10.6084/m9.figshare.5314564.v1
Simone Villani
Simone
Villani
Renata Adami
Renata
Adami
Ernesto Reverchon
Ernesto
Reverchon
Anna Maria Ferretti
Anna Maria
Ferretti
Alessandro Ponti
Alessandro
Ponti
Marilena Lepretti
Marilena
Lepretti
Ivana Caputo
Ivana
Caputo
Lorella Izzo
Lorella
Izzo
pH-sensitive polymersomes: controlling swelling via copolymer structure and chemical composition
Taylor & Francis Group
2017
pH-sensitive polymersomes
ATRP
vesicles
controlled drug-release
2017-08-16 09:56:40
Journal contribution
https://tandf.figshare.com/articles/journal_contribution/pH-sensitive_polymersomes_controlling_swelling_via_copolymer_structure_and_chemical_composition/5314564
<p>pH-sensitive vesicles used as drug delivery systems (DDSs) are generally composed of protonable copolymers. The disaggregation of these nanoparticles (NPs) during drug release implies the dispersion of positively charged cytotoxic polyelectrolytes in the human body. To alleviate such issue, we synthesised A(BC)<i><sub>n</sub></i> amphiphilic block copolymers with linear (<i>n</i> = 1) and branched (<i>n</i> = 2) architectures to obtain pH-sensitive vesicles capable of releasing drugs in acidic conditions via controlled swelling instead of disaggregation. We obtained this feature by fine-tuning the relative amount of pH-sensitive and hydrophobic monomers. We studied pH-driven swelling by measuring NPs size in neutral and acidic conditions, the latter typical of tumours or inflamed tissues (pH∼6) and lysosomes (pH∼4.5). Dynamic light scattering (DLS) and zeta potential data provided useful indications about the influence of architecture and chemical composition on NPs swelling, stability and polycation release. Results demonstrated that vesicles made of linear copolymers with ∼22–28% in mol of protonable monomers in the ‘BC’ block swelled more than other species following a pH change from pH 7.4 to pH 4.5. We finally evaluated the cytotoxicity of vesicles composed of linear species, and paclitaxel (PTX) release from the latter in both cancer and normal cells.</p>