Precise engineering of Iguratimod and Rapamycin drugs loaded polymeric nanomaterials for the treatment of glioma cancer cells

Abstract Malignant glioma is among the worst kinds of brain cancer, and despite breakthroughs in therapy, patient prognosis remains dismal, with an average life of 15 months. Treatment with standard chemotherapy does not provide the appropriate medication dosage to the cancer location, owing to insufficient blood-brain barrier (BBB) permeability, especially hydrophilic drugs. The present study was to construct and assess the therapeutic efficacy of Iguratimod (IGU) and Rapamycin (RAPA) encapsulated-polylactic-co-glycolic acid (PLGA) and polyethylene glycol (PEG)-based nanomaterials (IGU/RAPA@NMs), which displayed inhibition of glioma cells proliferation in vitro. IGU/RAPA@NMs with an average size of 50–100 nm have fabricated using an improved double-emulsion (W/O/W) approach. The electron microscopic techniques have confirmed newly constructed IGU/RAPA@NMs morphology. Following successful synthesis, the anticancer properties of LN229 and U251 glioma cancer cell lines were assessed. The morphological and apoptosis biochemical studies including AO-EB (acridine bromide orange ethidium), nuclear staining. Importantly, choosing IGU/RAPA@NMs as a target nanomaterial, a suggestively improved safety profile relative to the animal model was confirmed, suggesting that these nanomaterials can be utilized as potential candidates for glioma cancer therapy and deserve further investigations.