Purpose: Malignant cerebral tumors have poor prognosis and the blood-brain barrier is a major hindrance for most drugs to reach those tumors. Lipid nanoparticles (LDE) that bind to lipoprotein receptors may carry anticancer drugs and penetrate the cells through those receptors that are overexpressed in gliomas. The aim was to investigate the in vivo uptake of LDE by human cerebral tumors.
Methods: Twelve consecutive patients (4 with glioblastomas, 1 meduloblastoma, 1 primary lymphoma, 2 with non-cerebral metastases and 4 with benign tumors) scheduled for tumor excision surgery were injected intravenously, 12 h before surgery, with LDE labeled 14C-cholesterol oleate. Fragments of tumors and of normal head tissues (muscle, periosteum, dura mater) discarded by the surgeon were submitted to lipid extraction and radioactive counting.
Results: Tumor LDE uptake (range: 10-283 d.p.m./g of tissue) was not lower than that of normal tissues (range: 20-263 d.p.m./g). Malignant tumor uptake was threefold greater than benign tumor uptake (140 ± 93 vs 46 ± 18 d.p.m./g, p < 0.05). Results show that LDE can concentrate in brain malignant tumors and may be used to carry drugs directed against those tumors.
Conclusion: As LDE was previously shown to markedly decrease drug toxicity this new therapeutic strategy should be tested in future trials.
Keywords: Blood–brain barrier; Glioma treatment; LDL-receptor and cancer; Nanoemulsions; Solid lipid nanoparticles.
© 2022. The Author(s), under exclusive licence to Springer Science+Business Media, LLC, part of Springer Nature.