Preparation of temozolomide-loaded polymer particles and study of their antitumor activity in models of glioma and melanoma

• Published in: Russian journal of bioorganic chemistry Vol. 43; no. 5; pp. 552 - 560
• Main Authors: Nikolskaya, E. D., Zhunina, O. A., Vasilenko, E. A., Yabbarov, N. G., Tereshchenko, O. G., Sokol, M. B., Popenko, V. I., Severin, E. S.
• Format: Journal Article
• Language: English
• Published: Moscow Pleiades Publishing 01.09.2017; Springer Nature B.V
• Subjects: Anticancer properties; Biochemistry; Biomedical and Life Sciences; Biomedicine; Bioorganic Chemistry; Formulations; Life Sciences; Life span; Melanoma; Nanoparticles; Organic Chemistry; Pharmacology; Polymers; Rodents; Toxicity; temozolomide; glioma; melanoma; polymer nanoparticles; PLGA; antitumor activity
• ISSN: 1068-1620; 1608-330X
• DOI: 10.1134/S1068162017050090

Temozolomide (TMZ) is a cytostatic drug used in treatment of patients with malignant gliomas and melanomas. The development of innovative formulations for delivery of TMZ into target cells in order to reduce its systemic toxicity and gain prolonged effect is a topical problem of modern biotechnology and pharmacology. The article presents experimental data on development of the TMZ polymer-based formulation. The TMZ formulation presents nanoparticles with average size of 300 nm exhibiting high in vitro cytotoxic activity against melanoma and glioma cells (cell lines C6, U377MG, B16, and Mel-10). Melanoma (B16 cell line) bearing mice (C57Bl/61) treated by TMZ polymer nanoparticles revealed inhibition of tumor growth and increase of the animal lifespan. Also, loading of TMZ into the polymer particles was shown to decrease acute toxicity of the drug compared to the intact drug.