Preparation and cytotoxicity of 2-methoxyestradiol-loaded solid lipid nanoparticles.
Anticancer Drugs
; 23(2): 185-90, 2012 Feb.
Article
em En
| MEDLINE
| ID: mdl-22027535
ABSTRACT
The objective of this study was to prepare 2-methoxyestradiol (2-ME)-loaded solid lipid nanoparticles (SLN) by hot homogenization-ultrasonication and evaluate their cytotoxicity on three cell lines, breast cancer [Michigan Cancer Foundation-7 (MCF-7)], prostatic carcinoma (PC-3), and glioma (SK-N-SH), by the sulforhodamineB method. The particle sizes and zeta potentials of the prepared SLN were around 120 nm and -40 mV, respectively. Differential scanning calorimetry (DSC) measurements revealed that the monostearin and 2-ME existed in solid and amorphous states in the SLN prepared, respectively. The high drug entrapment efficiency (>85%) indicated that most 2-ME was incorporated in the SLN. An in-vitro drug release study showed that 2-ME was released from the SLN in a slow but time-dependent manner. The cytotoxicity of 2-ME in SLN on each cell line was significantly enhanced compared with the solution. 2-ME SLN composed of Tween80 was approximately 17-fold more effective on PC-3 cells and 6.7-fold more effective on SK-N-SH cells than in the solution, whereas a lower sensitivity was achieved on MCF-7 cells. In each cell line, the cellular uptake percentages of 2-ME in SLN were much higher than the solution, respectively. In addition, surfactants may exert different effects on the cytotoxicity of 2-ME SLN depending on the cell line. The above assay demonstrated that SLN could significantly enhance the cytotoxicity of 2-ME compared with the free drug because of the increased cellular internalization and concentration of 2-ME. The results suggested that SLN could be an excellent carrier candidate to entrap 2-ME for improving the effectiveness of tumor chemotherapy.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Portadores de Fármacos
/
Estradiol
/
Nanopartículas
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Lipídeos
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Antineoplásicos
Limite:
Humans
Idioma:
En
Revista:
Anticancer Drugs
Ano de publicação:
2012
Tipo de documento:
Article