pH-responsive niosome-based nanocarriers of antineoplastic agents

• DOI: 10.1039/d4ra01334d
• Publication Date: 2024-04-11T12:55:21Z
• Authors: Viliana Gugleva; Rositsa Mihaylova; Georgi Momekov; Katya Kamenova; Aleksander Forys; Barbara Trzebicka; Maria Petrova; Iva Ugrinova; Denitsa Momekova; Petar D. Petrov
• Keywords: Nanocarriers; Niosome

Differences in pH between the tumour interstitium and healthy tissues can be used to induce conformational changes nanocarrier structure, thereby triggering drug release at desired site. In present study, novel pH-responsive nanocarriers were developed by modifying conventional niosomes with hexadecyl-poly(acrylic acid)n copolymers (HD-PAAn). Niosomal vesicles prepared thin film hydration method using Span 60, 60/Tween 60 cholesterol as main constituents, HD-PAA modifiers of different concentrations (0.5, 1, 2.5, 5 mol%). Next, two model substances, a water-soluble fluorescent dye (calcein) hydrophobic agent pronounced antineoplastic activity (curcumin), loaded aqueous core membrane elaborated niosomes, respectively. Physicochemical properties blank such hydrodynamic diameter (Dh), size distribution, zeta potential, morphology pH-responsiveness investigated detail. The cytotoxicity niosomal curcumin was evaluated against human malignant cell lines origins (MJ, T-24, HUT-78), mechanistic aspects proapoptotic effects elucidated. formulation composed 60/cholesterol/2.5% HD-PAA17 exhibited optimal physicochemical characteristics (Dh 302 nm; ζ potential -22.1 mV; high entrapment 83%), pH-dependent improved cytotoxic apoptogenic compared free curcumin.