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  • Ескіз
    Документ
    Experiment planning at the pharmaceutical development of liposomal cytostatics
    (Національний фармацевтичний університет, 2017) Stadnichenko, A. V.; Krasnopolsky, Yu. M.; Yarnykh, T. G.
    At present, there is an increasing interest in developing new ways of drug delivery and targeted therapy, using nanotechnology and nanomaterials. Aim – to study the order of carrying out of pharmaceutical development of liposoms with cytostatics. Propose the scope of the experiment to optimize the planned quality indicators and technological parameters. Materials and methods. Analysis of normative documents, scientific literature and also the results of previous personal experimental studies, which became the basis for determining the methodology for the creation of liposomal drugs based on oxaliplatin and irinotecan. Lipids manufactured by Lipoid, Germany, were used to make liposomes. The lipid film was produced on a Buchi 210 rotary evaporator with a vacuum controller, at a residual pressure of 0.02 atm. For homogenization, a high pressure extrusion method was used, which was carried out on a Microfluidiser M-110P (Microfluidics, USA). Results and discussion. With the development of the pharmaceutical industry, there is a growing interest to the use of nanotechnology and nanomaterials. One of the practical implementation of nanotechnology is liposomes with cytostatics. Concentration of the active substance; pH and salt API; method of loading for API into liposomes; lipid to lipid ratio, lipids concentration; particle size and internal volume; lipid solubility in the step of lipid film preparation; stability testing of of finished products are factors that need to be studied and solved for the successful implementation of the development. Planning an experiment in the pharmaceutical development of liposomal oxaliplatin and liposomal irinotecan are complex studyes with using the principles of Quality by Design (QbD). Conclusions. The requirements of normative documentation for creating liposomal forms of medicinal products are considered. At pharmaceutical development it is necessary to use the complex approach as the majority of the put questions can not be solved separately. An experiment planning system for the pharmaceutical development of liposomal preparations of irinotecan and oxaliplatin is proposed.
  • Ескіз
    Документ
    Study of the composition of cryoprotector and technological regime in liophilization of liposomes with oxaliplatinum
    (НВП ПП "Технологічний Центр", 2017) Stadnichenko, A. V.; Krasnopolsky, Yu. M.; Yarnykh, T. G.
    Lyophilization is one of the most prospective and technologically logical methods for preserving the structure of nanobiotechnological products. Liposomes with oxaliplatin were obtained, and a screening experiment was performed to select a cryoprotectant. Aim. The aim of the research is to obtain liposomes with oxaliplatin, determine the type of cryoprotectant and its quantity, study the parameters of lyophilisation to obtain the product with maximum encapsulation of oxaliplatin, with the save of the size of liposomes in the nano diapason, and the optimum residual moisture content. Methods. Lyophilization was carried out in a Quarco lyophilizer (PRC). The liposomal form of oxaliplatin was obtained by the method of “passive” encapsulation in combination with the ion sorption method. Results. Lactose, sucrose, maltose and trehalose dihydrate were studied as cryoprotectants. As the most perspective, was chosen - trehalose dihydrate. The optimal concentration of trehalose dihydrate in the liposomal form of oxaliplatin was researched at 8 % by weight. Also was optimized the program of freeze-drying. Primary drying with a duration of 1740 minutes was not sufficient. When the program was increased for 300 min, up to 2040 min, the values of the loss of encapsulation rate of 8 %, from 65 % before drying, to 57 % after drying were obtained. This is a good indicator, which shows an effectiveness of cryoprotectant and a rational program of freeze-drying. The size of the liposomes after drying was 112 nm, the residual moisture content, measured by K. Fischer’s method, was 2.3 %, which is within the scope of the target range. Conclusion. A technology for obtaining liposomes with encapsulated oxaliplatin has been proposed and screening studies have been carried out to determine the optimal cryoprotectant. It is proposed to use as a cryoprotector trehalose dihydrate as the most perspective. The effect of different content of trehalose dihydrate on the degree of encapsulation of oxaliplatin in liposomes was studied. It was found= that the optimal cryoprotectant concentration in the preparation is 8 % (by mass). Technological parameters of the lyophilization process of liposomes with oxaliplatin have been developed: drying time and freezing temperature. The decrease in the incorporation of oxaliplatin into liposomes during lyophilisation did not exceed 8.0 % with a residual water content of about 2.3 %. The size of liposomes after lyophilization in the nanoscale is 112 nm.