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Pesticide Formulations and Their Importance in the Development of Promising Protectants for Cereal Crops
Abstract
The importance of the role of a formulation in realizing the potential of a new substance and promoting the preparation (medicinal or pesticide) on the market is undeniable. When developing a pesticide formulation, it is necessary to address the following issues: a convenient application form, drug fixation on the plant surface, penetration of an active substance into the plant, and high efficiency against weeds, plant diseases and pests. The modern formulations of nanoscale pesticides facilitate better realization of the biological potential of an active substance. This article gives a brief overview of the literature on pesticide formulations and their varieties, the preparation methods and effectiveness published in the last 10 years, with a particular focus on the authors' own work.
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Recent requirements of the pesticide industry have become much severer, and pesticides (formulated products) are required to satisfy higher safety to both human beings and the environment, higher biological efficacy, lower price, and labor-saving. This review explains the outline of basic pesticide formulation technology, followed by recent advances in developing new formulations and application technologies. Labor-saving formulations and application technologies, environmental load reduction technologies, and user-friendly formulations and application technologies are elucidated.
Because of the rapid development of nanotechnologies, materials, in particular, solid dispersions (SDs), which are actively introduced into the life of modern man, have been obtained. Special progress in this area is observed in industry and medicine. The use of SDs in agriculture is lagging far behind, despite the growing number of scientific papers on this topic. At the same time, the prospects for the introduction of SDs in the agro-industrial complex are obvious. The review presents the results of research on the development of innovative preparations based on SD to protect plants from diseases and pests of cultivated plants, as well as parasiticides to protect animal health based on modern achievements of nanotechnology. One of these technologies is the methods of mechanochemistry, which improve the properties of poorly soluble biologically active substances by their joint mechanical treatment with water-soluble polymers and auxiliary substances.
Pesticides are indispensable in agricultural production. They have been used by farmers to control weeds and insects, and their remarkable increases in agricultural products have been reported. The increase in the world’s population in the 20th century could not have been possible without a parallel increase in food production. About one-third of agricultural products are produced depending on the application of pesticides. Without the use of pesticides, there would be a 78% loss of fruit production, a 54% loss of vegetable production, and a 32% loss of cereal production. Therefore, pesticides play a critical role in reducing diseases and increasing crop yields worldwide. Thus, it is essential to discuss the agricultural development process; the historical perspective, types and specific uses of pesticides; and pesticide behavior, its contamination, and adverse effects on the natural environment. The review study indicates that agricultural development has a long history in many places around the world. The history of pesticide use can be divided into three periods of time. Pesticides are classified by different classification terms such as chemical classes, functional groups, modes of action, and toxicity. Pesticides are used to kill pests and control weeds using chemical ingredients; hence, they can also be toxic to other organisms, including birds, fish, beneficial insects, and non-target plants, as well as air, water, soil, and crops. Moreover, pesticide contamination moves away from the target plants, resulting in environmental pollution. Such chemical residues impact human health through environmental and food contamination. In addition, climate change-related factors also impact on pesticide application and result in increased pesticide usage and pesticide pollution. Therefore, this review will provide the scientific information necessary for pesticide application and management in the future.
The chemicalization of agriculture is an important component of an integrated plant protection system to obtain stably high crop yields and provide food products to the rapidly growing population of the Earth. Seed dressing with fungicides is a determining element in the plant protection system, and systemic drugs give the best effect. The absence of such protection of cultivated plants can lead to a decrease in wheat productivity by more than 20% due to the development of Fusarium and Helminthosporious infection. At the same time, indicators such as protein content can decrease by 10.0%, and gluten - by 8-10%. Therefore, it is very important to develop the scientific basis for the preparation of complex preparations with a low consumption rate of the active substance and the inclusion of biological products, including plant growth regulators, which enhance the growth processes and yield of the main crop. In recent years, areas for the modification of known and practiced fungicides using various methods, including methods of mechanochemistry, are promising. At the same time, high permeability of active substances is achieved both due to auxiliary substances (in particular, polysaccharides), which increase the solubility of drugs, and by adding surfactants and other formative components to the formulations. The review of the literature on the development of alternative preparative forms of fungicidal preparations based on triazole derivatives and known fungicides, as well as their biological activity, is presented.
Abstract Glycyrrhizin or glycyrrhizic acid (GA) - triterpene glycoside extracted from licorice root - has been intensively studied over the past decade and is considered to be a potential drug delivery system. Glycyrrhizin was found to enhance the therapeutic effect of various drugs; however the detailed mechanism of these effects is still unknown and attracts the attention of researchers. In this work, we have made an attempt to clarify the mechanism of Glycyrrhizin activity on molecular and cellular level. The influence of GA on the functional properties of biomembranes was investigated via NMR spectroscopy and atomic force microscopy (AFM) using human erythrocytes as a model system. GA was shown to increase the permeability (about 60%) and to decrease elasticity modulus of cell membranes (by an order of magnitude) even in micromolar concentrations. Changes on the erythrocyte surface were also detected by AFM. These results could provide a new insight on the mechanism of bioavailability enhancement of some drugs in the presence of glycyrrhizin, as well as the mechanism of its own biological activity. The role of cholesterol-glycyrrhizin binding in the observed effects is also discussed.
Drug discovery in the late 20th century has increasingly focused on the definition and characterization of the macromolecular substrates that serve as targets for drug design. The advent of genomics and the molecular biology revolution has permitted both the definition of new targets and the characterization of the genetic basis of disease states. The introduction of powerful new technologies should greatly accelerate the pace of new drug discovery. Although genomics, both human and nonhuman, should in principle increase the number of potential drug targets and provide a greater understanding of cellular events contributing to the pathology of disease this has yet to occur in practice, primarily because of the underlying complexity of cellular signaling processes. The emerging discipline of systems biology is attempting to bring both order and understanding to these signaling processes. Genomics has, however, impacted on drug discovery in ways that are important beyond a mere increase in potential drug target numbers. Genomics has provided the tools of contemporary drug discovery, the pharmacogenomic pathways to personalized medicine, and has greatly influenced the nature of synthetic organic chemistry, a discipline that is still the cornerstone of contemporary drug discovery. In the future, genomics and the tools of molecular biology will have a corresponding impact on drug delivery processes and mechanisms through introduction of drug delivery machines capable of both synthesis and activation by disease-specific signals. Such machines will be based on a synthetic genome, using an expanded genetic code, and designed for specific drug synthesis and delivery and activation by a pathological signal. This essay is based upon a lecture of the same title presented at the Faculty of Medicine, Kuwait University during a visit in the spring of 2005. It is intended, as was the lecture, to be a broad, descriptive and speculative overview rather than a comprehensive and detailed review.
Currently, nanotechnologies are being actively introduced into agriculture, in
particular in the field of creating new effective plant protection products. This is achieved
through the development of nanosized controlled release systems, such as polymer
nanoparticles, micelles, and so on using a wide variety of materials. In the present study,
we applied original approach based on “green” mechanochemical technology to prepare
new nanocomposites of pesticide Tebuconazole (TBC) for treating wheat seeds against
pathogenic microflora (B. sorokiniana, Fusarium spp., Alternaria spp., Penicillum spp.).
The size distribution of nanoparticles for three TBC formulations (microcapsules,
microemulsionsб nanosuspensions) was measured using dynamic light scattering
technique. All formulations contained nanoparticles (10-300 nm) and we aimed to find the
most suitable size for effective penetration into cell membranes. The narrowest size
distribution (225±40 nm) was observed for nanosuspension based on Licorice Extract
(LE). The microcapsules based on Na-CMC also contained micro-sized particles (1,500
nm), which are apparently aggregates of nanoparticles. The laboratory and field
biological tests revealed a high activity of the developed formulations against all
pathogenic microflora under study, with a low retardant effect. Nanosuspension is
considered as the most “environmentally friendly preparation”, since it contains only
natural LE as an adjunct. This formulation with a consumption rate of 0.25 Lt-1
suppressed 100% B. sorokiniana, Fusarium spp. and Penicillum spp. infections, possibly
due to the presence of natural saponin glycyrrhizic acid, which interacts with plant
membranes and promotes better penetration of TBC into the grain.
The solubility behavior of drugs remains one of the most challenging aspects in formulation development. With the advent of combinatorial chemistry and high throughput screening, the number of poorly water soluble compounds has dramatically increased. Although solid solutions have tremendous potential for improving drug solubility. This article reviews the various preparation techniques for solid dispersion and gives some of the recent technology transfers. Some of the important practical aspects to be considered for the preparation of solid dispersions, such as selection of carrier and methods of physicochemical characterization. New manufacturing processes to obtain solid dispersions have also been developed to reduce the drawbacks of the initial process. In this review, it is intended to discuss the recent advances related on the area of solid dispersions. Solid dispersion technologies are particularly promising for improving the oral absorption and bioavailability of BCS Class II drugs. The focus of this review article on the method of preparation, carrier used, characterization, advantages, disadvantages and the application of the solid dispersion.
The primary objectives of formulation technology are to optimise the biological activity of the pesticide, and to give a product
which is safe and convenient for use. However, because of the wide variety of pesticide active ingredients which are available,
many different types of formulations have been developed depending mainly on the physico-chemical properties of the active
ingredients. In the past most formulations were based on simple solutions in water (SL), emulsifiable concentrates in a petroleum-based
solvent (EC), or dusts (DP) and wettable powders (WP). The presence of petroleum-based solvents in EC formulations and dusty
powders in DP and WP formulations can lead to safety hazards in use and a negative impact on the envirnoment generally. Most
government and regulatory authorities are now demanding formulations which are cleaner and safer for the user, have minimal
impact on the environment, and can be applied at the lowest dose rate. Developments in formulation technology and novel formulation
types, sometimes in special packaging such as water-soluble packs, can also give products a competitive advantage, add value
or extend the lif-cycle of active ingredients. There is also a demand from government authorities and consumer groups to use
safer formulation additives and adjuvants, and to minimise the residues of pesticides on food crops after spraying. All of
these aspects are putting increasing pressure on the development of improved formulation and adjuvant technologies. Pesticide
formulations for spray application and for seed treatment are discussed, along with developments in bioenchancement.
Orally administered, immediate-release (IR) drug products in the top 200 drug product lists from the United States (US), Great Britain (GB), Spain (ES), and Japan (JP) were provisionally classified based on the Biopharmaceutics Classification System (BCS). The provisional classification is based on the aqueous solubility of the drugs reported in readily available reference literature and a correlation of human intestinal membrane permeability for a set of 29 reference drugs with their calculated partition coefficients. Oral IR drug products constituted more that 50% of the top 200 drug products on all four lists, and ranged from 102 to 113 in number. Drugs with dose numbers less than or equal to unity are defined as high-solubility drugs. More than 50% of the oral IR drug products on each list were determined to be high-solubility drugs (55-59%). The provisional classification of permeability is based on correlations of the human intestinal permeabilities of 29 reference drugs with the calculated Log P or CLogP lipophilicity values for the uncharged chemical form. The Log P and CLogP estimates were linearly correlated (r2 = 0.79) for 187 drugs. Metoprolol was chosen as the reference compound for permeability and Log P or CLogP. A total of 62-69.0% and 56-60% of the drugs on the four lists exhibited CLogP and Log P estimates, respectively, greater than or equal to the corresponding metoprolol value and are provisionally classified as high-permeability drugs. We have compared the BCS classification in this study with the recently proposed BDDCS classification based on fraction dose metabolism. Although the two approaches are based on different in vivo processes, fraction dose metabolized and fraction dose absorbed are highly correlated and, while depending on the choice of reference drug for permeability classification, e.g., metoprolol vs cimetidine or atenolol, show excellent agreement in drug classification. In summary, more than 55% of the drug products were classified as high-solubility (Class 1 and Class 3) drugs in the four lists, suggesting that in vivo bioequivalence (BE) may be assured with a less expensive and more easily implemented in vitro dissolution test.
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