4.0 Article

Lomustine Incorporated Lipid Nanostructures Demonstrated Preferential Anticancer Properties in C6 Glioma Cell Lines with Enhanced Pharmacokinetic Profile in Mice

Journal

ACTA CHIMICA SLOVENICA
Volume 68, Issue 4, Pages 970-982

Publisher

SLOVENSKO KEMIJSKO DRUSTVO
DOI: 10.17344/acsi.2021.6977

Keywords

Lomustine; lipid nanostructure; C6 glioma cells; cellular uptake; pharmacokinetic; hemolysis

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The study aimed to improve the delivery of lomustine to brain tumor cells using lipid-based nanostructures, and experimental results showed potential anti-cancer effects. The selected LNLs demonstrated improved pharmacokinetic profiles in blood and brain in experimental mouse models, indicating potential for future clinical translation.
Effective treatment of glioma still stands as a challenge in medical science. The work aims for the fabrication and evaluation of lipid based nanostructures for improved delivery of lomustine to brain tumor cells. Experimental formulations (LNLs) were developed by modified lipid layer hydration technique and evaluated for different in vitro characteristics like particle size analysis, surface charge, surface morphology, internal structure, in vitro drug loading, drug release profile etc. Anticancer potential of selected LNLs was tested in vitro on C6 glioma cell line. Electron microscopic study depicted a size of less than 50 nm for the selected LNLs along wirh 8.8% drug loading with a sustained drug release tendency over 48 h study period. Confocal microscopy revealed resonable internalization of the selected LNL in C6 cells. LNLs were found more cytotoxic than free drug and blank nanocarriers as depicted from MTT assay. The selected LNL showed improved pharmacokinetic profile both in blood and brain in the experimental mice models along with negligible hemolysis in mice blood cells. Further studies are warranted for the future translation of LNLs at clinics.

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