The development of new technology of the dosage form for intravenous administration indolocarbazole derivative LHS-1208


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Abstract

Objective. Aim of this work was to create a stable liposomal dosage form of native hydrophobic antitumor compound from the group of indolocarbazoles - LHS-1208. Materials and methods. Quantitative analysis of the drug content in liposomes was determined by spectrophotometry with a standard sample at X = 320 ± 2 nm. The encapsulation was investigated as the ratio of LHS-1208 concentration in the liposomal dispersion after extrusion through nylon membrane filters 0.22 ^m “Pall” to concentration LHS-1208 in liposomal dispersions before filtration. pH of the liposome was determitaned by the method of potentiometry. The size of liposomes was evaluated by nanosizer. Cytotoxic activity was studied by MTT-test. Results. Experimental liposomal models of LHS-1208 with different molar ratios of the components were obtained and analyzed. Composition with the molar ratios LHS-1208: lecithin 1:150, and lecithin : cholesterol: PEG-2000 - 1:0,2:0,003 was selected. Encapsulation percentage of LHS-1208 was 94 % and size of the vesicles was 185±10 nm. Cytotoxic activity of liposomal LHS-1208 was studied, IC0 was 1.24 ^g/ml. Conclusion. As a result of complex pharmaceutical research determined the optimum composition of the components and the technology for production of liposomal dosage form LHS-1208.

About the authors

I. D. Gulyakin

N.N. Blokhin Russian Cancer Research Center, Ministry of Health of Russia

Author for correspondence.
Email: ilya.gulyakin@yandex.ru
Russian Federation

A. . Hashem

N.N. Blokhin Russian Cancer Research Center, Ministry of Health of Russia

Russian Federation

L. L. Nikolaeva

N.N. Blokhin Russian Cancer Research Center, Ministry of Health of Russia

Russian Federation

M. V. Dmitrieva

N.N. Blokhin Russian Cancer Research Center, Ministry of Health of Russia

Russian Federation

D. A. Afanasieva

N.N. Blokhin Russian Cancer Research Center, Ministry of Health of Russia

Russian Federation

M. A. Baryshnikova

N.N. Blokhin Russian Cancer Research Center, Ministry of Health of Russia

Russian Federation

N. A. Oborotova

N.N. Blokhin Russian Cancer Research Center, Ministry of Health of Russia

Russian Federation

A. V. Lantsova

N.N. Blokhin Russian Cancer Research Center, Ministry of Health of Russia

Russian Federation

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