Evaluation of the cytotoxic potential of liposomal gemcitabine

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Abstract

Background. Gemcitabine is used in oncology for the treatment of various solid tumors, including lung cancer. Gemcitabine exhibits high therapeutic efficacy by inhibiting DNA synthesis and inducing apoptosis in tumor cells. However, the drug has drawbacks, such as a short half-life and rapid metabolic degradation, necessitating frequent administration of high doses, which increases the risk of side effects. To reduce toxicity and enhance therapeutic efficacy, we developed a liposomal formulation of gemcitabine.

Aim. To compare the cytotoxic activity of liposomal gemcitabine and gemcitabine solution on the A549 lung cancer cell line.

Materials and methods. The cytotoxicity of liposomal gemcitabine and gemcitabine solution was evaluated on the human lung adenocarcinoma cell line A549. Cells were cultured in the presence of liposomal gemcitabine and gemcitabine solution in vitro for 72 hours, and the cytotoxicity of the drugs was assessed using the MTT assay.

Results. Liposomal gemcitabine demonstrated higher cytotoxicity compared to free gemcitabine. Half maximal inhibitory concentration value for liposomal gemcitabine was 0.47 μM, while that for free gemcitabine was 9.6 μM.

Conclusion. The liposomal form of gemcitabine exhibits significantly higher cytotoxic activity compared to the free gemcitabine solution against the A549 lung cancer cell line. Incorporation of gemcitabine into liposomes improved drug penetration into tumor cells and protected it from premature degradation.

About the authors

G. A. Oborotov

N.N. Blokhin National Medical Research Center of Oncology, Ministry of Health of Russia; I.M. Sechenov First Moscow State Medical University, Ministry of Health of Russia

Author for correspondence.
Email: oborot-off@yandex.ru
ORCID iD: 0009-0001-5671-1923

Grigory A. Oborotov.

24 Kashirskoe Shosse, Moscow 115522; Bld. 8, 2 Trubetskaya St., Moscow 119048

Russian Federation

A. A. Rudakova

N.N. Blokhin National Medical Research Center of Oncology, Ministry of Health of Russia

ORCID iD: 0000-0001-7266-7689

Anna A. Rudakova.

24 Kashirskoe Shosse, Moscow 115522

Russian Federation

M. A. Baryshnikova

N.N. Blokhin National Medical Research Center of Oncology, Ministry of Health of Russia

ORCID iD: 0000-0002-6688-8423

Maria A. Baryshnikova.

24 Kashirskoe Shosse, Moscow 115522

Russian Federation

M. V. Dmitrieva

N.N. Blokhin National Medical Research Center of Oncology, Ministry of Health of Russia

ORCID iD: 0000-0001-6740-5692

Мaria V. Dmitrieva.

24 Kashirskoe Shosse, Moscow 115522

Russian Federation

I. I. Krasnyuk

I.M. Sechenov First Moscow State Medical University, Ministry of Health of Russia

ORCID iD: 0000-0002-7242-2988

Ivan I. Krasnyuk.

Bld. 8, 2 Trubetskaya St., Moscow 119048

Russian Federation

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