Design and Characterization of Maltoheptaose-b-Polystyrene Nanoparticles, as a Potential New Nanocarrier for Oral Delivery of Tamoxifen

Molecules

Fabio Sonvico¹  Annalisa Bianchera¹  Adryana Rocha Clementino¹  Francesca Buttini¹  Redouane Borsali²  Eride Quarta³  Ilaria Dotti³  Marcos Antonio Villetti⁴  Patricia Regina Ebani⁴ 

[1] Biopharmanet-TEC, University of Parma, 43124 Parma, Italy;Department of Chemistry, University Grenoble Alpes, CNRS, CERMAV, 38000 Grenoble, France;Department of Food and Drug, University of Parma, 43124 Parma, Italy;Laboratório de Espectroscopia e Polímeros (Lepol), Departamento de Física, Universidade Federal de Santa Maria,Santa Maria 97105-900, Brazil;

关键词: tamoxifen citrate;    block copolymer;    cytotoxicity;    breast cancer;   

DOI  :  10.3390/molecules26216507

来源: DOAJ

【 摘 要 】

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.

【 授权许可】

Unknown