Разработка и регистрация лекарственных средств (May 2019)

Study of Desorbtion and Exemption of Terpeno-indole Alkaloids of Vinkristin and Vinblastin from Erythrocitary Cell Carriers

  • O. V. Trineeva,
  • A. D. Khalahakun

DOI
https://doi.org/10.33380/2305-2066-2019-8-2-16-21
Journal volume & issue
Vol. 8, no. 2
pp. 16 – 21

Abstract

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Introduction. Employees of the Department of Pharmaceutical Chemistry and Pharmaceutical Technology have obtained modified forms of terpino-indole alkaloids (ТIA) and vinbristine (VCR) and vinblastine (VBL) known in the treatment of cancer diseases by incorporating them into the erythrocyte carriers (EN) by the modified method of hypoosmotic lysis in the modified (aprotic solvent dimethyl sulfoxide (DMSO) and polyethylene glycol (PEG 4000) and unmodified media.Aim. The aim of the work was to study the desorption and release of terpene-indole vincristine and vinblastine alkaloids from previously obtained cellular erythrocyte carriers.Materials and methods. In the experiment performed, the release characteristics of encapsulated preparations from erythrocytes were determined. TIA preparations were released from erythrocyte form in 6 hours: VCR – 54.5305%, VCR : PEG-4000 (1:5) – 53.3305%, VCR : PEG-4000 (1:10) – 40.1283%, VCR : PEG-4000 (1:20) – 39.9869%, VCR : DMSO (2 mg/ml) – 54.2354%, VBL – 68.0656%; VBL : PEG-4000 (1:10) – 63.8941%; VBL : PEG-4000 (1:20) – 60.7455%; VBL : PEG-400 (1:20) – 60.3529%; VBL : DMSO (2 mg/ml) – 64.5006%. The rate of release from an erythrocyte form encapsulated in a medium modified with DMSO is significantly higher than that encapsulated in an unmodified medium. The average rate of TIA release from erythrocyte forms encapsulated in PEG medium is approximately the same.Results and discussion. The results show that the release of hemoglobin from TIA encapsulated erythrocytes compared with non-encapsulated EN is small. The results show that, on average, 8.242 ± 0.3135% of hemoglobin is released from TIA encapsulated with EN, compared to control erythrocytes – 7.53% after 6 h of incubation at 37 °C. The release of hemoglobin from the TIA of encapsulated erythrocytes in modified media is less than that encapsulated in unmodified medium.Conclusion. Based on these results, it can be suggested that PEG can bind to the erythrocyte membrane and stabilize it.

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