Efficient polymer-mediated delivery system for thiocyclam: Nanometerization remarkably improves the bioactivity toward green peach aphids.

The unscientific application of synthetic pesticides has brought various negative effects on the environment, hindering the sustainable development of agriculture. Nanoparticles can be applied as carriers to improve pesticide delivery, showing great potential in the development of pesticide formulation in recent years. Herein, a star polymer (SPc) was constructed as an efficient pesticide nanocarrier/adjuvant that could spontaneously assemble with thiocyclam or monosultap into a complex, through hydrophobic association and hydrogen bonding, respectively, with the pesticide-loading contents of 42.54% and 19.3%. This complexation reduced the particle sizes of thiocyclam from 543.54 to 52.74 nm for pure thiocyclam, and 3 814.16 to 1 185.89 nm for commercial preparation (cp) of thiocyclam. Interestingly, the introduction of SPc decreased the contact angles of both pure and cp thiocyclam on plant leaves, and increased the plant uptake of cp thiocyclam to 2.4-1.9 times of that without SPc. Meanwhile, the SPc could promote the bioactivity of pure/cp thiocyclam against green peach aphids through leaf dipping method and root application. For leaf dipping method, the 50% lethal concentration decreased from 0.532 to 0.221 g/L after the complexation of pure thiocyclam with SPc, and that decreased from 0.390 to 0.251 g/L for cp thiocyclam. SPc seems a promising adjuvant for nanometerization of both pure and cp insecticides, which is beneficial for improving the delivery efficiency and utilization rate of pesticides.

A nano-delivery system expands the insecticidal target of thiamethoxam to include a devastating pest, the fall armyworm.

Nano-delivery systems have been applied to deliver various synthetic/botanical pesticides to increase the efficiency of pesticide use and reduce the volumes of pesticides applied. Previous studies have supported the hypothesis that the nanocarriers can help expand the insecticidal target of pesticides to include non-target pests. However, the potential mechanism underlying this interesting phenomenon remains unclear. Herein, a widely applied star polycation (SPc) nanocarrier was synthesized to construct a thiamethoxam (TMX) nano-delivery system. The SPc-based delivery system could promote the translocation of exogenous substances across the membrane of Sf9 cells, increase the cytotoxicity of TMX against Sf9 cells by nearly 20%, and expand the insecticidal target of TMX to include Spodoptera frugiperda (the fall armyworm), with a 27.5% mortality increase at a concentration of 0.25 mg/mL. Moreover, the RNA-seq analysis demonstrated that the SPc could upregulate various transport-related genes, such as Rab, SORT1, CYTH, and PIKfyve, for the enhanced cellular uptake of TMX. Furthermore, enhanced cell death in larvae treated with the TMX-SPc complex was observed through changes in the expression levels of death-related genes, such as Casp7, BIRC5, MSK1, and PGAM5. The SPc-based nano-delivery system improved the cellular uptake of TMX and expanded its insecticidal target by adjusting the expression levels of death-related genes. The current study mainly identified the transport and cell death genes related to nanocarrier-based insecticidal target expansion, which is beneficial for understanding the bioactivity enhancement of the nano-delivery system.

Nanometerization of thiamethoxam by a cationic star polymer nanocarrier efficiently enhances the contact and plant-uptake dependent stomach toxicity against green peach aphids.

BACKGROUND: The utilization efficiency of conventional insecticides is comparatively low in agricultural production, which leads to their excessive application and environmental pollution. Insecticide nanometerization by polymers and polymeric materials has advantages, particularly increased utilization efficiency and reduced insecticide application. RESULTS: To increase the utilization efficiency of insecticides, a star polycation (SPc) was selected as a drug carrier that could be complexed with thiamethoxam through electrostatic interaction. Formation of the complex decreased the particle size of thiamethoxam from 575.77 to 116.16 nm in aqueous solution. Plant uptake of SPc-delivered thiamethoxam was increased 1.69-1.84 times compared with thiamethoxam alone. Nano-sized thiamethoxam/SPc complexes showed enhanced contact and stomach toxicity against green peach aphids. CONCLUSION: SPc is a promising insecticide adjuvant for insecticide nanometerization, and is beneficial in improving insecticidal activity and decreasing the application amounts and application rates of conventional insecticides. © 2020 Society of Chemical Industry.

Internalization of hydroxyapatite nanoparticles in liver cancer cells.

Hydroxyapatite (HAP) is the main inorganic component of hard tissues and shows excellent biocompatibility and osteoconductivity properties. Nanoparticles of HAP can be synthesised by the precipitation method in distilled water. The needle shaped particles are below 100 nm in size with low-crystallinity and high-surfacial activation. Recent studies showed toxic effects of HAP nanoparticles on cancer cells. Other studies focus on the application of HAP nanoparticles as drug and gene delivery system or cell marker. However, to date, the exact internalization pathway of HAP nanoparticles into cells has not been determined. When HAP nanoparticles were added to cell culture medium, the particles immediately became instable and formed agglomerates with a size of about 500-700 nm. Hence, cells seldom encounter single HAP nanoparticles in the environment of cell culture or body fluid. The TEM showed internalized HAP captured by vacuoles in the cytoplasm of the hepatocellular carcinoma cells. The invaginations in the cell membrane before nanoparticle uptake suggested endocytic pathways as internalization mechanism. This study revealed that agglomerated HAP nanoparticles were internalized by cells through the energy-dependent process of clathrin-mediated endocytosis. Depletion of intracellular potassium arrested the formation of coated pit, which inhibited the uptake of HAP.

Establishment of a new model for culturing rabbit osteoblasts in vitro.

To establish an experimental model for culturing rabbit osteoblasts in vitro, the osteoblasts were isolated from the calvarial bone of a 15-day old rabbit using a method of culturing the bone pieces in a medium after they had been digested by an enzyme for 15 min. The acquired cells were assayed by cell morphology, alkaline phosphatase activity and production of a mineralized matrix. The results showed that the cells had the morphologic characteristics and some biological behaviours of osteoblasts. Based on the primary isolation of osteoblasts from bone and combining digestion with explants, a novel model for culturing rabbit osteoblasts in vitro was established, which is easy, efficient and effective. This model can be used in many studies of osteogenesis mechanisms and bone replacement materials.

Effect of hydroxyapatite nanoparticles on the ultrastructure and function of hepatocellular carcinoma cells in vitro.

The interaction of Bel-7402 hepatocellular carcinoma cells (HCC) as a single cell suspension with hydroxyapatite (HAP) nanoparticles was investigated. It was observed by an inverted microscope that the cells were still homogeneously distributed in the culture medium after 24 h. A TEM analysis showed that the HAP nanoparticles attached to the Bel-7402 cells were finally swallowed by the cells after 4 h, and induced ultrastructural changes of the cells after 4 days. A MTT assay and cell count test for the HAP nanoparticles of various concentrations from 0.14 to 0.56 mmol L(-1) showed that the HAP nanoparticles at a concentration of 0.56 mmol L(-1) induced the strongest effect on the inhibition of Bel-7402 cell proliferation and induced a dramatic decline in cell numbers. Proliferation of Bel-7402 was inhibited by more than 70%, compared to the control. A cell cycle analysis revealed that HAP can arrest Bel-7402 cells at the G1 phase with increasing effect over time. These findings demonstrated that HAP can enter into HCC very easily, change their ultrastructure, and evidently suppress their proliferation.