Lipid and poly (ethylene glycol)-conjugated bi-functionalized chlorine e6 micelles for NIR-light induced photodynamic therapy

[Display omitted] •Ce6 was linked to PEG, DOPE to form an amphiphilic polymer, DP-Ce6.•The amphiphilic polymer self-assembled to form polymeric micelles, DP-Ce6-M.•The micelles prevented Ce6 aggregation, increased solubility, and cellular permeability.•Micellar treatment exhibited enhanced photo-toxicity compared to Ce6 in monolayer and 3D spheroids of lung cancer cells. To develop a photosensitizer, chlorin e6 (Ce6)-based amphiphilic polymer, DP-Ce6, where DOPE and PEG are conjugated to Ce6, which would self-assemble to form polymeric micelles (DP-Ce6-M) in aqueous environment. DP-Ce6-M were characterized for particle size, zeta potential, and singlet oxygen (1O2) generation. Cellular internalization, phototoxicity were investigated against monolayer and 3D spheroids of human lung adenocarcinoma cells (A549). DP-Ce6-M formed stable micelles with particles size of 58.2 ± 1.6 nm. Solubility of Ce6 was improved. Photoactivity of DP-Ce6-M was sustained in regard to 1O2 generation compared to free Ce6. The DP-Ce6-M showed enhanced internalization and growth inhibition in monolayer and spheroidal cells. Overall, DP-Ce6-M demonstrated the potential for further exploration as PDT agent for cancer treatment.