Formulation and characterization of stimuli-responsive lecithin-based liposome complexes with poly(acrylic acid)/poly(N,N-dimethylaminoethyl methacrylate) and Pluronic® copolymers for controlled drug delivery

SIMÕES, M.G.; HUGO, A. A.; GOMEZ-ZAVAGLIA, ANDREA; SIMOES, P.N; ALVES, P.A

Pharmaceutics

MDPI

Lugar: Basel; Año: 2022

1999-4923

Polymer-liposome complexes (PLCs) can be efficiently applied for the treatment and/or diagnosis of cancerous, neurological, dermatological, ophthalmic, and orthopedic diseases. This work reports the development and characterization of temperature/pH sensitive PLCs-based systems for controlled release. The selected hydrophilic polymeric setup consists in copolymers of Pluronic®-poly(acrylic acid) (PLU-PAA) and Pluronic®-poly(N,N-dimethylaminoethyl methacrylate) (PLU-PD) synthesized by atom transfer radical polymerization (ATRP). The copolymers were incorporated into liposomes formulated from soybean lecithin, with different copolymer/phospholipid ratios (2.5, 5 and 10 %). The developed PLCs were characterized in terms of particle size, polydispersity, surface charge, capacity of release and encapsulation efficiency. Their cytotoxic potential was assessed by determining the viability of human epithelial cells exposed to them. The results showed that the incorporation of the synthesized copolymers positively contributed to the stabilization of the liposomes. The main accomplishments of this work were the innovative synthesis of PLU-PD and PLU-PAA by ATRP, and the liposome stabilization by their incorporation. The formulated PLCs exhibited relevant characteristics, notably stimuli-responsive attributes upon slight changes of pH and/or temperature, with proved absence of cellular toxicity, which could be of interest for the treatment or diagnosis of all diseases that cause some particular pH/temperature change in the target area.