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

Tamoxifen citrate (TMC), a non-steroidal antiestrogen drug used for the treatment of breast cancer, was loaded in a block copolymer of maltoheptaose- -polystyrene (MH- -PS) nanoparticles, a potential drug delivery system to optimize oral chemotherapy. The nanoparticles were obtained from self-assemb...

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Bibliographic Details
Published in:	Molecules (Basel, Switzerland) Vol. 26; no. 21; p. 6507
Main Authors:	Villetti, Marcos Antonio, Clementino, Adryana Rocha, Dotti, Ilaria, Ebani, Patricia Regina, Quarta, Eride, Buttini, Francesca, Sonvico, Fabio, Bianchera, Annalisa, Borsali, Redouane
Format:	Journal Article
Language:	English
Published:	Switzerland MDPI AG 28-10-2021 MDPI
Subjects:	Antiestrogens block copolymer Block copolymers Breast cancer Breast carcinoma Breast Neoplasms Cell Line, Tumor Cell Survival - drug effects Chemical Phenomena Chemotherapy Chromatography, High Pressure Liquid Citric acid Controlled release Copolymers Cytotoxicity Dose-Response Relationship, Drug Drug Carriers - chemistry Drug Compounding Drug delivery Drug Delivery Systems Drug Liberation Efficiency Encapsulation Estrogens Female Glucans - chemistry Humans Kinetics Lipophilic Manufacturing Metabolism Metabolites Models, Theoretical Molecular Structure Morphology Nanoparticles Nanoparticles - chemistry Nanostructured materials Particle Size Particle size distribution Permeability Physicochemical properties Polyethylene glycol Polystyrene resins Polystyrenes - chemistry Selective Estrogen Receptor Modulators - administration & dosage Self-assembly Size distribution Solvents Sustained release Tamoxifen Tamoxifen - administration & dosage Tamoxifen - chemistry Tamoxifen citrate Ultrasonic imaging Zeta potential block copolymer breast cancer tamoxifen citrate cytotoxicity
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Summary:	Tamoxifen citrate (TMC), a non-steroidal antiestrogen drug used for the treatment of breast cancer, was loaded in a block copolymer of maltoheptaose- -polystyrene (MH- -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 ) 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.
ISSN:	1420-3049 1420-3049
DOI:	10.3390/molecules26216507