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-b-polystyrene (MH-b-PS) nanoparticles, a potential drug delivery system to optimize oral chemotherapy. The nanopa...

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Autores principales:	Marcos Antonio Villetti, Adryana Rocha Clementino, Ilaria Dotti, Patricia Regina Ebani, Eride Quarta, Francesca Buttini, Fabio Sonvico, Annalisa Bianchera, Redouane Borsali
Formato:	article
Lenguaje:	EN
Publicado:	MDPI AG 2021
Materias:	tamoxifen citrate block copolymer cytotoxicity breast cancer Organic chemistry QD241-441
Acceso en línea:	https://doaj.org/article/a6d6ee2b69a846b0bd87357dab1c2a3a
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spelling	oai:doaj.org-article:a6d6ee2b69a846b0bd87357dab1c2a3a2021-11-11T18:30:22ZDesign and Characterization of Maltoheptaose-<i>b</i>-Polystyrene Nanoparticles, as a Potential New Nanocarrier for Oral Delivery of Tamoxifen10.3390/molecules262165071420-3049https://doaj.org/article/a6d6ee2b69a846b0bd87357dab1c2a3a2021-10-01T00:00:00Zhttps://www.mdpi.com/1420-3049/26/21/6507https://doaj.org/toc/1420-3049Tamoxifen citrate (TMC), a non-steroidal antiestrogen drug used for the treatment of breast cancer, was loaded in a block copolymer of maltoheptaose-<i>b</i>-polystyrene (MH-<i>b</i>-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<sup>−1</sup>) 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.Marcos Antonio VillettiAdryana Rocha ClementinoIlaria DottiPatricia Regina EbaniEride QuartaFrancesca ButtiniFabio SonvicoAnnalisa BiancheraRedouane BorsaliMDPI AGarticletamoxifen citrateblock copolymercytotoxicitybreast cancerOrganic chemistryQD241-441ENMolecules, Vol 26, Iss 6507, p 6507 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	tamoxifen citrate block copolymer cytotoxicity breast cancer Organic chemistry QD241-441
spellingShingle	tamoxifen citrate block copolymer cytotoxicity breast cancer Organic chemistry QD241-441 Marcos Antonio Villetti Adryana Rocha Clementino Ilaria Dotti Patricia Regina Ebani Eride Quarta Francesca Buttini Fabio Sonvico Annalisa Bianchera Redouane Borsali Design and Characterization of Maltoheptaose-<i>b</i>-Polystyrene Nanoparticles, as a Potential New Nanocarrier for Oral Delivery of Tamoxifen
description	Tamoxifen citrate (TMC), a non-steroidal antiestrogen drug used for the treatment of breast cancer, was loaded in a block copolymer of maltoheptaose-<i>b</i>-polystyrene (MH-<i>b</i>-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<sup>−1</sup>) 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.
format	article
author	Marcos Antonio Villetti Adryana Rocha Clementino Ilaria Dotti Patricia Regina Ebani Eride Quarta Francesca Buttini Fabio Sonvico Annalisa Bianchera Redouane Borsali
author_facet	Marcos Antonio Villetti Adryana Rocha Clementino Ilaria Dotti Patricia Regina Ebani Eride Quarta Francesca Buttini Fabio Sonvico Annalisa Bianchera Redouane Borsali
author_sort	Marcos Antonio Villetti
title	Design and Characterization of Maltoheptaose-<i>b</i>-Polystyrene Nanoparticles, as a Potential New Nanocarrier for Oral Delivery of Tamoxifen
title_short	Design and Characterization of Maltoheptaose-<i>b</i>-Polystyrene Nanoparticles, as a Potential New Nanocarrier for Oral Delivery of Tamoxifen
title_full	Design and Characterization of Maltoheptaose-<i>b</i>-Polystyrene Nanoparticles, as a Potential New Nanocarrier for Oral Delivery of Tamoxifen
title_fullStr	Design and Characterization of Maltoheptaose-<i>b</i>-Polystyrene Nanoparticles, as a Potential New Nanocarrier for Oral Delivery of Tamoxifen
title_full_unstemmed	Design and Characterization of Maltoheptaose-<i>b</i>-Polystyrene Nanoparticles, as a Potential New Nanocarrier for Oral Delivery of Tamoxifen
title_sort	design and characterization of maltoheptaose-<i>b</i>-polystyrene nanoparticles, as a potential new nanocarrier for oral delivery of tamoxifen
publisher	MDPI AG
publishDate	2021
url	https://doaj.org/article/a6d6ee2b69a846b0bd87357dab1c2a3a
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Design and Characterization of Maltoheptaose-<i>b</i>-Polystyrene Nanoparticles, as a Potential New Nanocarrier for Oral Delivery of Tamoxifen

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