Determination of Optimal Technological Conditions for the Process of Production a Liposomal Dosage Form of Cyphetrylin
Introduction. The Laboratory for the development of dosage forms of the N. N. Blokhin National Medical Research Center of Oncology of the Ministry of Health of Russian Federation has developed a composition of an injectable liposomal dosage form based on soybean phosphatidylcholine, a hydrophobic an...
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| Language: | Russian |
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LLC Center of Pharmaceutical Analytics (LLC «CPHA»)
2022-02-01
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| Series: | Разработка и регистрация лекарственных средств |
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| Online Access: | https://www.pharmjournal.ru/jour/article/view/1165 |
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| author | M. V. Dmitrieva O. L. Orlova A. V. Lantsova I. I. Krasnyuk |
| author_facet | M. V. Dmitrieva O. L. Orlova A. V. Lantsova I. I. Krasnyuk |
| author_sort | M. V. Dmitrieva |
| collection | DOAJ |
| description | Introduction. The Laboratory for the development of dosage forms of the N. N. Blokhin National Medical Research Center of Oncology of the Ministry of Health of Russian Federation has developed a composition of an injectable liposomal dosage form based on soybean phosphatidylcholine, a hydrophobic analog of the hypothalamic hormone somatostatin − cyphetrylin, intended for the treatment of neuroendocrine tumors.Aim. Determination of optimal technological conditions for the process of obtaining a liposomal dosage form of cyphetrylin.Materials and methods. The study used the substance cyphetrylin synthesized in the of Chemical Synthesis Laboratory of the N. N. Blokhin National Medical Research Center of Oncology of the Ministry of Health of Russian Federation; soybean phosphatidylcholine S PC and polyethylene glycol-2000-distearoylphosphatidylethanolamine, produced by Lipoid GmbH (Germany); cholesterol ≥99 % (Sigma-Aldrich, Japan). For the preparation of phospholipid vesicles loaded with cyphetrylin and "empty", the methods of lipid film hydration with subsequent extrusion or homogenization of the dispersion of multi-layer liposomes were used. The obtained liposomal samples were evaluated by quality indicators − the effectiveness of the inclusion of cyphetrylin in vesicles, their average size and surface charge (zeta potential), the viscosity of the dispersion. To evaluate these characteristics, the methods of spectrophotometry, laser scattering spectroscopy, determination of the electrophoretic mobility of particles and viscometry were used.Results and discussion. It was found that the most suitable organic solvent for obtaining a solution of cyphetrylin and lipid components of the dosage form is chloroform. The duration of the drying period of the lipid film under vacuum to remove the residual solvent is determined by the ratio of the volume of the distillation flask used and the mass of its loading its loading. At the same time, hydration off the lipid film with water for injection should be carried out under conditions of low-pressure and room temperature. To obtain a dispersion of single-layer cyphetrylin liposomes of the required size, an extrusion method using nylon and polycarbonate membranes with a filter pore diameter of 0.22 and 0.2 um, respectively, was chosen.Conclusion. The optimal technological conditions for the process of obtaining a liposomal dosage form in the form of a dispersion of a hydrophobic analog of the hypothalamic hormone somatostatin − cyphetrylin are determined. |
| first_indexed | 2024-04-10T01:38:49Z |
| format | Article |
| id | doaj.art-1f357dd4999340f4ba807938708a8d35 |
| institution | Directory Open Access Journal |
| issn | 2305-2066 2658-5049 |
| language | Russian |
| last_indexed | 2024-04-10T01:38:49Z |
| publishDate | 2022-02-01 |
| publisher | LLC Center of Pharmaceutical Analytics (LLC «CPHA») |
| record_format | Article |
| series | Разработка и регистрация лекарственных средств |
| spelling | doaj.art-1f357dd4999340f4ba807938708a8d352023-03-13T09:14:02ZrusLLC Center of Pharmaceutical Analytics (LLC «CPHA»)Разработка и регистрация лекарственных средств2305-20662658-50492022-02-01111828910.33380/2305-2066-2022-11-1-82-89939Determination of Optimal Technological Conditions for the Process of Production a Liposomal Dosage Form of CyphetrylinM. V. Dmitrieva0O. L. Orlova1A. V. Lantsova2I. I. Krasnyuk3ФГБУ «Национальный медицинский исследовательский центр онкологии имени Н. Н. Блохина» Минздрава России (ФГБУ «НМИЦ онкологии им. Н.Н. Блохина» Минздрава России)ФГБУ «Национальный медицинский исследовательский центр онкологии имени Н. Н. Блохина» Минздрава России (ФГБУ «НМИЦ онкологии им. Н.Н. Блохина» Минздрава России)ФГБУ «Национальный медицинский исследовательский центр онкологии имени Н. Н. Блохина» Минздрава России (ФГБУ «НМИЦ онкологии им. Н.Н. Блохина» Минздрава России)ФГАОУ ВО Первый МГМУ им. И. М. Сеченова Минздрава России (Сеченовский университет)Introduction. The Laboratory for the development of dosage forms of the N. N. Blokhin National Medical Research Center of Oncology of the Ministry of Health of Russian Federation has developed a composition of an injectable liposomal dosage form based on soybean phosphatidylcholine, a hydrophobic analog of the hypothalamic hormone somatostatin − cyphetrylin, intended for the treatment of neuroendocrine tumors.Aim. Determination of optimal technological conditions for the process of obtaining a liposomal dosage form of cyphetrylin.Materials and methods. The study used the substance cyphetrylin synthesized in the of Chemical Synthesis Laboratory of the N. N. Blokhin National Medical Research Center of Oncology of the Ministry of Health of Russian Federation; soybean phosphatidylcholine S PC and polyethylene glycol-2000-distearoylphosphatidylethanolamine, produced by Lipoid GmbH (Germany); cholesterol ≥99 % (Sigma-Aldrich, Japan). For the preparation of phospholipid vesicles loaded with cyphetrylin and "empty", the methods of lipid film hydration with subsequent extrusion or homogenization of the dispersion of multi-layer liposomes were used. The obtained liposomal samples were evaluated by quality indicators − the effectiveness of the inclusion of cyphetrylin in vesicles, their average size and surface charge (zeta potential), the viscosity of the dispersion. To evaluate these characteristics, the methods of spectrophotometry, laser scattering spectroscopy, determination of the electrophoretic mobility of particles and viscometry were used.Results and discussion. It was found that the most suitable organic solvent for obtaining a solution of cyphetrylin and lipid components of the dosage form is chloroform. The duration of the drying period of the lipid film under vacuum to remove the residual solvent is determined by the ratio of the volume of the distillation flask used and the mass of its loading its loading. At the same time, hydration off the lipid film with water for injection should be carried out under conditions of low-pressure and room temperature. To obtain a dispersion of single-layer cyphetrylin liposomes of the required size, an extrusion method using nylon and polycarbonate membranes with a filter pore diameter of 0.22 and 0.2 um, respectively, was chosen.Conclusion. The optimal technological conditions for the process of obtaining a liposomal dosage form in the form of a dispersion of a hydrophobic analog of the hypothalamic hormone somatostatin − cyphetrylin are determined.https://www.pharmjournal.ru/jour/article/view/1165липосомылекарственная формадисперсиятехнологические факторыцифетрилинсоевый фосфатидилхолин |
| spellingShingle | M. V. Dmitrieva O. L. Orlova A. V. Lantsova I. I. Krasnyuk Determination of Optimal Technological Conditions for the Process of Production a Liposomal Dosage Form of Cyphetrylin Разработка и регистрация лекарственных средств липосомы лекарственная форма дисперсия технологические факторы цифетрилин соевый фосфатидилхолин |
| title | Determination of Optimal Technological Conditions for the Process of Production a Liposomal Dosage Form of Cyphetrylin |
| title_full | Determination of Optimal Technological Conditions for the Process of Production a Liposomal Dosage Form of Cyphetrylin |
| title_fullStr | Determination of Optimal Technological Conditions for the Process of Production a Liposomal Dosage Form of Cyphetrylin |
| title_full_unstemmed | Determination of Optimal Technological Conditions for the Process of Production a Liposomal Dosage Form of Cyphetrylin |
| title_short | Determination of Optimal Technological Conditions for the Process of Production a Liposomal Dosage Form of Cyphetrylin |
| title_sort | determination of optimal technological conditions for the process of production a liposomal dosage form of cyphetrylin |
| topic | липосомы лекарственная форма дисперсия технологические факторы цифетрилин соевый фосфатидилхолин |
| url | https://www.pharmjournal.ru/jour/article/view/1165 |
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