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At the present stage of plant protection should be considered as a prospective direction to minimize the impact of biotic stressors and the optimizing regulatory capacity of agricultural technologies, which negate the environmental and economic risks and promote sustainable agriculture. In this respect, to protect seeds is one of the most environmentally friendly ways of pesticide use and therefore in all developed countries of the world the protecting of seeds refers to the law of mandatory phytosanitary measures directed against a complex of pathogens of crops, transmitted by seeds and remaining in the soil. It is obvious that the efficacy of pesticides is not only dependent on the nature of the active substance (AS) and its activity, but also the correct choice of formulation AS retaining beneficial properties, the stability of working solutions providing quality of the application and adherence to the treated surface. Development of the formulation takes place on the basis of the adaptation of common methodological principles of nanomaterials research methods, technical means and nanotechnology. And we should expect that these techniques and technologies will improve formulations of pesticides on three main criteria - effectiveness, efficiency and environmental friendliness to the environment. It is known that most biologically active substances, in particular of pesticides’ AS, belong to the class or bad-insoluble and physiologically active media, which involves excessive use dosages AS and thereby leads to higher drug price and increases its toxicity to the environment . In this regard, our research on the development of innovative medicines based on mechano-chemical methods of modification of the physico-chemical and biological properties of wellknown pesticides, are very popular and relevant. The essence of the approach developed by us is to provide preparations in the form of solid dispersions of pesticides and watersoluble polymers by their joint mechanochemical treatment in a controlled energy input mills. Using the method of mechanochemical modifications refers to regulate properties of pesticides and take the compositions with high water solubility, which suggests an increase in biological activity of the compositions. In this paper the results of research will be given to the creation of innovative seed treatment of cereals. For example, it was noted a positive effect on almost all indicators of the structure of productivity of grain crops, which ultimately impact on increasing grain yield. It was shown that integrated seed protectants offered by us have a complex effect, namely, exhibit the properties of a fungicide, a plant growth regulator and herbicide antidote residues in the soil. The results indicate the prospects of further studies to optimize the formulation methods of protectants by Mechanochemistry.