278
Volume 5, Issue 10: Special Issue
(EJAR)
ISSN: 2181-2020
MPHAPP
THE 6TH INTERNATIONAL SCIENTIFIC AND PRACTICAL
CONFERENCE
“
MODERN PHARMACEUTICS: ACTUAL
PROBLEMS AND PROSPECTS
”
TASHKENT, OCTOBER 17, 2025
in-academy.uz
SYNTHESIS OF IMATINIB ESSINATE AND ITS INCLUSION COMPLEXES
INHIBITING CANCER CELL PROLIFERATION
Tuymurodova R.A.
Islomov B.R.
Saidov R.R.
Tashkent Pharmaceutical Institute, Tashkent city, Republic of Uzbekistan
e-mail: barakatulloislomov@gmail.com
https://doi.org/10.5281/zenodo.17334317
Relevance:
Cancer is one of the fastest-growing diseases and ranks second worldwide after
cardiovascular diseases in terms of mortality. The number of patients diagnosed with cancer is
increasing every year, and it is predicted that by 2040 about 29.4 million new cases will be registered.
Such alarming data highlight the urgent need to discover new anticancer drugs and develop effective
treatment methods. Over the past two decades, 237 new bioactive substances have been developed
and recommended for medical use worldwide for cancer therapy. More than 70 of them inhibit cancer
cell proliferation through tyrosine kinase receptor inhibition. One of these drugs is imatinib mesylate.
Although imatinib has been successful in cancer treatment, its use has certain limitations. More than
50% of patients treated with imatinib develop resistance, leading to therapy modification in 30–40%
of cases. In addition, more than 60% of patients experience edema as an adverse effect. Therefore,
the discovery of new anticancer agents with higher efficacy and fewer side effects remains an urgent
task.
Objective:
To synthesize imatinib essinate and its inclusion complex.
Methods:
An ethanolic solution of imatinib was gradually mixed with an ethanolic solution of
escin under constant stirring at a controlled temperature for 3 hours using a magnetic stirrer. The
reaction was carried out in a non-hermetic vessel at 40°C, during which the evaporation of ethanol
led to a decrease in the solution volume. The increasing viscosity of escin may also have contributed
to the reduced movement of the stir bar. The solution gradually became lighter in color upon visual
observation. The resulting mixture was then stored in the dark for 16 hours, yielding a transparent,
light green solution. This solution was filtered using filter paper.
For the synthesis of the escimatrin substance, 0.49 g of imatinib, 1.13 g of escin, and 1.14 g of
hydroxypropyl-β-cyclodextrin were each dissolved separately in 20 ml of ethanol and stirred until
complete dissolution. Afterwards, at a constant temperature of 40°C, the escin solution was slowly
added to the imatinib solution. Hydroxypropyl-β-cyclodextrin was then introduced, and the mixture
was stirred at 300–700 rpm for 4 hours using a magnetic stirrer. The resulting solution was filtered
through filter paper and evaporated.
Results:
The synthesis was carried out five times, and the average yields were calculated,
resulting in 89.3% for imatinib essinate and 91.8% for escimatrin. The obtained substances were
analyzed using Scanning Electron Microscopy (SEM), Powder X-ray Diffraction (XRD), IR and UV
spectroscopy, as well as Thermogravimetric/Differential Thermal Analysis (TG/DTA). Comparative
analyses with the starting materials confirmed that the synthesized compounds represent individual
substances.
Conclusion:
Visual observations along with SEM, UV, IR, TG/DTA, and XRD analyses
confirmed the successful synthesis of imatinib essinate and escimatrin. Future in vitro and in vivo
studies will help to further elucidate the pharmacological properties of these compounds.
