content as an alternative to encapsulate roasted coffee oil. An in vitro digestion model consisting of mouth, gastric and intestinal phases was used to characterize the rate and extent of lipid phase digestion, emulsion microstructure, and bioaccessibility of total phenolic compounds. All emulsions presented some structural changes attributed to flocculation and coalescence throughout simulated gastrointestinal digestion. Better droplet stabilization using the deprotonation method was achieved when lower oil content was used, leading to higher bioaccessibility of total phenolic compounds.

Reproductive performance of goats treated with free gonadorelin or nanoconjugated gonadorelin at estrus

The reproductive performance of goats that received a GnRH analog (gonadorelin) fabricated with or without chitosan-sodium tripolyphosphate (TPP) nanoparticles on the day of estrus (day 0) was evaluated. The chitosan-TPP polymer was conjugated with gonadorelin using an ionic gelation method. Thirty-three multiparous Zaraiebi goats were synchronized for estrus with 2 intramuscular (im) injections of 125 μg prostaglandin F2α 14 d apart. Goats showing signs of estrus were divided equally into 3 experimental groups and received a single im injection of 1 mL physiological saline (placebo; control), 50 μg/mL gonadorelin (GnRH), or 12.5 μg (quarter of GnRH dose)/mL chitosan-TPP–conjugated gonadorelin nanoparticles (NGnRH). Each goat underwent ultrasound imaging of their ovaries at day 0 and at day 10 after mating, and pregnancy was diagnosed 28 and 45 d after mating. The concentrations of estradiol (E2) and progesterone (P4) were determined at day 0 and at days 7, 14, 21, and 42 after mating. NGnRH size, polydispersity, and zeta potential were 93.91 nm, 0.302, and 11.6 mV, respectively. Chitosan-TPP nanoparticles showed 91.2% entrapment efficiency for GnRH. No differences in estrus rate, interval to estrus, or ovarian structure at day 0 were observed among the experimental groups, but the GnRH and NGnRH treatments significantly decreased the duration of estrus compared with the control. At day 10 after mating, both GnRH and NGnRH increased (P = 0.011) the number of corpora lutea compared with the control. Treatment with GnRH increased (P = 0.023) serum E2 concentrations from day 7 to 42 after mating compared with NGnRH and control treatments. The highest (P = 0.043) serum P4 concentration was observed in the GnRH group, followed by the NGnRH and control groups. The increase in serum P4 concentration started earlier a on day 7 in the GnRH group but later on day 14 in the NGnRH group. Compared with the control, GnRH resulted in a higher (P = 0.041) P4-to-E2 ratio, followed by NGnRH. Both gonadorelin treatments significantly increased the twinning rate, the number of embryos at days 28 and 42, and prolificacy and decreased pregnancy losses compared with the control. In conclusion, the administration of GnRH at the time of estrus improved the prolificacy of goats by increasing both the ovulation rate and the number of embryos. In addition, the nanoformulation developed in this study allowed a 75% reduction in the conventional dose of gonadorelin without affecting the fertility and prolificacy of goats, indicating the bioavailability of the reduced GnRH dose after conjugation with developed nanoformula.

Immunogenicity and protective efficacy of mucosal delivery of recombinant hcp of Campylobacter jejuni Type VI secretion system (T6SS) in chickens

The type VI secretion system (T6SS) has recently emerged as a new pattern of protein secretions in Campylobacter jejuni (C. jejuni). Within the T6SS cluster, hemolysin co-regulated protein (hcp) is considered as a hallmark of functional T6SS and holds key role in bacterial virulence. As poultry is the primary reservoir of C. jejuni and the major sources for human infection, we evaluated the capacity of recombinant hcp (rhcp) immunization in blocking C. jejuni colonization in chickens with an aim to control bacterial transmission to humans via poultry food chain. Considering the mucosal route is the primary portal for C. jejuni entry and gut mucosa offers the apposite site for C. jejuni adherence, we investigated the immune-protective potential of intra-gastric administration of rhcp using chitosan-based nanoparticles. To achieve this goal, full length coding sequence of hcp gene from C. jejuni was cloned and expressed in E. coli. Purified rhcp was entrapped in chitosan-Sodium tripolyphosphate nanoparticles (CS-TPP NPs) and orally gavaged in chickens. Our results suggest that intra-gastric immunization of CS-TPP-rhcp induces consistent and steady increase in intestinal (sIgA) and systemic antibody (IgY) response against rhcp with significant reduction in cecal load of C. jejuni. The protection afforded by rhcp associated cellular responses with Th1 and Th17 profile in terms of increased expression of NFkB, IL-1β, IL-8, IL-6, IFN-γ and IL-17 A genes. Though systemic immunization of rhcp with IFA resulting in a robust systemic (IgY) and local (sIgA) antibody response, mucosal administration of rhcp loaded CS-TPP NPs was found to be superior in terms of bacterial clearance. Altogether, present study suggests that chitosan based intra-gastric delivery of rhcp have several advantages over the injectable composition and could be a promising vaccine approach to effectively control C. jejuni colonization in chickens.