Abstract
Tamoxifen citrate (TMC), a non-steroidal antiestrogen drug used for the treatment of breast cancer, was loaded in a block copolymer of maltoheptaose-b-polystyrene (MH-b-PS) nanoparticles, a potential drug delivery system to optimize oral chemotherapy. The nanoparticles were obtained from self-assembly of MH-b-PS using the standard and reverse nanoprecipitation methods. The MH-b-PS@TMC nanoparticles were characterized by their physicochemical properties, morphology, drug loading and encapsulation efficiency, and release kinetic profile in simulated intestinal fluid (pH 7.4). Finally, their cytotoxicity towards the human breast carcinoma MCF-7 cell line was assessed. The standard nanoprecipitation method proved to be more efficient than reverse nanoprecipitation to produce nanoparticles with small size and narrow particle size distribution. Moreover, tamoxifen-loaded nanoparticles displayed spherical morphology, a positive zeta potential and high drug content (238.6 ± 6.8 µg mL−1) and encapsulation efficiency (80.9 ± 0.4 %). In vitro drug release kinetics showed a burst release at early time points, followed by a sustained release profile controlled by diffusion. MH-b-PS@TMC nanoparticles showed higher cytotoxicity towards MCF-7 cells than free tamoxifen citrate, confirming their effectiveness as a delivery system for administration of lipophilic anticancer drugs.
Highlights
In the field of oncology, special attention has been paid to the potential use of alternative routes to parenteral administration of anticancer drugs in order to improve the quality of life of patients
When a maltoheptaose-based copolymer is dissolved in a solvent that is thermodynamically good for one block but poor for the other, spontaneous self-assembling occurs, leading to the formation of a core-shell structure with the solvophobic block forming the core and the solvophilic part forming the shell of the nanoparticle
Another important feature of the maltoheptaose-based copolymer is that it has suitable characteristics to interact with different target cancer cells: many cancer cells are known to have increased metabolism and overexpression of glucose transporters, a phenomenon known as Warburg effect [26]
Summary
In the field of oncology, special attention has been paid to the potential use of alternative routes to parenteral administration of anticancer drugs in order to improve the quality of life of patients. When a maltoheptaose-based copolymer is dissolved in a solvent that is thermodynamically good for one block but poor for the other, spontaneous self-assembling occurs, leading to the formation of a core-shell structure with the solvophobic block forming the core and the solvophilic part forming the shell of the nanoparticle Another important feature of the maltoheptaose-based copolymer is that it has suitable characteristics to interact with different target cancer cells: many cancer cells are known to have increased metabolism and overexpression of glucose transporters, a phenomenon known as Warburg effect [26]. Several manufacturing parameters were evaluated to optimize the physico–chemical and biopharmaceutical properties of the nanoparticles, such as content of oil, drug, copolymer and mixture of solvents (THF/H2 O), temperature, filtration, and use of ultrasound This is the first report on the development of MH-b-PS@TMC nanoparticles with a detailed investigation of its physicochemical properties, morphology, drug content and encapsulation efficiency, drug release profile in simulated intestinal fluid (pH 7.4), and cytotoxicity towards the human breast carcinoma cell line MCF-7
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