OpenNano (Nov 2022)
pH-sensitive oleuropein-loaded niosome: Efficient treatment for metastatic brain tumors in initial steps in-vivo
Abstract
Brain tumors remain life-threatening cancer cases in humans. The short survival rates are almost related to therapeutic restrictions, insufficiency in accurate diagnosis, and the inability of the available therapeutics to reach the brain tissue with the efficient doses required for treatment. The present study aims to present oleuropein-loaded niosome (Oleu-Nio) as an efficient drug delivery system to the brain parenchyma of female rats bearing 4T1 metastatic breast cancer (MBC) cells. The Nio formulation, as Tween 60/ cholesterol 1:1 M ratio, was selected regarding the small size of 79.37 ± 0.12 nm, polydispersity index (Pdi) 0.230 ± 0.043, Zeta-potential 1.38 ± 0.074 mv, high stability for more than 50 days, and high entrapment efficiency 96.89 ± 0.241. Furthermore, it has described sensitivity to acidic pH = 5.3, resulting in a controlled release behavior in-vitro vs. neutral pH = 7.4. In-vitro, the viability of 4T1 cancer cells has decreased significantly in the presence of Oleu-Nio (IC50 = 92.679 µg/ml) compared to free Oleu, where IC50 was none detected. Fluorescent microscopy figures have uncovered the role of Nio in increasing the uptake via 4T1 cancer cells. Moreover, treating female rats presenting brain metastasis (BM) with 10 doses of Oleu-Nio (25 mg/kg body weight) via intravenous route has improved the survival rate for more than 45 days vs. 34.5 days in those treated with Oleu and 16.5 days in the control group. These findings remain promising in drug delivery, especially for brain-related diseases like brain tumors. Additionally, Oleu could be presented as a suitable and safe treatment against primary and metastatic breast cancers.
