Unlocking the brain: Biodistribution insights into tween 80 nanoliposomes in healthy brains
Source: PubMed Central Open Access, NCBI / U.S. National Library of Medicine
Limited drug penetration across the blood–brain barrier hinders brain tumor therapy. This study evaluated doxorubicin-loaded nanoliposomes with varying Tween 80 contents, investigating formulation characteristics, release profiles, cytotoxicity on cancer and healthy cells, and tissue distribution in healthy models. Nanoliposomes were preparedthin-film hydration. Physicochemical properties,drug release at physiological and acidic pH, and cytotoxicity (MTT assay and IC) on C6 cells and normal NIH 3 T3 cells (including empty-carrier biosafety) were assessed.tissue distribution and histopathological safety were also examined in mice. Formulations showed composition-dependent size and 3-month stability. Formulation F2 emerged as the lead candidate, exhibiting optimal size (142.4 nm), PDI (0.139), encapsulation efficiency (82.4%), and pH-responsive release (80–90% at pH 5.5 90% viability with empty blanks and a markedly higher IC(20.67 μg/mL) than free DOX., F2 achieved superior brain accumulation at 24 and 48 h (2.61 and 2.78 μg/g;< 0.05DOX) while reducing cardiac uptake (2.2914.49 μg/g at 24 h). Formulation F2 balances colloidal stability, reduced cardiotoxicity, and superior brain accumulation, supporting its potential for neuro-oncology applications. ab0005 Graphical abstract Unlabelled Image http://www.w3.org/1999/xlink lk0050 float portrait ga1.webp f0050 anchor portrait graphical ab0010 Highlights • Tween 80-modified liposomes exhibited distinct cytotoxicity in C6 cells. li0
Abstract
Limited drug penetration across the blood–brain barrier hinders brain tumor therapy. This study evaluated doxorubicin-loaded nanoliposomes with varying Tween 80 contents, investigating formulation characteristics, release profiles, cytotoxicity on cancer and healthy cells, and tissue distribution in healthy models. Nanoliposomes were preparedthin-film hydration. Physicochemical properties,drug release at physiological and acidic pH, and cytotoxicity (MTT assay and IC) on C6 cells and normal NIH 3 T3 cells (including empty-carrier biosafety) were assessed.tissue distribution and histopathological safety were also examined in mice. Formulations showed composition-dependent size and 3-month stability. Formulation F2 emerged as the lead candidate, exhibiting optimal size (142.4 nm), PDI (0.139), encapsulation efficiency (82.4%), and pH-responsive release (80–90% at pH 5.5 90% viability with empty blanks and a markedly higher IC(20.67 μg/mL) than free DOX., F2 achieved superior brain accumulation at 24 and 48 h (2.61 and 2.78 μg/g;< 0.05DOX) while reducing cardiac uptake (2.2914.49 μg/g at 24 h). Formulation F2 balances colloidal stability, reduced cardiotoxicity, and superior brain accumulation, supporting its potential for neuro-oncology applications. ab0005 Graphical abstract Unlabelled Image http://www.w3.org/1999/xlink lk0050 float portrait ga1.webp f0050 anchor portrait graphical ab0010 Highlights • Tween 80-modified liposomes exhibited distinct cytotoxicity in C6 cells. li0005 • Doxorubicin release was accelerated under acidic tumor-like conditions. li0010 • The liposomes enhanced brain accumulation of doxorubicin. li0015 • Formulation with 0.25% Tween 80 showed a considerable brain accumulation. li0020 • Nanoliposomes remained physically stable for at least 3 months. li0025 simple l0005 author-highlights ab0015