Cholesterol-rich nanoemulsion (LDE) as a novel drug delivery system to diagnose, delineate, and treat human glioblastoma

Highlights: • Cholesterol-rich nanoemulsion produced LDE as novel drug delivery system • Aluminum Chloride Phthalocyanine (PcAlCl) was successful loaded into the LDE. • LDE and LDE- PcAlCl were stable over 18 months. • PcAlCl delivered by LDE and photoactivated by PDT (Photodynamic Therapy) caused a photodamage in Glioblastoma (U87-MG). We have prepared and characterized a cholesterol-rich nanoemulsion called LDE, a mimic of classic lipoprotein macromolecules, that can be applied as a new drug delivery system for aluminum phthalocyanine chloride (PcAlCl). The LDE containing PcAlCl system prepared herein had mean size and zeta potential of 127 nm and −29 mV, respectively, and encapsulation rate efficiency was 81%, and stability of 17 months. Compared to classical liposomes, LDE was more efficient, especially in brain diseases like glioblastoma (GBM), as revealed by tests on the U-87 MG cell line. The LDEPc formulation did not display dark cytotoxicity, as expected. The best light dose for LDEPc was 1.0 J·cm⁻²: its activity was 55% higher than PcAlCl in a compatible organic medium. In the U-87 MG cells, apoptosis was the preferential pathway activated by PDT. These results strongly support the use of LDE as a new theranostic system.