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

被引:4
|
作者
Villetti, Marcos Antonio [1 ]
Clementino, Adryana Rocha [2 ]
Dotti, Ilaria [3 ]
Ebani, Patricia Regina [1 ]
Quarta, Eride [3 ]
Buttini, Francesca [2 ,3 ]
Sonvico, Fabio [2 ,3 ]
Bianchera, Annalisa [2 ,3 ]
Borsali, Redouane [4 ]
机构
[1] Univ Fed Santa Maria, Dept Fis, Lab Espectroscopia & Polimeros Lepol, BR-97105900 Santa Maria, RS, Brazil
[2] Univ Parma, Biopharmanet TEC, I-43124 Parma, Italy
[3] Univ Parma, Dept Food & Drug, I-43124 Parma, Italy
[4] Univ Grenoble Alpes, CNRS, CERMAV, Dept Chem, F-38000 Grenoble, France
来源
MOLECULES | 2021年 / 26卷 / 21期
关键词
tamoxifen citrate; block copolymer; cytotoxicity; breast cancer; VITRO DRUG-RELEASE; IN-VITRO; POLYMERIC NANOPARTICLES; ZINC PHTHALOCYANINE; BLOCK-POLYSTYRENE; COPOLYMERS; PARAMETERS; SYSTEMS; POLY(EPSILON-CAPROLACTONE); CARAMELIZATION;
D O I
10.3390/molecules26216507
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
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 & PLUSMN; 6.8 mu g mL(-1)) and encapsulation efficiency (80.9 & PLUSMN; 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.
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页数:15
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