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

Nikolskaya, Elena; Жунина, О. А.; Vasilenko, E. A.; Yabbarov, N. G.; Tereshchenko, O. G.; Sokół, Maria; Попенко, В. И.; Severin, E. S.

doi:10.1134/s1068162017050090

Cited by 3 publications

(1 citation statement)

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“…Moreover, many regulators, including the FDA and the EMA, have already approved PLGA-based drugs for medical application [ 15 ]. Among the most important advantages of PLGA application, we can emphasize the following: support of the properties and structures of cytostatic and antimicrobial molecules loaded into matrixes [ 16 , 17 ]; the reproducible in silico simulation of drug–polymer interaction results [ 18 ]; the effective encapsulation of lipophilic compounds [ 19 ]; and the simplified application and administration of resultant PLGA formulations due to their high stability and water solubility [ 20 ].…”

Section: Introductionmentioning

confidence: 99%

Thymol-Modified Oleic and Linoleic Acids Encapsulated in Polymeric Nanoparticles: Enhanced Bioactivity, Stability, and Biomedical Potential

Sokol,

Sokhraneva,

Groza

et al. 2023

Polymers

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Unsaturated fatty acids, such as oleic acid (OA) and linoleic acid (LA), are promising antimicrobial and cytostatic agents. We modified OA and LA with thymol (TOA and TLA, respectively) to expand their bioavailability, stability, and possible applications, and encapsulated these derivatives in polymeric nanoparticles (TOA-NPs and TLA-NPs, respectively). Prior to synthesis, we performed mathematical simulations with PASS and ADMETlab 2.0 to predict the biological activity and pharmacokinetics of TOA and TLA. TOA and TLA were synthesized via esterification in the presence of catalysts. Next, we formulated nanoparticles using the single-emulsion solvent evaporation technique. We applied dynamic light scattering, Uv-vis spectroscopy, release studies under gastrointestinal (pH 1.2–6.8) and blood environment simulation conditions (pH 7.4), and in vitro biological activity testing to characterize the nanoparticles. PASS revealed that TOA and TLA have antimicrobial and anticancer therapeutic potential. ADMETlab 2.0 provided a rationale for TOA and TLA encapsulation. The nanoparticles had an average size of 212–227 nm, with a high encapsulation efficiency (71–93%), and released TOA and TLA in a gradual and prolonged mode. TLA-NPs possessed higher antibacterial activity against B. cereus and S. aureus and pronounced cytotoxic activity against MCF-7, K562, and A549 cell lines compared to TOA-NPs. Our findings expand the biomedical application of fatty acids and provide a basis for further in vivo evaluation of designed derivatives and formulations.

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