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


ERGİN A. D., Uner B.

Journal of Drug Delivery Science and Technology, cilt.84, 2023 (SCI-Expanded, Scopus) identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 84
  • Basım Tarihi: 2023
  • Doi Numarası: 10.1016/j.jddst.2023.104468
  • Dergi Adı: Journal of Drug Delivery Science and Technology
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Biotechnology Research Abstracts
  • Anahtar Kelimeler: Alzheimer, Cholesterole-free, Coenzyme Q10, Liposome, SH-SY-5Y
  • Trakya Üniversitesi Adresli: Evet

Özet

Objectives: 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. Material and methods: 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. Results: 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). Conclusions: 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.