Characterization, optimization, and in vitro evaluation of cholesterol-free liposomes

Alzheimer's disease (AD) is a neurological disorder that causes dementia and a progressive loss of thinking, social, and memory abilities. Afterwards, this worsening induces the person incapable of doing even the most fundamental duties. Recent research have proven that Coenzyme-q10 (CoQ10), one of the endogenous fatty acids, suppresses phosphorylated Tau protein which is GM1-ganglioside-bound amyloid β-protein (GM1-Aβ), and inhibiting the formation of amyloid plaques in Alzheimer's disease. Unfortunately, CoQ10 is poorly absorbed due to its high molecular weight (863.34 g/mol) and high lipophilicity, and its bioavailability is quite low. Therefore, we developed the CoQ10-loaded, cholesterol-free liposomes to get across the limitations. Liposomes were developed by ether injection method, and physicochemical characterization of the liposomes were evaluated in terms of particle size, size distribution (PDI), zeta potential, encapsulation efficiency (% EE), and process recovery as well. Release study, DSC analysis, morphological analysis, and cytotoxicity assay were performed with optimized formulations. The particle size, PDI, zeta potential, EE%, and process recovery of the formulations ranged from 343.8 to 167.9 nm; 0.269 to 0.431; (−56) to (−31.7); 18.15–93.48%; 74.63 to 99.62, respectively. According to cytotoxicity tests, liposomes have no significant toxic effect on cells while having decreased p-tau 181 and p-tau 231 proteins (p > 0.05). As a result, the novel cholesterol-free liposome formulation were proved that it might be candidate of including the therapeutical guideline for the future alzheimer's disease treatment with these substantial results.